Cayman

Showing 14251–14400 of 45550 results

  • CB-1954 is a prodrug that is enzymatically activated to generate an antitumor agent that forms DNA-DNA interstrand crosslinks.{33004} In rat Walker 256 carcinoma cells, CB-1954 is reduced by NAD(P)H:quinone oxidoreductase (NQO1) to the cytotoxic derivative 5-(aziridin-1-yl)-4-hydroxylamineo 2 nitrobenzamide, a bifunctional alkylating agent.{33004}  

     

    Brand:
    Cayman
    SKU:21023 -

    Out of stock

  • CB-1954 is a prodrug that is enzymatically activated to generate an antitumor agent that forms DNA-DNA interstrand crosslinks.{33004} In rat Walker 256 carcinoma cells, CB-1954 is reduced by NAD(P)H:quinone oxidoreductase (NQO1) to the cytotoxic derivative 5-(aziridin-1-yl)-4-hydroxylamineo 2 nitrobenzamide, a bifunctional alkylating agent.{33004}  

     

    Brand:
    Cayman
    SKU:21023 -

    Out of stock

  • CB-25 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 5.2 and 13 nM, respectively. CB-25 behaves as an inverse agonist for the CB1 receptor as assessed in a cyclic AMP (cAMP) functional assay.{14815,14816}  

     

    Brand:
    Cayman
    SKU:10010116 - 1 mg

    Available on backorder

  • CB-25 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 5.2 and 13 nM, respectively. CB-25 behaves as an inverse agonist for the CB1 receptor as assessed in a cyclic AMP (cAMP) functional assay.{14815,14816}  

     

    Brand:
    Cayman
    SKU:10010116 - 10 mg

    Available on backorder

  • CB-25 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 5.2 and 13 nM, respectively. CB-25 behaves as an inverse agonist for the CB1 receptor as assessed in a cyclic AMP (cAMP) functional assay.{14815,14816}  

     

    Brand:
    Cayman
    SKU:10010116 - 5 mg

    Available on backorder

  • CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).{32505,32506} It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.{32505,32506}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).{32505,32506} It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.{32505,32506}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).{32505,32506} It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.{32505,32506}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).{32505,32506} It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.{32505,32506}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CB-52 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 210 and 30 nM, respectively.{14815} In vitro, CB-52 behaves primarily as a CB1 receptor partial agonist and a CB2 receptor neutral antagonist.{14816}  

     

    Brand:
    Cayman
    SKU:10010117 - 1 mg

    Available on backorder

  • CB-52 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 210 and 30 nM, respectively.{14815} In vitro, CB-52 behaves primarily as a CB1 receptor partial agonist and a CB2 receptor neutral antagonist.{14816}  

     

    Brand:
    Cayman
    SKU:10010117 - 10 mg

    Available on backorder

  • CB-52 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 210 and 30 nM, respectively.{14815} In vitro, CB-52 behaves primarily as a CB1 receptor partial agonist and a CB2 receptor neutral antagonist.{14816}  

     

    Brand:
    Cayman
    SKU:10010117 - 5 mg

    Available on backorder

  • CB-52 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 210 and 30 nM, respectively.{14815} In vitro, CB-52 behaves primarily as a CB1 receptor partial agonist and a CB2 receptor neutral antagonist.{14816}  

     

    Brand:
    Cayman
    SKU:10010117 - 50 mg

    Available on backorder

  • CB-7921220 is an inhibitor of the adenylyl cyclase (AC) isoforms AC1 and AC6.{38294} It is selective, reducing AC1 and AC6 activity by 60% while having no effect on AC2 and AC5 in Sf9 membranes stimulated by forskolin (Item No. 11018) when used at a concentration of 100 μM.  

     

    Brand:
    Cayman
    SKU:23332 - 1 mg

    Available on backorder

  • CB-7921220 is an inhibitor of the adenylyl cyclase (AC) isoforms AC1 and AC6.{38294} It is selective, reducing AC1 and AC6 activity by 60% while having no effect on AC2 and AC5 in Sf9 membranes stimulated by forskolin (Item No. 11018) when used at a concentration of 100 μM.  

     

    Brand:
    Cayman
    SKU:23332 - 10 mg

    Available on backorder

  • CB-7921220 is an inhibitor of the adenylyl cyclase (AC) isoforms AC1 and AC6.{38294} It is selective, reducing AC1 and AC6 activity by 60% while having no effect on AC2 and AC5 in Sf9 membranes stimulated by forskolin (Item No. 11018) when used at a concentration of 100 μM.  

     

    Brand:
    Cayman
    SKU:23332 - 25 mg

    Available on backorder

  • CB-7921220 is an inhibitor of the adenylyl cyclase (AC) isoforms AC1 and AC6.{38294} It is selective, reducing AC1 and AC6 activity by 60% while having no effect on AC2 and AC5 in Sf9 membranes stimulated by forskolin (Item No. 11018) when used at a concentration of 100 μM.  

     

    Brand:
    Cayman
    SKU:23332 - 5 mg

    Available on backorder

  • CB-839 is an orally bioavailable noncompetitive inhibitor of the glutaminase 1 (GLS1) splice variants, kidney-type (KGA) and glutaminase C (GAC), which convert glutamine into glutamate.{35064} CB-839 inhibits human recombinant GAC with IC50 values of less than 50 nM, varying based on the length of preincubation. It inhibits GLS1 activity in tissue homogenates (IC50s = 28 and 23 nM, respectively for brain and kidney), but it does not inhibit GLS2 (IC50 > 1,000 nM for liver). It possesses antiproliferative activity against the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (IC50s = 49 and 26 nM, respectively) but not against estrogen receptor-positive T47D cells (IC50 > 1,000 nM). In a patient-derived TNBC mouse xenograft model, CB-839 (200 mg/kg, p.o.) inhibits tumor growth by 61% relative to vehicle control. It also possesses antiproliferative properties in vitro against acute myeloid leukemia (AML) and in synergy with erlotinib (Item No. 10483) in EGFR-driven non-small cell lung cancer (NSCLC) in vitro and in xenografts.{35065,35066,35067}  

     

    Brand:
    Cayman
    SKU:22038 -

    Out of stock

  • CB-839 is an orally bioavailable noncompetitive inhibitor of the glutaminase 1 (GLS1) splice variants, kidney-type (KGA) and glutaminase C (GAC), which convert glutamine into glutamate.{35064} CB-839 inhibits human recombinant GAC with IC50 values of less than 50 nM, varying based on the length of preincubation. It inhibits GLS1 activity in tissue homogenates (IC50s = 28 and 23 nM, respectively for brain and kidney), but it does not inhibit GLS2 (IC50 > 1,000 nM for liver). It possesses antiproliferative activity against the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (IC50s = 49 and 26 nM, respectively) but not against estrogen receptor-positive T47D cells (IC50 > 1,000 nM). In a patient-derived TNBC mouse xenograft model, CB-839 (200 mg/kg, p.o.) inhibits tumor growth by 61% relative to vehicle control. It also possesses antiproliferative properties in vitro against acute myeloid leukemia (AML) and in synergy with erlotinib (Item No. 10483) in EGFR-driven non-small cell lung cancer (NSCLC) in vitro and in xenografts.{35065,35066,35067}  

     

    Brand:
    Cayman
    SKU:22038 -

    Out of stock

  • CB-839 is an orally bioavailable noncompetitive inhibitor of the glutaminase 1 (GLS1) splice variants, kidney-type (KGA) and glutaminase C (GAC), which convert glutamine into glutamate.{35064} CB-839 inhibits human recombinant GAC with IC50 values of less than 50 nM, varying based on the length of preincubation. It inhibits GLS1 activity in tissue homogenates (IC50s = 28 and 23 nM, respectively for brain and kidney), but it does not inhibit GLS2 (IC50 > 1,000 nM for liver). It possesses antiproliferative activity against the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (IC50s = 49 and 26 nM, respectively) but not against estrogen receptor-positive T47D cells (IC50 > 1,000 nM). In a patient-derived TNBC mouse xenograft model, CB-839 (200 mg/kg, p.o.) inhibits tumor growth by 61% relative to vehicle control. It also possesses antiproliferative properties in vitro against acute myeloid leukemia (AML) and in synergy with erlotinib (Item No. 10483) in EGFR-driven non-small cell lung cancer (NSCLC) in vitro and in xenografts.{35065,35066,35067}  

     

    Brand:
    Cayman
    SKU:22038 -

    Out of stock

  • CB-839 is an orally bioavailable noncompetitive inhibitor of the glutaminase 1 (GLS1) splice variants, kidney-type (KGA) and glutaminase C (GAC), which convert glutamine into glutamate.{35064} CB-839 inhibits human recombinant GAC with IC50 values of less than 50 nM, varying based on the length of preincubation. It inhibits GLS1 activity in tissue homogenates (IC50s = 28 and 23 nM, respectively for brain and kidney), but it does not inhibit GLS2 (IC50 > 1,000 nM for liver). It possesses antiproliferative activity against the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (IC50s = 49 and 26 nM, respectively) but not against estrogen receptor-positive T47D cells (IC50 > 1,000 nM). In a patient-derived TNBC mouse xenograft model, CB-839 (200 mg/kg, p.o.) inhibits tumor growth by 61% relative to vehicle control. It also possesses antiproliferative properties in vitro against acute myeloid leukemia (AML) and in synergy with erlotinib (Item No. 10483) in EGFR-driven non-small cell lung cancer (NSCLC) in vitro and in xenografts.{35065,35066,35067}  

     

    Brand:
    Cayman
    SKU:22038 -

    Out of stock

  • CB-86 is a resorcinol-anandamide hybrid compound that acts as a partial agonist for the central cannabinoid (CB1) receptor and a neutral antagonist for the peripheral cannabinoid (CB2) receptor with Ki values of 5.6 and 7.9 nM, respectively.{18014} Its demonstrated potency is similar to that of WIN 55,212-2 (Ki = 21 and 2.1 nM for CB1 and CB2, respectively).{18014} CB-86 (1 mg/kg) exhibits antinociceptive effects in mice treated with formalin.{18014}  

     

    Brand:
    Cayman
    SKU:-
  • CB-86 is a resorcinol-anandamide hybrid compound that acts as a partial agonist for the central cannabinoid (CB1) receptor and a neutral antagonist for the peripheral cannabinoid (CB2) receptor with Ki values of 5.6 and 7.9 nM, respectively.{18014} Its demonstrated potency is similar to that of WIN 55,212-2 (Ki = 21 and 2.1 nM for CB1 and CB2, respectively).{18014} CB-86 (1 mg/kg) exhibits antinociceptive effects in mice treated with formalin.{18014}  

     

    Brand:
    Cayman
    SKU:-
  • CB-86 is a resorcinol-anandamide hybrid compound that acts as a partial agonist for the central cannabinoid (CB1) receptor and a neutral antagonist for the peripheral cannabinoid (CB2) receptor with Ki values of 5.6 and 7.9 nM, respectively.{18014} Its demonstrated potency is similar to that of WIN 55,212-2 (Ki = 21 and 2.1 nM for CB1 and CB2, respectively).{18014} CB-86 (1 mg/kg) exhibits antinociceptive effects in mice treated with formalin.{18014}  

     

    Brand:
    Cayman
    SKU:-
  • CB-86 is a resorcinol-anandamide hybrid compound that acts as a partial agonist for the central cannabinoid (CB1) receptor and a neutral antagonist for the peripheral cannabinoid (CB2) receptor with Ki values of 5.6 and 7.9 nM, respectively.{18014} Its demonstrated potency is similar to that of WIN 55,212-2 (Ki = 21 and 2.1 nM for CB1 and CB2, respectively).{18014} CB-86 (1 mg/kg) exhibits antinociceptive effects in mice treated with formalin.{18014}  

     

    Brand:
    Cayman
    SKU:-
  • Immunogen: Synthetic peptide from the C-terminal region of human protein CB1 receptor • Host: rabbit • Species Reactivity: (+) human, mouse, and rat CB1 receptor • Application(s): IHC and WB • This antibody has been raised against the C-terminal (amino acids 461-472) intracellular region of the human CB1 receptor, a GPCR that binds the active component of cannabis, D9-tetrahydrocannabinol  

     

    Brand:
    Cayman
    SKU:10006590- 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the C-terminal region of human protein CB1 receptor • Host: rabbit • Species Reactivity: (+) human, mouse, and rat CB1 receptor • Application(s): IHC and WB • This antibody has been raised against the C-terminal (amino acids 461-472) intracellular region of the human CB1 receptor, a GPCR that binds the active component of cannabis, D9-tetrahydrocannabinol  

     

    Brand:
    Cayman
    SKU:10006590- 1 ea
  • The CB1 receptor is a G-protein coupled receptor that binds the active component of cannabis, Δ9-tetrahydrocannabinol. This antibody has been raised against the C-terminal (amino acids 461-472) intracellular region of the human CB1 receptor and can be used for western blotting.{6749,6747} Human and rat CB1 receptors exhibit 97.3% homology at the amino acid level over the complete protein, and 100% homology within the peptide sequence used to make this antibody.{6629,6628} This peptide exhibits no homology with the CB2 receptor. Based on the amino acid sequence, the CB1 receptor has a molecular weight of approximately 52,800.{6628} The CB1 receptor and the splice variant CB1a are localized mainly in the brain, whereas the CB2 receptor is localized predominantly in peripheral tissues, including the spleen and hemopoietic cells.{6629,6628,6726,6727}  

     

    Brand:
    Cayman
    SKU:10006590 - 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal extracellular region of human CB1 receptor • Species Reactivity: (+) Human, mouse, and rat • Host: Rabbit • Applications: WB and IHC  

     

    Brand:
    Cayman
    SKU:101500- 1 ea
  • The CB1 receptor and the splice variant CB1a are localized mainly in the brain.{6628,6726,6724} The CB1 receptor is a G-protein coupled receptor that binds the active component of cannabis, Δ9-tetrahydrocannabinol. Human and rat CB1 receptors exhibit 97.3% homology at the amino acid level over the complete protein, and 100% homology within the peptide sequence used to make this antibody.{6629,6628} This peptide exhibits no homology with the CB2 receptor. Based on the amino acid sequence, the CB1 receptor has a molecular weight of approximately 52,800.{6628} The CB1 receptor and the splice variant CB1a are localized mainly in the brain, whereas the CB2 receptor is localized predominantly in peripheral tissues, including the spleen and hemopoietic cells.{6629,6628,6726,6724} Cayman’s CB1 Receptor Polyclonal Antibody can be used for Western blot and immunohistochemistry applications. The antibody recognizes the N-terminal extracellular region of the CB1 receptor at 40 kDa from human samples.  

     

    Brand:
    Cayman
    SKU:101500 - 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal extracellular region of human CB1 receptor • Species Reactivity: (+) Human, mouse, and rat • Host: Rabbit • Applications: WB and IHC  

     

    Brand:
    Cayman
    SKU:101500- 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal region of human CB2 receptor • Host: Rabbit • Species Reactivity: (+) Human and mouse • Cross Reactivity: (+) CB2 receptor • Applications: IHC and WB  

     

    Brand:
    Cayman
    SKU:101550- 1 ea
  • The CB2 receptor is localized predominantly in peripheral tissues, including the spleen and hemopoietic cells.{6724} · The CB1 and CB2 receptors are G-protein coupled receptors that bind the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide which is an endogenous CB receptor ligand. This antibody has been raised against a sequence between the N-terminus and the first transmembrane domain of the protein of the human CB2 receptor.{6724} It can be used for western blotting and immunohistochemistry applications. Conserved amino acids between the CB1 and CB2 receptors in this region are minimal.{6727} Human and murine CB2 receptors exhibit 82% homology at the amino acid level over the complete protein.{6727} The CB2 receptor is localized predominantly in peripheral tissues, including the spleen and hemopoietic cells.{6724}  

     

    Brand:
    Cayman
    SKU:101550 - 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal region of human CB2 receptor • Host: Rabbit • Species Reactivity: (+) Human and mouse • Cross Reactivity: (+) CB2 receptor • Applications: IHC and WB  

     

    Brand:
    Cayman
    SKU:101550- 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal region of human CB2 receptor • Host: Rabbit • Species Reactivity: (+) Human • Applications: FC and IF  

     

    Brand:
    Cayman
    SKU:10010712- 500 µl
  • The central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors are G protein-coupled receptors (GPCRs) that bind the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide which is an endogenous CB receptor ligand. This antibody has been raised against a sequence between the N-terminal and the first transmembrane domain of the protein of the human CB2 receptor.{6724} Conserved amino acids between the CB1 and CB2 receptors in this region are minimal.{6727} Human and mouse CB2 receptors exhibit 82% homology at the amino acid level over the complete protein.{6727} The CB2 receptor is localized predominantly in peripheral tissues, including the spleen and hemopoietic cells.{6724}  

     

    Brand:
    Cayman
    SKU:10010712 - 500 µl

    Available on backorder

  • Immunogen: Synthetic peptide from the N-terminal region of human CB2 receptor • Host: Rabbit • Species Reactivity: (+) Human • Applications: FC and IF  

     

    Brand:
    Cayman
    SKU:10010712- 500 µl

    Available on backorder

  • CBDB (Item No. 29031) is an analytical reference standard categorized as a phytocannabinoid.{50945} CBDB has been found in strains of cannabis and hemp.{50945,50420} CBDB is considered an impurity in commercial extractions of cannabidiol (CBD) from hemp.{50420} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the US.  

     

    Brand:
    Cayman
    SKU:29031 - 1 mg

    Available on backorder

  • CBDB (Item No. 29031) is an analytical reference standard categorized as a phytocannabinoid.{50945} CBDB has been found in strains of cannabis and hemp.{50945,50420} CBDB is considered an impurity in commercial extractions of cannabidiol (CBD) from hemp.{50420} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the US.  

     

    Brand:
    Cayman
    SKU:29031 - 5 mg

    Available on backorder

  • CBDP (Item No. 30169) is an analytical reference standard categorized as a phytocannabinoid.{45824} It is a bis-homolog of cannabidiol (Item Nos. 90080 | ISO60156) that has been found in certain strains of Cannabis.{50948} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the US.  

     

    Brand:
    Cayman
    SKU:30169 - 1 mg

    Available on backorder

  • CBDP (Item No. 30169) is an analytical reference standard categorized as a phytocannabinoid.{45824} It is a bis-homolog of cannabidiol (Item Nos. 90080 | ISO60156) that has been found in certain strains of Cannabis.{50948} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the US.  

     

    Brand:
    Cayman
    SKU:30169 - 5 mg

    Available on backorder

  • Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ.{27439} CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias.{27439,27440} CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 µM).{27441} It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.{27441}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ.{27439} CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias.{27439,27440} CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 µM).{27441} It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.{27441}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ.{27439} CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias.{27439,27440} CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 µM).{27441} It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.{27441}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • CBGQ is an analytical reference standard categorized as an oxidative product of cannabigerol (CBG; Item Nos. 20164 | 15293).{53781} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the U.S.  

     

    Brand:
    Cayman
    SKU:30862 - 1 mg

    Available on backorder

  • CBGQ is an analytical reference standard categorized as an oxidative product of cannabigerol (CBG; Item Nos. 20164 | 15293).{53781} This product is intended for research and forensic applications. This item has been tested to contain ≤0.3% Δ9-THC on a dry weight basis meeting the 2018 Farm Bill requirements to be a non-controlled substance in the U.S.  

     

    Brand:
    Cayman
    SKU:30862 - 5 mg

    Available on backorder

  • Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. Importantly, HDAC inhibitors induce apoptosis in some cancer cells and show promise in the treatment of certain forms of cancer. CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively.{17174} CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM){17175} and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg.{17176} The efficacy of CBHA for suppressing tumor growth in mice is enhanced by the addition of retinoic acid.{17176}  

     

    Brand:
    Cayman
    SKU:-
  • Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. Importantly, HDAC inhibitors induce apoptosis in some cancer cells and show promise in the treatment of certain forms of cancer. CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively.{17174} CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM){17175} and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg.{17176} The efficacy of CBHA for suppressing tumor growth in mice is enhanced by the addition of retinoic acid.{17176}  

     

    Brand:
    Cayman
    SKU:-
  • Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. Importantly, HDAC inhibitors induce apoptosis in some cancer cells and show promise in the treatment of certain forms of cancer. CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively.{17174} CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM){17175} and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg.{17176} The efficacy of CBHA for suppressing tumor growth in mice is enhanced by the addition of retinoic acid.{17176}  

     

    Brand:
    Cayman
    SKU:-
  • CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity.{30977} CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 value of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity.{30977} CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 value of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity.{30977} CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 value of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBR-5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 µM.{30606} It does not affect other NAD+-dependent dehydrogenases, including lactate dehydrogenase and malate dehydrogenase 1. CBR-5884 inhibits the proliferation of cancer cells by blocking de novo serine synthesis and is selectively cytotoxic for cells with high serine biosynthetic activity.{30606}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBR-5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 µM.{30606} It does not affect other NAD+-dependent dehydrogenases, including lactate dehydrogenase and malate dehydrogenase 1. CBR-5884 inhibits the proliferation of cancer cells by blocking de novo serine synthesis and is selectively cytotoxic for cells with high serine biosynthetic activity.{30606}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBR-5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 µM.{30606} It does not affect other NAD+-dependent dehydrogenases, including lactate dehydrogenase and malate dehydrogenase 1. CBR-5884 inhibits the proliferation of cancer cells by blocking de novo serine synthesis and is selectively cytotoxic for cells with high serine biosynthetic activity.{30606}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CBR-5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 µM.{30606} It does not affect other NAD+-dependent dehydrogenases, including lactate dehydrogenase and malate dehydrogenase 1. CBR-5884 inhibits the proliferation of cancer cells by blocking de novo serine synthesis and is selectively cytotoxic for cells with high serine biosynthetic activity.{30606}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-115 is a potent dual inhibitor of mTOR and DNA-PK (IC50s = 22 and 15 nM, respectively).{34733} CC-115 reduces PC3 cancer cell growth in vitro (IC50 = 138 nM) and exhibits effective reduction of murine PC3 tumor xenografts (mEC50 = 1 mg/kg). In a Phase I clinical trial, formulations containing CC-115 reduced lymph node sizes in almost all patients with chronic lymphocytic leukemia (CLL) that also have ataxia telangiectasia mutated (ATM) kinase deletions.{34734}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-115 is a potent dual inhibitor of mTOR and DNA-PK (IC50s = 22 and 15 nM, respectively).{34733} CC-115 reduces PC3 cancer cell growth in vitro (IC50 = 138 nM) and exhibits effective reduction of murine PC3 tumor xenografts (mEC50 = 1 mg/kg). In a Phase I clinical trial, formulations containing CC-115 reduced lymph node sizes in almost all patients with chronic lymphocytic leukemia (CLL) that also have ataxia telangiectasia mutated (ATM) kinase deletions.{34734}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-115 is a potent dual inhibitor of mTOR and DNA-PK (IC50s = 22 and 15 nM, respectively).{34733} CC-115 reduces PC3 cancer cell growth in vitro (IC50 = 138 nM) and exhibits effective reduction of murine PC3 tumor xenografts (mEC50 = 1 mg/kg). In a Phase I clinical trial, formulations containing CC-115 reduced lymph node sizes in almost all patients with chronic lymphocytic leukemia (CLL) that also have ataxia telangiectasia mutated (ATM) kinase deletions.{34734}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-115 is a potent dual inhibitor of mTOR and DNA-PK (IC50s = 22 and 15 nM, respectively).{34733} CC-115 reduces PC3 cancer cell growth in vitro (IC50 = 138 nM) and exhibits effective reduction of murine PC3 tumor xenografts (mEC50 = 1 mg/kg). In a Phase I clinical trial, formulations containing CC-115 reduced lymph node sizes in almost all patients with chronic lymphocytic leukemia (CLL) that also have ataxia telangiectasia mutated (ATM) kinase deletions.{34734}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-122 is a pleiotropic pathway modifier with anticancer activity.{50163} It binds to cereblon, a substrate receptor protein of the Cullin 4 RING E3 ubiquitin ligase complex, in U266 multiple myeloma cell extracts and induces recruitment and degradation of the cereblon substrates Aiolos and Ikaros in TMD8, OCI-LY10, and Karpas 422 diffuse large B cell lymphoma (DLBCL) cells when used at concentrations of 0.1, 1, and 10 μM. CC-122 (0.1-10,000 nM) decreases proliferation and induces apoptosis in activated B cell (ABC) and germinal center B cell (GCB) DLBCL cell lines. It also stimulates IL-2 production in mouse primary T cells. CC-122 (30 mg/kg) decreases tumor levels of Aiolos and Ikaros and reduces tumor growth in OCI-LY10 ABC DLBCL and WSU-DLCL2 GCB DLBCL mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26257 - 1 mg

    Available on backorder

  • CC-122 is a pleiotropic pathway modifier with anticancer activity.{50163} It binds to cereblon, a substrate receptor protein of the Cullin 4 RING E3 ubiquitin ligase complex, in U266 multiple myeloma cell extracts and induces recruitment and degradation of the cereblon substrates Aiolos and Ikaros in TMD8, OCI-LY10, and Karpas 422 diffuse large B cell lymphoma (DLBCL) cells when used at concentrations of 0.1, 1, and 10 μM. CC-122 (0.1-10,000 nM) decreases proliferation and induces apoptosis in activated B cell (ABC) and germinal center B cell (GCB) DLBCL cell lines. It also stimulates IL-2 production in mouse primary T cells. CC-122 (30 mg/kg) decreases tumor levels of Aiolos and Ikaros and reduces tumor growth in OCI-LY10 ABC DLBCL and WSU-DLCL2 GCB DLBCL mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26257 - 10 mg

    Available on backorder

  • CC-122 is a pleiotropic pathway modifier with anticancer activity.{50163} It binds to cereblon, a substrate receptor protein of the Cullin 4 RING E3 ubiquitin ligase complex, in U266 multiple myeloma cell extracts and induces recruitment and degradation of the cereblon substrates Aiolos and Ikaros in TMD8, OCI-LY10, and Karpas 422 diffuse large B cell lymphoma (DLBCL) cells when used at concentrations of 0.1, 1, and 10 μM. CC-122 (0.1-10,000 nM) decreases proliferation and induces apoptosis in activated B cell (ABC) and germinal center B cell (GCB) DLBCL cell lines. It also stimulates IL-2 production in mouse primary T cells. CC-122 (30 mg/kg) decreases tumor levels of Aiolos and Ikaros and reduces tumor growth in OCI-LY10 ABC DLBCL and WSU-DLCL2 GCB DLBCL mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26257 - 25 mg

    Available on backorder

  • CC-122 is a pleiotropic pathway modifier with anticancer activity.{50163} It binds to cereblon, a substrate receptor protein of the Cullin 4 RING E3 ubiquitin ligase complex, in U266 multiple myeloma cell extracts and induces recruitment and degradation of the cereblon substrates Aiolos and Ikaros in TMD8, OCI-LY10, and Karpas 422 diffuse large B cell lymphoma (DLBCL) cells when used at concentrations of 0.1, 1, and 10 μM. CC-122 (0.1-10,000 nM) decreases proliferation and induces apoptosis in activated B cell (ABC) and germinal center B cell (GCB) DLBCL cell lines. It also stimulates IL-2 production in mouse primary T cells. CC-122 (30 mg/kg) decreases tumor levels of Aiolos and Ikaros and reduces tumor growth in OCI-LY10 ABC DLBCL and WSU-DLCL2 GCB DLBCL mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26257 - 5 mg

    Available on backorder

  • CC-223 is a potent inhibitor of mTOR (IC50 = 16 nM) that shows selectivity for mTOR over a panel of 246 other kinases.{33446} It blocks signaling through both mTORC1 and mTORC2, inhibiting the phosphorylation of S6RP, 4EBP1, and Akt(S473) in cellular systems.{33446} CC-223 inhibits growth and induces apoptosis in hematologic and solid tumor cell lines in vitro, and it exhibits dose-dependent tumor growth inhibition in multiple solid tumor xenografts in vivo.{33446}  

     

    Brand:
    Cayman
    SKU:19917 -

    Available on backorder

  • CC-223 is a potent inhibitor of mTOR (IC50 = 16 nM) that shows selectivity for mTOR over a panel of 246 other kinases.{33446} It blocks signaling through both mTORC1 and mTORC2, inhibiting the phosphorylation of S6RP, 4EBP1, and Akt(S473) in cellular systems.{33446} CC-223 inhibits growth and induces apoptosis in hematologic and solid tumor cell lines in vitro, and it exhibits dose-dependent tumor growth inhibition in multiple solid tumor xenografts in vivo.{33446}  

     

    Brand:
    Cayman
    SKU:19917 -

    Available on backorder

  • CC-223 is a potent inhibitor of mTOR (IC50 = 16 nM) that shows selectivity for mTOR over a panel of 246 other kinases.{33446} It blocks signaling through both mTORC1 and mTORC2, inhibiting the phosphorylation of S6RP, 4EBP1, and Akt(S473) in cellular systems.{33446} CC-223 inhibits growth and induces apoptosis in hematologic and solid tumor cell lines in vitro, and it exhibits dose-dependent tumor growth inhibition in multiple solid tumor xenografts in vivo.{33446}  

     

    Brand:
    Cayman
    SKU:19917 -

    Available on backorder

  • CC-223 is a potent inhibitor of mTOR (IC50 = 16 nM) that shows selectivity for mTOR over a panel of 246 other kinases.{33446} It blocks signaling through both mTORC1 and mTORC2, inhibiting the phosphorylation of S6RP, 4EBP1, and Akt(S473) in cellular systems.{33446} CC-223 inhibits growth and induces apoptosis in hematologic and solid tumor cell lines in vitro, and it exhibits dose-dependent tumor growth inhibition in multiple solid tumor xenografts in vivo.{33446}  

     

    Brand:
    Cayman
    SKU:19917 -

    Available on backorder

  • c-Jun N-terminal kinases (JNKs) are MAP kinase family members that become highly activated after cells are exposed to stress conditions and are poorly activated by exposure to growth factors or mitogens.{17156} CC-401 is a potent inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM).{30558,30557} It has at least 40-fold selectivity for JNK compared with other related kinases. CC-401 is bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model.{30557} It also has been shown to decrease hepatic necrosis and apoptosis after orthotopic liver transplantation and prevent acute renal failure following ischemia/reperfusion associated with renal transplantation in rats.{30558,30556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • c-Jun N-terminal kinases (JNKs) are MAP kinase family members that become highly activated after cells are exposed to stress conditions and are poorly activated by exposure to growth factors or mitogens.{17156} CC-401 is a potent inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM).{30558,30557} It has at least 40-fold selectivity for JNK compared with other related kinases. CC-401 is bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model.{30557} It also has been shown to decrease hepatic necrosis and apoptosis after orthotopic liver transplantation and prevent acute renal failure following ischemia/reperfusion associated with renal transplantation in rats.{30558,30556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • c-Jun N-terminal kinases (JNKs) are MAP kinase family members that become highly activated after cells are exposed to stress conditions and are poorly activated by exposure to growth factors or mitogens.{17156} CC-401 is a potent inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM).{30558,30557} It has at least 40-fold selectivity for JNK compared with other related kinases. CC-401 is bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model.{30557} It also has been shown to decrease hepatic necrosis and apoptosis after orthotopic liver transplantation and prevent acute renal failure following ischemia/reperfusion associated with renal transplantation in rats.{30558,30556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CC-671 is a dual inhibitor of the spindle assembly checkpoint kinase Mps1/TTK and Cdc2-like kinase (Clk2; IC50s = 5 and 3 nM, respectively).{49100} It is selective for Mps1/TTK and Clk2 over a panel of 255 kinases at 3 μM, but does inhibit DYRK3, DYRK1A, PHKG, DYRK1B, and Clk1 (IC50s = 99, 104, 136, 157, and 300 nM, respectively). CC-671 selectively inhibits the growth of Cal-51 triple negative breast cancer (TNBC) cells over BT-474 luminal breast cancer cells (IC50s = 60 and 6,970 nM, respectively). In vivo, CC-671 (20 mg/kg) reduces tumor volume in a Cal-51 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:26184 - 1 mg

    Available on backorder

  • CC-671 is a dual inhibitor of the spindle assembly checkpoint kinase Mps1/TTK and Cdc2-like kinase (Clk2; IC50s = 5 and 3 nM, respectively).{49100} It is selective for Mps1/TTK and Clk2 over a panel of 255 kinases at 3 μM, but does inhibit DYRK3, DYRK1A, PHKG, DYRK1B, and Clk1 (IC50s = 99, 104, 136, 157, and 300 nM, respectively). CC-671 selectively inhibits the growth of Cal-51 triple negative breast cancer (TNBC) cells over BT-474 luminal breast cancer cells (IC50s = 60 and 6,970 nM, respectively). In vivo, CC-671 (20 mg/kg) reduces tumor volume in a Cal-51 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:26184 - 10 mg

    Available on backorder

  • CC-671 is a dual inhibitor of the spindle assembly checkpoint kinase Mps1/TTK and Cdc2-like kinase (Clk2; IC50s = 5 and 3 nM, respectively).{49100} It is selective for Mps1/TTK and Clk2 over a panel of 255 kinases at 3 μM, but does inhibit DYRK3, DYRK1A, PHKG, DYRK1B, and Clk1 (IC50s = 99, 104, 136, 157, and 300 nM, respectively). CC-671 selectively inhibits the growth of Cal-51 triple negative breast cancer (TNBC) cells over BT-474 luminal breast cancer cells (IC50s = 60 and 6,970 nM, respectively). In vivo, CC-671 (20 mg/kg) reduces tumor volume in a Cal-51 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:26184 - 5 mg

    Available on backorder

  • CC-885 is a modulator of the E3 ligase protein cereblon with antiproliferative effects on human myeloid leukemia cell lines.{31560} It forms a complex with cereblon and the cell cycle regulator and translation termination factor GSPT1.{31560} The antitumour activity of CC-885 relies on cereblon-dependent ubiquitination and degradation of the GSPT1.{31560}  

     

    Brand:
    Cayman
    SKU:19966 -

    Available on backorder

  • CC-885 is a modulator of the E3 ligase protein cereblon with antiproliferative effects on human myeloid leukemia cell lines.{31560} It forms a complex with cereblon and the cell cycle regulator and translation termination factor GSPT1.{31560} The antitumour activity of CC-885 relies on cereblon-dependent ubiquitination and degradation of the GSPT1.{31560}  

     

    Brand:
    Cayman
    SKU:19966 -

    Available on backorder

  • CC-885 is a modulator of the E3 ligase protein cereblon with antiproliferative effects on human myeloid leukemia cell lines.{31560} It forms a complex with cereblon and the cell cycle regulator and translation termination factor GSPT1.{31560} The antitumour activity of CC-885 relies on cereblon-dependent ubiquitination and degradation of the GSPT1.{31560}  

     

    Brand:
    Cayman
    SKU:19966 -

    Available on backorder

  • CC-885 is a modulator of the E3 ligase protein cereblon with antiproliferative effects on human myeloid leukemia cell lines.{31560} It forms a complex with cereblon and the cell cycle regulator and translation termination factor GSPT1.{31560} The antitumour activity of CC-885 relies on cereblon-dependent ubiquitination and degradation of the GSPT1.{31560}  

     

    Brand:
    Cayman
    SKU:19966 -

    Available on backorder

  • CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.  

     

    Brand:
    Cayman
    SKU:22466 -

    Out of stock

  • CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.  

     

    Brand:
    Cayman
    SKU:22466 -

    Out of stock

  • CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.  

     

    Brand:
    Cayman
    SKU:22466 -

    Out of stock

  • CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.  

     

    Brand:
    Cayman
    SKU:22466 -

    Out of stock

  • CCCP is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential.{39958} It inhibits mitochondrial respiration and ATPase activity when used at concentrations of 110 and 35 nM, respectively.{39959} CCCP inhibits activation of stimulation of interferon genes (STING), decreasing the expression of downstream STING targets, including IFN-β, TBK1, and IRF3 when used at a concentration of 50 µM in RAW 264.7 cells.{39960} It induces mitochondrial fission in a manner dependent on the GTPase Drp1. CCCP (4 mg/kg) increases body temperature as well as left ventricular systolic and diastolic dimensions and decreases fractional shortening in rats.{39961} It also increases myocardial glucose and fatty acid uptake in rats.  

     

    Brand:
    Cayman
    SKU:25458 - 100 mg

    Available on backorder

  • CCCP is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential.{39958} It inhibits mitochondrial respiration and ATPase activity when used at concentrations of 110 and 35 nM, respectively.{39959} CCCP inhibits activation of stimulation of interferon genes (STING), decreasing the expression of downstream STING targets, including IFN-β, TBK1, and IRF3 when used at a concentration of 50 µM in RAW 264.7 cells.{39960} It induces mitochondrial fission in a manner dependent on the GTPase Drp1. CCCP (4 mg/kg) increases body temperature as well as left ventricular systolic and diastolic dimensions and decreases fractional shortening in rats.{39961} It also increases myocardial glucose and fatty acid uptake in rats.  

     

    Brand:
    Cayman
    SKU:25458 - 250 mg

    Available on backorder

  • CCCP is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential.{39958} It inhibits mitochondrial respiration and ATPase activity when used at concentrations of 110 and 35 nM, respectively.{39959} CCCP inhibits activation of stimulation of interferon genes (STING), decreasing the expression of downstream STING targets, including IFN-β, TBK1, and IRF3 when used at a concentration of 50 µM in RAW 264.7 cells.{39960} It induces mitochondrial fission in a manner dependent on the GTPase Drp1. CCCP (4 mg/kg) increases body temperature as well as left ventricular systolic and diastolic dimensions and decreases fractional shortening in rats.{39961} It also increases myocardial glucose and fatty acid uptake in rats.  

     

    Brand:
    Cayman
    SKU:25458 - 500 mg

    Available on backorder

  • CCF-642 is an inhibitor of protein disulfide isomerase (PDI).{48409} It inhibits the reducing capacity of PDI when used at a concentration of 1 µM. It inhibits proliferation in ten multiple myeloma cell lines with IC50 values of less than 1 µM. It is cytotoxic to primary cells isolated from patients with refractory myeloma who developed secondary plasma cell leukemia (IC50 = <1 µM) but not to normal bone marrow mononuclear (NLBM) cells up to a concentration of 6.75 µM. CCF-642 (3 µM) also induces acute endoplasmic reticulum (ER) stress, increasing ERK phosphorylation and dimerization of IRE1-α, indicating an increase in the amount of misfolded ER proteins. It increases calcium accumulation and cleaved caspase-3 in MM1.S cells and induces apoptosis. CCF-642 increases survival in a 5TGM1 mouse syngeneic model of myeloma when administered at a dose of 10 mg/kg three times per week.  

     

    Brand:
    Cayman
    SKU:27054 - 1 mg

    Available on backorder

  • CCF-642 is an inhibitor of protein disulfide isomerase (PDI).{48409} It inhibits the reducing capacity of PDI when used at a concentration of 1 µM. It inhibits proliferation in ten multiple myeloma cell lines with IC50 values of less than 1 µM. It is cytotoxic to primary cells isolated from patients with refractory myeloma who developed secondary plasma cell leukemia (IC50 = <1 µM) but not to normal bone marrow mononuclear (NLBM) cells up to a concentration of 6.75 µM. CCF-642 (3 µM) also induces acute endoplasmic reticulum (ER) stress, increasing ERK phosphorylation and dimerization of IRE1-α, indicating an increase in the amount of misfolded ER proteins. It increases calcium accumulation and cleaved caspase-3 in MM1.S cells and induces apoptosis. CCF-642 increases survival in a 5TGM1 mouse syngeneic model of myeloma when administered at a dose of 10 mg/kg three times per week.  

     

    Brand:
    Cayman
    SKU:27054 - 10 mg

    Available on backorder

  • CCF-642 is an inhibitor of protein disulfide isomerase (PDI).{48409} It inhibits the reducing capacity of PDI when used at a concentration of 1 µM. It inhibits proliferation in ten multiple myeloma cell lines with IC50 values of less than 1 µM. It is cytotoxic to primary cells isolated from patients with refractory myeloma who developed secondary plasma cell leukemia (IC50 = <1 µM) but not to normal bone marrow mononuclear (NLBM) cells up to a concentration of 6.75 µM. CCF-642 (3 µM) also induces acute endoplasmic reticulum (ER) stress, increasing ERK phosphorylation and dimerization of IRE1-α, indicating an increase in the amount of misfolded ER proteins. It increases calcium accumulation and cleaved caspase-3 in MM1.S cells and induces apoptosis. CCF-642 increases survival in a 5TGM1 mouse syngeneic model of myeloma when administered at a dose of 10 mg/kg three times per week.  

     

    Brand:
    Cayman
    SKU:27054 - 25 mg

    Available on backorder

  • CCF-642 is an inhibitor of protein disulfide isomerase (PDI).{48409} It inhibits the reducing capacity of PDI when used at a concentration of 1 µM. It inhibits proliferation in ten multiple myeloma cell lines with IC50 values of less than 1 µM. It is cytotoxic to primary cells isolated from patients with refractory myeloma who developed secondary plasma cell leukemia (IC50 = <1 µM) but not to normal bone marrow mononuclear (NLBM) cells up to a concentration of 6.75 µM. CCF-642 (3 µM) also induces acute endoplasmic reticulum (ER) stress, increasing ERK phosphorylation and dimerization of IRE1-α, indicating an increase in the amount of misfolded ER proteins. It increases calcium accumulation and cleaved caspase-3 in MM1.S cells and induces apoptosis. CCF-642 increases survival in a 5TGM1 mouse syngeneic model of myeloma when administered at a dose of 10 mg/kg three times per week.  

     

    Brand:
    Cayman
    SKU:27054 - 5 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding.{15012} CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 µM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.{19162}  

     

    Brand:
    Cayman
    SKU:10787 - 10 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding.{15012} CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 µM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.{19162}  

     

    Brand:
    Cayman
    SKU:10787 - 25 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding.{15012} CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 µM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.{19162}  

     

    Brand:
    Cayman
    SKU:10787 - 5 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding.{15012} CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 µM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.{19162}  

     

    Brand:
    Cayman
    SKU:10787 - 50 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.{15012} It inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Gα13 with an IC50 value of 1 µM. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines at nanomolar to low micromolar concentrations.{15012}  

     

    Brand:
    Cayman
    SKU:10010350 - 10 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.{15012} It inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Gα13 with an IC50 value of 1 µM. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines at nanomolar to low micromolar concentrations.{15012}  

     

    Brand:
    Cayman
    SKU:10010350 - 25 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.{15012} It inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Gα13 with an IC50 value of 1 µM. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines at nanomolar to low micromolar concentrations.{15012}  

     

    Brand:
    Cayman
    SKU:10010350 - 5 mg

    Available on backorder

  • The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.{15012} It inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Gα13 with an IC50 value of 1 µM. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines at nanomolar to low micromolar concentrations.{15012}  

     

    Brand:
    Cayman
    SKU:10010350 - 50 mg

    Available on backorder

  • Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).{15012} The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.{15012} CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.{25536} This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.{25536} CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.{25536} It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.{25536}  

     

    Brand:
    Cayman
    SKU:-
  • Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).{15012} The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.{15012} CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.{25536} This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.{25536} CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.{25536} It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.{25536}  

     

    Brand:
    Cayman
    SKU:-
  • Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).{15012} The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.{15012} CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.{25536} This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.{25536} CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.{25536} It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.{25536}  

     

    Brand:
    Cayman
    SKU:-
  • Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).{15012} The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.{15012} CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.{25536} This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.{25536} CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.{25536} It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.{25536}  

     

    Brand:
    Cayman
    SKU:-
  • CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively).{58101} It is selective for GRKs over protein kinase A (PKA; IC50 = 120 μM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 μM, respectively).{58102}  

     

    Brand:
    Cayman
    SKU:31120 - 1 mg

    Available on backorder

  • CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively).{58101} It is selective for GRKs over protein kinase A (PKA; IC50 = 120 μM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 μM, respectively).{58102}  

     

    Brand:
    Cayman
    SKU:31120 - 10 mg

    Available on backorder

  • CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively).{58101} It is selective for GRKs over protein kinase A (PKA; IC50 = 120 μM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 μM, respectively).{58102}  

     

    Brand:
    Cayman
    SKU:31120 - 25 mg

    Available on backorder

  • CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively).{58101} It is selective for GRKs over protein kinase A (PKA; IC50 = 120 μM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 μM, respectively).{58102}  

     

    Brand:
    Cayman
    SKU:31120 - 5 mg

    Available on backorder

  • CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971 (Item No. 15075).{35196} CCG-232601 inhibits MRTF-dependent transcription in HEK293T cells (IC50 = 0.55 µM in a luciferase reporter assay). It also reduces expression of α-smooth muscle actin (α-SMA) in TGF-β-stimulated human dermal fibroblasts to 31% of control when used at a concentration of 10 µM. CCG-232601 (50 mg/kg) inhibits increases in dermal thickness and hydroxyproline content in a mouse model of dermal fibrosis induced by bleomycin (Item No. 13877).  

     

    Brand:
    Cayman
    SKU:24382 - 1 mg

    Available on backorder

  • CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971 (Item No. 15075).{35196} CCG-232601 inhibits MRTF-dependent transcription in HEK293T cells (IC50 = 0.55 µM in a luciferase reporter assay). It also reduces expression of α-smooth muscle actin (α-SMA) in TGF-β-stimulated human dermal fibroblasts to 31% of control when used at a concentration of 10 µM. CCG-232601 (50 mg/kg) inhibits increases in dermal thickness and hydroxyproline content in a mouse model of dermal fibrosis induced by bleomycin (Item No. 13877).  

     

    Brand:
    Cayman
    SKU:24382 - 5 mg

    Available on backorder

  • CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins.{19235} RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins.{19235} CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.{19235}  

     

    Brand:
    Cayman
    SKU:10802 - 1 mg

    Available on backorder

  • CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins.{19235} RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins.{19235} CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.{19235}  

     

    Brand:
    Cayman
    SKU:10802 - 10 mg

    Available on backorder

  • CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins.{19235} RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins.{19235} CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.{19235}  

     

    Brand:
    Cayman
    SKU:10802 - 5 mg

    Available on backorder

  • CCK (26-30) is an N-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} The sulfated form of CCK (26-30) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 10% when used at a concentration of 0.1 mM.{38952}  

     

    Brand:
    Cayman
    SKU:24949 - 1 mg

    Available on backorder

  • CCK (26-30) is an N-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} The sulfated form of CCK (26-30) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 10% when used at a concentration of 0.1 mM.{38952}  

     

    Brand:
    Cayman
    SKU:24949 - 5 mg

    Available on backorder

  • CCK (26-30) is an N-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} The sulfated form of CCK (26-30) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 10% when used at a concentration of 0.1 mM.{38952}  

     

    Brand:
    Cayman
    SKU:24949 - 500 µg

    Available on backorder

  • CCK (26-31) is an N-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606}  

     

    Brand:
    Cayman
    SKU:24951 - 1 mg

    Available on backorder

  • CCK (26-31) is an N-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} The sulfated form of CCK (26-31) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 21% when used at a concentration of 0.1 mM.{38952}  

     

    Brand:
    Cayman
    SKU:24950 - 1 mg

    Available on backorder

  • CCK (27-33) is a C-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 µM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 µM), an effect that can be reversed by naloxone.{39623} Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in mice when administered at doses up to 1 µmol/kg.{39624}  

     

    Brand:
    Cayman
    SKU:24952 - 1 mg

    Available on backorder

  • CCK (27-33) is a C-terminal fragment of CCK (Item Nos. 23371 | 24404), a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 µM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 µM), an effect that can be reversed by naloxone.{39623} Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in mice when administered at doses up to 1 µmol/kg.{39624}  

     

    Brand:
    Cayman
    SKU:24952 - 500 µg

    Available on backorder

  • Cholecystokinin (CCK) octapeptide is a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} It is a cleaved product of the full CCK preprohormone that is more potent than the full length enzyme in stimulating contraction of guinea pig gallbladder but with a shorter duration.{40606,40716} CCK octapeptide (sulfated) is 300-fold more active than the non-sulfated CCK octapeptide (Item No. 24404).{40606}  

     

    Brand:
    Cayman
    SKU:23371 - 1 mg

    Available on backorder

  • Cholecystokinin (CCK) octapeptide is a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} It is a cleaved product of the full CCK preprohormone that is more potent than the full length enzyme in stimulating contraction of guinea pig gallbladder but with a shorter duration.{40606,40716} CCK octapeptide (sulfated) is 300-fold more active than the non-sulfated CCK octapeptide (Item No. 24404).{40606}  

     

    Brand:
    Cayman
    SKU:23371 - 5 mg

    Available on backorder

  • Cholecystokinin (CCK) octapeptide is a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety.{40607,40606} It is a cleaved product of the full CCK preprohormone that is more potent than the full length enzyme in stimulating contraction of guinea pig gallbladder but with a shorter duration.{40606,40716} CCK octapeptide (sulfated) is 300-fold more active than the non-sulfated CCK octapeptide (Item No. 24404).{40606}  

     

    Brand:
    Cayman
    SKU:23371 - 500 µg

    Available on backorder

  • CCL2 also known as the monocyte chemoattractant protein-1 (MCP-1) is a chemokine and more particularly an C-C chemokine. Initially discovered in 1983, it is a monomeric polypeptide of 73 amino acids (13 kDa). It belongs to a family composed at least of members (MCP-1, -2, -3, and -4). CCL-2 is produced by the immune-cells (monocyte/macrophages) and non-immune cells (endothelial cells-fibroblast-myocyte). The main function of the CCL2 is the chimiotactism and more particularly the regulation of the migration and the infiltration of monocytes, memory T lymphocytes, and natural killer (NK) cells on an infection site. CCL2 is involved in many diseases like HIV-1 pathogenesis, cancer, cardiovascular disease, or diabetes. [Bertin Catalog No. A05415]  

     

    Brand:
    Cayman
    SKU:23621 - 96 wells

    Available on backorder

  • CCR2-RA-[R] is an allosteric antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 103 nM).{50108,50109,50110} It inhibits [35S]GTPγS binding and β-arrestin recruitment induced by chemokine (C-C motif) ligand 2 (CCL2) in U2OS membranes and cells, respectively, expressing CCR2 (IC50s = 24 and 25 nM, respectively).{50108}  

     

    Brand:
    Cayman
    SKU:28423 - 1 mg

    Available on backorder

  • CCR2-RA-[R] is an allosteric antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 103 nM).{50108,50109,50110} It inhibits [35S]GTPγS binding and β-arrestin recruitment induced by chemokine (C-C motif) ligand 2 (CCL2) in U2OS membranes and cells, respectively, expressing CCR2 (IC50s = 24 and 25 nM, respectively).{50108}  

     

    Brand:
    Cayman
    SKU:28423 - 10 mg

    Available on backorder

  • CCR2-RA-[R] is an allosteric antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 103 nM).{50108,50109,50110} It inhibits [35S]GTPγS binding and β-arrestin recruitment induced by chemokine (C-C motif) ligand 2 (CCL2) in U2OS membranes and cells, respectively, expressing CCR2 (IC50s = 24 and 25 nM, respectively).{50108}  

     

    Brand:
    Cayman
    SKU:28423 - 25 mg

    Available on backorder

  • CCR2-RA-[R] is an allosteric antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 103 nM).{50108,50109,50110} It inhibits [35S]GTPγS binding and β-arrestin recruitment induced by chemokine (C-C motif) ligand 2 (CCL2) in U2OS membranes and cells, respectively, expressing CCR2 (IC50s = 24 and 25 nM, respectively).{50108}  

     

    Brand:
    Cayman
    SKU:28423 - 5 mg

    Available on backorder

  • CCT007093 is an inhibitor of protein phosphatase 1D (PPM1D, also known as PP2Cδ and WIP1; IC50 = 8.4 µM), which is encoded by a putative oncogene that is amplified in multiple cancer types.{32263} It does not inhibit PPM1A. CCT007093 selectively inhibits the growth of cancer cells that overexpress PPM1D, including MCF-7, KPL-1, and MCF-3B cells, as well as certain ovarian clear cell carcinoma cells.{32263,32264} CCT007093 has been used to elucidate the mechanism by which PPM1D drives growth in medulloblastoma cells.{32262}  

     

    Brand:
    Cayman
    SKU:19992 -

    Available on backorder

  • CCT007093 is an inhibitor of protein phosphatase 1D (PPM1D, also known as PP2Cδ and WIP1; IC50 = 8.4 µM), which is encoded by a putative oncogene that is amplified in multiple cancer types.{32263} It does not inhibit PPM1A. CCT007093 selectively inhibits the growth of cancer cells that overexpress PPM1D, including MCF-7, KPL-1, and MCF-3B cells, as well as certain ovarian clear cell carcinoma cells.{32263,32264} CCT007093 has been used to elucidate the mechanism by which PPM1D drives growth in medulloblastoma cells.{32262}  

     

    Brand:
    Cayman
    SKU:19992 -

    Available on backorder

  • CCT007093 is an inhibitor of protein phosphatase 1D (PPM1D, also known as PP2Cδ and WIP1; IC50 = 8.4 µM), which is encoded by a putative oncogene that is amplified in multiple cancer types.{32263} It does not inhibit PPM1A. CCT007093 selectively inhibits the growth of cancer cells that overexpress PPM1D, including MCF-7, KPL-1, and MCF-3B cells, as well as certain ovarian clear cell carcinoma cells.{32263,32264} CCT007093 has been used to elucidate the mechanism by which PPM1D drives growth in medulloblastoma cells.{32262}  

     

    Brand:
    Cayman
    SKU:19992 -

    Available on backorder

  • CCT007093 is an inhibitor of protein phosphatase 1D (PPM1D, also known as PP2Cδ and WIP1; IC50 = 8.4 µM), which is encoded by a putative oncogene that is amplified in multiple cancer types.{32263} It does not inhibit PPM1A. CCT007093 selectively inhibits the growth of cancer cells that overexpress PPM1D, including MCF-7, KPL-1, and MCF-3B cells, as well as certain ovarian clear cell carcinoma cells.{32263,32264} CCT007093 has been used to elucidate the mechanism by which PPM1D drives growth in medulloblastoma cells.{32262}  

     

    Brand:
    Cayman
    SKU:19992 -

    Available on backorder

  • The heat shock protein 90 (Hsp90) is a molecular chaperone that activates and maintains the biological functioning of several client proteins, many of which are associated with oncogenic signaling pathways. Its activity is driven by ATP and regulated by co-chaperones such as Hsp72. CCT018159 is a 3,4-diaryl pyrazoloresorcinol compound that inhibits the ATPase activity of Hsp90 with IC50 values of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively.{16508} At concentrations up to 100 µM, CCT018159 does not inhibit human Hsp72 ATPase or topoisomerase II, yet at 50 µM CCT018159 inhibits 13 out of a panel of 20 commonly studied kinases.{16508} In human tumor xenografts, such as SKMEL 28 melanoma cells, CCT018159 induces Hsp72 expression and dc-Raf, ERBB2, and Cdk4.{16508}  

     

    Brand:
    Cayman
    SKU:10012591 - 1 mg

    Available on backorder

  • The heat shock protein 90 (Hsp90) is a molecular chaperone that activates and maintains the biological functioning of several client proteins, many of which are associated with oncogenic signaling pathways. Its activity is driven by ATP and regulated by co-chaperones such as Hsp72. CCT018159 is a 3,4-diaryl pyrazoloresorcinol compound that inhibits the ATPase activity of Hsp90 with IC50 values of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively.{16508} At concentrations up to 100 µM, CCT018159 does not inhibit human Hsp72 ATPase or topoisomerase II, yet at 50 µM CCT018159 inhibits 13 out of a panel of 20 commonly studied kinases.{16508} In human tumor xenografts, such as SKMEL 28 melanoma cells, CCT018159 induces Hsp72 expression and dc-Raf, ERBB2, and Cdk4.{16508}  

     

    Brand:
    Cayman
    SKU:10012591 - 10 mg

    Available on backorder

  • The heat shock protein 90 (Hsp90) is a molecular chaperone that activates and maintains the biological functioning of several client proteins, many of which are associated with oncogenic signaling pathways. Its activity is driven by ATP and regulated by co-chaperones such as Hsp72. CCT018159 is a 3,4-diaryl pyrazoloresorcinol compound that inhibits the ATPase activity of Hsp90 with IC50 values of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively.{16508} At concentrations up to 100 µM, CCT018159 does not inhibit human Hsp72 ATPase or topoisomerase II, yet at 50 µM CCT018159 inhibits 13 out of a panel of 20 commonly studied kinases.{16508} In human tumor xenografts, such as SKMEL 28 melanoma cells, CCT018159 induces Hsp72 expression and dc-Raf, ERBB2, and Cdk4.{16508}  

     

    Brand:
    Cayman
    SKU:10012591 - 5 mg

    Available on backorder

  • The heat shock protein 90 (Hsp90) is a molecular chaperone that activates and maintains the biological functioning of several client proteins, many of which are associated with oncogenic signaling pathways. Its activity is driven by ATP and regulated by co-chaperones such as Hsp72. CCT018159 is a 3,4-diaryl pyrazoloresorcinol compound that inhibits the ATPase activity of Hsp90 with IC50 values of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively.{16508} At concentrations up to 100 µM, CCT018159 does not inhibit human Hsp72 ATPase or topoisomerase II, yet at 50 µM CCT018159 inhibits 13 out of a panel of 20 commonly studied kinases.{16508} In human tumor xenografts, such as SKMEL 28 melanoma cells, CCT018159 induces Hsp72 expression and dc-Raf, ERBB2, and Cdk4.{16508}  

     

    Brand:
    Cayman
    SKU:10012591 - 50 mg

    Available on backorder

  • CCT128930 is an ATP-competitive inhibitor of Akt2 (IC50 = 6 nM).{29493} It is selective for Akt over a panel of 47 other kinases, including the related protein kinase A and p70S6K.{29493} CCT128930 blocks the phosphorylation of Akt targets, inhibits proliferation of multiple tumor cell lines in vitro, and prevents the growth of human tumor xenografts in mice.{29493} CCT128930 has been used to elucidate the role of Akt2 in regulating the function of interacting proteins, modulating DNA damage and autophagy in HepG2 hepatoma cells, and cell survival and vasculogenesis in endothelial colony forming cells.{29488,29492,29491}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CCT128930 is an ATP-competitive inhibitor of Akt2 (IC50 = 6 nM).{29493} It is selective for Akt over a panel of 47 other kinases, including the related protein kinase A and p70S6K.{29493} CCT128930 blocks the phosphorylation of Akt targets, inhibits proliferation of multiple tumor cell lines in vitro, and prevents the growth of human tumor xenografts in mice.{29493} CCT128930 has been used to elucidate the role of Akt2 in regulating the function of interacting proteins, modulating DNA damage and autophagy in HepG2 hepatoma cells, and cell survival and vasculogenesis in endothelial colony forming cells.{29488,29492,29491}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CCT128930 is an ATP-competitive inhibitor of Akt2 (IC50 = 6 nM).{29493} It is selective for Akt over a panel of 47 other kinases, including the related protein kinase A and p70S6K.{29493} CCT128930 blocks the phosphorylation of Akt targets, inhibits proliferation of multiple tumor cell lines in vitro, and prevents the growth of human tumor xenografts in mice.{29493} CCT128930 has been used to elucidate the role of Akt2 in regulating the function of interacting proteins, modulating DNA damage and autophagy in HepG2 hepatoma cells, and cell survival and vasculogenesis in endothelial colony forming cells.{29488,29492,29491}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CCT128930 is an ATP-competitive inhibitor of Akt2 (IC50 = 6 nM).{29493} It is selective for Akt over a panel of 47 other kinases, including the related protein kinase A and p70S6K.{29493} CCT128930 blocks the phosphorylation of Akt targets, inhibits proliferation of multiple tumor cell lines in vitro, and prevents the growth of human tumor xenografts in mice.{29493} CCT128930 has been used to elucidate the role of Akt2 in regulating the function of interacting proteins, modulating DNA damage and autophagy in HepG2 hepatoma cells, and cell survival and vasculogenesis in endothelial colony forming cells.{29488,29492,29491}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 μM in cell-free assays.{45586} It is selective for Aurora A and B over a panel of 13 kinases at 1 μM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 μM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).{45587} In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model.{45586} It also potentiates the antitumor effects of vincristine (Item No. 11764) in a KBv200 mouse xenograft model.{45587}  

     

    Brand:
    Cayman
    SKU:29053 - 1 mg

    Available on backorder

  • CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 μM in cell-free assays.{45586} It is selective for Aurora A and B over a panel of 13 kinases at 1 μM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 μM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).{45587} In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model.{45586} It also potentiates the antitumor effects of vincristine (Item No. 11764) in a KBv200 mouse xenograft model.{45587}  

     

    Brand:
    Cayman
    SKU:29053 - 10 mg

    Available on backorder

  • CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 μM in cell-free assays.{45586} It is selective for Aurora A and B over a panel of 13 kinases at 1 μM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 μM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).{45587} In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model.{45586} It also potentiates the antitumor effects of vincristine (Item No. 11764) in a KBv200 mouse xenograft model.{45587}  

     

    Brand:
    Cayman
    SKU:29053 - 5 mg

    Available on backorder

  • CCT137690 is a potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively).{27919} It also inhibits the receptor tyrosine kinase FLT3 as well as the constitutively active form of FLT3 bearing internal-tandem duplications (FLT3-ITD; IC50s = 1.2 and 4.9 nM, respectively).{27919} CCT137690 is orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice without inducing body weight loss.{27919} It blocks signaling through Aurora kinases in MYCN-amplified neuroblastoma cells, suppressing N-Myc expression and preventing proliferation.{27916} It inhibits growth of FLT3-ITD cells harboring a D835Y mutation, which confers resistance to other FLT3 inhibitors.{27917} CCT137690 also sensitizes colorectal carcinoma cells to radiotherapy.{27918}  

     

    Brand:
    Cayman
    SKU:-
  • CCT137690 is a potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively).{27919} It also inhibits the receptor tyrosine kinase FLT3 as well as the constitutively active form of FLT3 bearing internal-tandem duplications (FLT3-ITD; IC50s = 1.2 and 4.9 nM, respectively).{27919} CCT137690 is orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice without inducing body weight loss.{27919} It blocks signaling through Aurora kinases in MYCN-amplified neuroblastoma cells, suppressing N-Myc expression and preventing proliferation.{27916} It inhibits growth of FLT3-ITD cells harboring a D835Y mutation, which confers resistance to other FLT3 inhibitors.{27917} CCT137690 also sensitizes colorectal carcinoma cells to radiotherapy.{27918}  

     

    Brand:
    Cayman
    SKU:-
  • CCT137690 is a potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively).{27919} It also inhibits the receptor tyrosine kinase FLT3 as well as the constitutively active form of FLT3 bearing internal-tandem duplications (FLT3-ITD; IC50s = 1.2 and 4.9 nM, respectively).{27919} CCT137690 is orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice without inducing body weight loss.{27919} It blocks signaling through Aurora kinases in MYCN-amplified neuroblastoma cells, suppressing N-Myc expression and preventing proliferation.{27916} It inhibits growth of FLT3-ITD cells harboring a D835Y mutation, which confers resistance to other FLT3 inhibitors.{27917} CCT137690 also sensitizes colorectal carcinoma cells to radiotherapy.{27918}  

     

    Brand:
    Cayman
    SKU:-
  • CCT196969 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 100, 40, 12, 26, and 14 nM, respectively).{41909} It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 μM. CCT196969 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT196969 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT196969 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib (Item No. 16989) and trametinib (Item No. 16292).  

     

    Brand:
    Cayman
    SKU:25537 - 1 mg

    Available on backorder

  • CCT196969 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 100, 40, 12, 26, and 14 nM, respectively).{41909} It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 μM. CCT196969 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT196969 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT196969 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib (Item No. 16989) and trametinib (Item No. 16292).  

     

    Brand:
    Cayman
    SKU:25537 - 10 mg

    Available on backorder

  • CCT196969 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 100, 40, 12, 26, and 14 nM, respectively).{41909} It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 μM. CCT196969 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT196969 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT196969 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib (Item No. 16989) and trametinib (Item No. 16292).  

     

    Brand:
    Cayman
    SKU:25537 - 25 mg

    Available on backorder

  • CCT196969 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 100, 40, 12, 26, and 14 nM, respectively).{41909} It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 μM. CCT196969 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT196969 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT196969 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib (Item No. 16989) and trametinib (Item No. 16292).  

     

    Brand:
    Cayman
    SKU:25537 - 5 mg

    Available on backorder