Cayman

Showing 28201–28350 of 45550 results

  • LY2608204 is an activator of glucokinase (GK; EC50 = 42 nM).{41671} It stimulates glucose metabolism in INS-1E rat insulinoma cells (mean EC50 = 579 nM). LY2608204 (30 mg/kg) decreases plasma glucose levels in a dose-dependent manner in fasted rats.  

     

    Brand:
    Cayman
    SKU:22914 - 5 mg

    Available on backorder

  • LY266097 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.5 nM).{49230} It is selective for 5-HT2B over 5-HT2A and 5-HT2C receptors (Kis = 19.5 and 24.55 nM, respectively).{49231} LY266097 (100 nmol, intrathecal) reduces hind paw tactile allodynia induced by L5/L6 spinal nerve ligation in a rat model of neuropathic pain.{49232} It also reduces hyperlocomotion induced by cocaine in rats when administered at a dose of 0.63 mg/kg without reducing cocaine-induced dopamine outflow in the nucleus accumbens shell.{36202}  

     

    Brand:
    Cayman
    SKU:11935 - 1 mg

    Available on backorder

  • LY266097 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.5 nM).{49230} It is selective for 5-HT2B over 5-HT2A and 5-HT2C receptors (Kis = 19.5 and 24.55 nM, respectively).{49231} LY266097 (100 nmol, intrathecal) reduces hind paw tactile allodynia induced by L5/L6 spinal nerve ligation in a rat model of neuropathic pain.{49232} It also reduces hyperlocomotion induced by cocaine in rats when administered at a dose of 0.63 mg/kg without reducing cocaine-induced dopamine outflow in the nucleus accumbens shell.{36202}  

     

    Brand:
    Cayman
    SKU:11935 - 10 mg

    Available on backorder

  • LY266097 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.5 nM).{49230} It is selective for 5-HT2B over 5-HT2A and 5-HT2C receptors (Kis = 19.5 and 24.55 nM, respectively).{49231} LY266097 (100 nmol, intrathecal) reduces hind paw tactile allodynia induced by L5/L6 spinal nerve ligation in a rat model of neuropathic pain.{49232} It also reduces hyperlocomotion induced by cocaine in rats when administered at a dose of 0.63 mg/kg without reducing cocaine-induced dopamine outflow in the nucleus accumbens shell.{36202}  

     

    Brand:
    Cayman
    SKU:11935 - 5 mg

    Available on backorder

  • LY266097 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.5 nM).{49230} It is selective for 5-HT2B over 5-HT2A and 5-HT2C receptors (Kis = 19.5 and 24.55 nM, respectively).{49231} LY266097 (100 nmol, intrathecal) reduces hind paw tactile allodynia induced by L5/L6 spinal nerve ligation in a rat model of neuropathic pain.{49232} It also reduces hyperlocomotion induced by cocaine in rats when administered at a dose of 0.63 mg/kg without reducing cocaine-induced dopamine outflow in the nucleus accumbens shell.{36202}  

     

    Brand:
    Cayman
    SKU:11935 - 500 µg

    Available on backorder

  • LY272015 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{49231} It binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM). LY272015 is selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM, respectively), as well as α1-adrenergic receptors.{49231,52703} It reduces 5-HT-induced migration of isolated mouse aortic smooth muscle cells when used at a concentration of 100 nM.{52704} LY272015 (1 and 3 mg/kg) decreases mean arterial pressure in hypertensive DOCA-SALT rats.{52705}  

     

    Brand:
    Cayman
    SKU:31471 - 1 mg

    Available on backorder

  • LY272015 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{49231} It binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM). LY272015 is selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM, respectively), as well as α1-adrenergic receptors.{49231,52703} It reduces 5-HT-induced migration of isolated mouse aortic smooth muscle cells when used at a concentration of 100 nM.{52704} LY272015 (1 and 3 mg/kg) decreases mean arterial pressure in hypertensive DOCA-SALT rats.{52705}  

     

    Brand:
    Cayman
    SKU:31471 - 5 mg

    Available on backorder

  • LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively).{27398} It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form.{27398} When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets.{27398} JAK inhibitors, including LY2784544, may be useful in hematological malignancies.{27397}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively).{27398} It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form.{27398} When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets.{27398} JAK inhibitors, including LY2784544, may be useful in hematological malignancies.{27397}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively).{27398} It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form.{27398} When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets.{27398} JAK inhibitors, including LY2784544, may be useful in hematological malignancies.{27397}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively).{27398} It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form.{27398} When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets.{27398} JAK inhibitors, including LY2784544, may be useful in hematological malignancies.{27397}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM).{48025} It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.  

     

    Brand:
    Cayman
    SKU:25978 - 1 mg

    Available on backorder

  • LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM).{48025} It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.  

     

    Brand:
    Cayman
    SKU:25978 - 10 mg

    Available on backorder

  • LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM).{48025} It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.  

     

    Brand:
    Cayman
    SKU:25978 - 5 mg

    Available on backorder

  • LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM).{48025} It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.  

     

    Brand:
    Cayman
    SKU:25978 - 50 mg

    Available on backorder

  • Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.{16791} Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.{16790} LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.{27584} LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.{27584} Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.{27584}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.{16791} Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.{16790} LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.{27584} LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.{27584} Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.{27584}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.{16791} Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.{16790} LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.{27584} LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.{27584} Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.{27584}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.{16791} Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.{16790} LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.{27584} LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.{27584} Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.{27584}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM).{43815} It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). It reduces differences in hind paw weight bearing between monoiodoacetic acid- and saline-injected knees in a rat model of knee joint-related chronic pain induced by monoiodoacetic acid (MIA) when administered at doses greater than or equal to 0.1 mg/kg. LY2828360 dose-dependently reduces mechanical and cold allodynia induced by paclitaxel (Item No. 10461) in mice and prevents development of morphine tolerance when administered at dose of 3 mg/kg per day for 12 days.{43816} It also reduces paclitaxel-induced allodynia in morphine-tolerant mice.  

     

    Brand:
    Cayman
    SKU:26791 - 1 mg

    Available on backorder

  • LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM).{43815} It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). It reduces differences in hind paw weight bearing between monoiodoacetic acid- and saline-injected knees in a rat model of knee joint-related chronic pain induced by monoiodoacetic acid (MIA) when administered at doses greater than or equal to 0.1 mg/kg. LY2828360 dose-dependently reduces mechanical and cold allodynia induced by paclitaxel (Item No. 10461) in mice and prevents development of morphine tolerance when administered at dose of 3 mg/kg per day for 12 days.{43816} It also reduces paclitaxel-induced allodynia in morphine-tolerant mice.  

     

    Brand:
    Cayman
    SKU:26791 - 10 mg

    Available on backorder

  • LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM).{43815} It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). It reduces differences in hind paw weight bearing between monoiodoacetic acid- and saline-injected knees in a rat model of knee joint-related chronic pain induced by monoiodoacetic acid (MIA) when administered at doses greater than or equal to 0.1 mg/kg. LY2828360 dose-dependently reduces mechanical and cold allodynia induced by paclitaxel (Item No. 10461) in mice and prevents development of morphine tolerance when administered at dose of 3 mg/kg per day for 12 days.{43816} It also reduces paclitaxel-induced allodynia in morphine-tolerant mice.  

     

    Brand:
    Cayman
    SKU:26791 - 25 mg

    Available on backorder

  • LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM).{43815} It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). It reduces differences in hind paw weight bearing between monoiodoacetic acid- and saline-injected knees in a rat model of knee joint-related chronic pain induced by monoiodoacetic acid (MIA) when administered at doses greater than or equal to 0.1 mg/kg. LY2828360 dose-dependently reduces mechanical and cold allodynia induced by paclitaxel (Item No. 10461) in mice and prevents development of morphine tolerance when administered at dose of 3 mg/kg per day for 12 days.{43816} It also reduces paclitaxel-induced allodynia in morphine-tolerant mice.  

     

    Brand:
    Cayman
    SKU:26791 - 5 mg

    Available on backorder

  • LY2835219 is an orally bioavailable dual inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 (IC50s = 2 and 10 nM, respectively).{29192} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29193}  

     

    Brand:
    Cayman
    SKU:21560 -

    Out of stock

  • LY2835219 is an orally bioavailable dual inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 (IC50s = 2 and 10 nM, respectively).{29192} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29193}  

     

    Brand:
    Cayman
    SKU:21560 -

    Out of stock

  • LY2835219 is an orally bioavailable dual inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 (IC50s = 2 and 10 nM, respectively).{29192} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29193}  

     

    Brand:
    Cayman
    SKU:21560 -

    Out of stock

  • LY2835219 is an orally bioavailable dual inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 (IC50s = 2 and 10 nM, respectively).{29192} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29193}  

     

    Brand:
    Cayman
    SKU:21560 -

    Out of stock

  • LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively).{28691,29192,29193} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29192,29193}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively).{28691,29192,29193} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29192,29193}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively).{28691,29192,29193} Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.{29192,29193}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY2874455 is a pan-inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases with IC50 values of 2.8, 2.6, 6.4, 6, and 7 nM for FGFR1, FGFR2, FGFR3, FGFR4, and VEGFR2, respectively.{33523} It has been shown to inhibit proliferation of KMS-11, OPM-2, SNU-16, and KATO-III cancer cells in vitro and in tumor xenografts in mice.{33523}  

     

    Brand:
    Cayman
    SKU:20843 -

    Out of stock

  • LY2874455 is a pan-inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases with IC50 values of 2.8, 2.6, 6.4, 6, and 7 nM for FGFR1, FGFR2, FGFR3, FGFR4, and VEGFR2, respectively.{33523} It has been shown to inhibit proliferation of KMS-11, OPM-2, SNU-16, and KATO-III cancer cells in vitro and in tumor xenografts in mice.{33523}  

     

    Brand:
    Cayman
    SKU:20843 -

    Out of stock

  • LY2874455 is a pan-inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases with IC50 values of 2.8, 2.6, 6.4, 6, and 7 nM for FGFR1, FGFR2, FGFR3, FGFR4, and VEGFR2, respectively.{33523} It has been shown to inhibit proliferation of KMS-11, OPM-2, SNU-16, and KATO-III cancer cells in vitro and in tumor xenografts in mice.{33523}  

     

    Brand:
    Cayman
    SKU:20843 -

    Out of stock

  • LY2874455 is a pan-inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases with IC50 values of 2.8, 2.6, 6.4, 6, and 7 nM for FGFR1, FGFR2, FGFR3, FGFR4, and VEGFR2, respectively.{33523} It has been shown to inhibit proliferation of KMS-11, OPM-2, SNU-16, and KATO-III cancer cells in vitro and in tumor xenografts in mice.{33523}  

     

    Brand:
    Cayman
    SKU:20843 -

    Out of stock

  • LY2886721 selectively inhibits the β-site amyloid protein cleaving enzyme (BACE) (IC50 = 20 nM for recombinant hBACE1).{33660} BACE performs the first cleavage step in the Aβ cascade; thus, its inhibition by LY2886721 decreases production of all forms of the Aβ peptide.{33661} A Phase II clinical study for the use of LY2886721 in the treatment of Alzheimer’s disease was terminated early due to abnormal liver biochemistry values in several patients. The toxic effects did not appear to be due to BACE inhibition.  

     

    Brand:
    Cayman
    SKU:21599 -

    Out of stock

  • LY2886721 selectively inhibits the β-site amyloid protein cleaving enzyme (BACE) (IC50 = 20 nM for recombinant hBACE1).{33660} BACE performs the first cleavage step in the Aβ cascade; thus, its inhibition by LY2886721 decreases production of all forms of the Aβ peptide.{33661} A Phase II clinical study for the use of LY2886721 in the treatment of Alzheimer’s disease was terminated early due to abnormal liver biochemistry values in several patients. The toxic effects did not appear to be due to BACE inhibition.  

     

    Brand:
    Cayman
    SKU:21599 -

    Out of stock

  • LY2886721 selectively inhibits the β-site amyloid protein cleaving enzyme (BACE) (IC50 = 20 nM for recombinant hBACE1).{33660} BACE performs the first cleavage step in the Aβ cascade; thus, its inhibition by LY2886721 decreases production of all forms of the Aβ peptide.{33661} A Phase II clinical study for the use of LY2886721 in the treatment of Alzheimer’s disease was terminated early due to abnormal liver biochemistry values in several patients. The toxic effects did not appear to be due to BACE inhibition.  

     

    Brand:
    Cayman
    SKU:21599 -

    Out of stock

  • LY2886721 selectively inhibits the β-site amyloid protein cleaving enzyme (BACE) (IC50 = 20 nM for recombinant hBACE1).{33660} BACE performs the first cleavage step in the Aβ cascade; thus, its inhibition by LY2886721 decreases production of all forms of the Aβ peptide.{33661} A Phase II clinical study for the use of LY2886721 in the treatment of Alzheimer’s disease was terminated early due to abnormal liver biochemistry values in several patients. The toxic effects did not appear to be due to BACE inhibition.  

     

    Brand:
    Cayman
    SKU:21599 -

    Out of stock

  • Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. LY293111 is a potent antagonist of the leukotriene B4 (LTB4) receptor, BLT1, that inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 17.6 nM and inhibits the LTB4-induced chemotaxis of human neutrophils with an IC50 value of 6.3 nM.{14782} LY293111 inhibits growth of MiaPaCa-2 and AsPC-1 human pancreatic cancer cells in vitro (250-1,000 nM) and subcutaneous xenografts in athymic mice (250 mg/kg/day), inducing apoptosis and S-phase arrest.{16702}  

     

    Brand:
    Cayman
    SKU:10009768 - 1 mg

    Available on backorder

  • Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. LY293111 is a potent antagonist of the leukotriene B4 (LTB4) receptor, BLT1, that inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 17.6 nM and inhibits the LTB4-induced chemotaxis of human neutrophils with an IC50 value of 6.3 nM.{14782} LY293111 inhibits growth of MiaPaCa-2 and AsPC-1 human pancreatic cancer cells in vitro (250-1,000 nM) and subcutaneous xenografts in athymic mice (250 mg/kg/day), inducing apoptosis and S-phase arrest.{16702}  

     

    Brand:
    Cayman
    SKU:10009768 - 10 mg

    Available on backorder

  • Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. LY293111 is a potent antagonist of the leukotriene B4 (LTB4) receptor, BLT1, that inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 17.6 nM and inhibits the LTB4-induced chemotaxis of human neutrophils with an IC50 value of 6.3 nM.{14782} LY293111 inhibits growth of MiaPaCa-2 and AsPC-1 human pancreatic cancer cells in vitro (250-1,000 nM) and subcutaneous xenografts in athymic mice (250 mg/kg/day), inducing apoptosis and S-phase arrest.{16702}  

     

    Brand:
    Cayman
    SKU:10009768 - 5 mg

    Available on backorder

  • Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. LY293111 is a potent antagonist of the leukotriene B4 (LTB4) receptor, BLT1, that inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 17.6 nM and inhibits the LTB4-induced chemotaxis of human neutrophils with an IC50 value of 6.3 nM.{14782} LY293111 inhibits growth of MiaPaCa-2 and AsPC-1 human pancreatic cancer cells in vitro (250-1,000 nM) and subcutaneous xenografts in athymic mice (250 mg/kg/day), inducing apoptosis and S-phase arrest.{16702}  

     

    Brand:
    Cayman
    SKU:10009768 - 500 µg

    Available on backorder

  • LY294002 is a selective phosphatidylinositol 3-kinase (PI3K) inhibitor with a 2.7-fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC50 of 1.4 µM.{6296}  

     

    Brand:
    Cayman
    SKU:70920 - 10 mg

    Available on backorder

  • LY294002 is a selective phosphatidylinositol 3-kinase (PI3K) inhibitor with a 2.7-fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC50 of 1.4 µM.{6296}  

     

    Brand:
    Cayman
    SKU:70920 - 25 mg

    Available on backorder

  • LY294002 is a selective phosphatidylinositol 3-kinase (PI3K) inhibitor with a 2.7-fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC50 of 1.4 µM.{6296}  

     

    Brand:
    Cayman
    SKU:70920 - 5 mg

    Available on backorder

  • LY294002 is a selective phosphatidylinositol 3-kinase (PI3K) inhibitor with a 2.7-fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC50 of 1.4 µM.{6296}  

     

    Brand:
    Cayman
    SKU:70920 - 50 mg

    Available on backorder

  • Smoothened (Smo) is a GPCR-like receptor that, with Patched, mediates hedgehog (Hh) signaling to regulate gene expression through the Gli transcription factors.{21774} LY2940680 is an antitumor agent that binds to the human Smo receptor and inhibits Sonic Hh-induced Gli1 expression (IC50 = ~2.4 nM in vitro).{27679,27681,27680} The potential anticancer activity of LY2940680 is currently under clinical investigation.  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (Smo) is a GPCR-like receptor that, with Patched, mediates hedgehog (Hh) signaling to regulate gene expression through the Gli transcription factors.{21774} LY2940680 is an antitumor agent that binds to the human Smo receptor and inhibits Sonic Hh-induced Gli1 expression (IC50 = ~2.4 nM in vitro).{27679,27681,27680} The potential anticancer activity of LY2940680 is currently under clinical investigation.  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (Smo) is a GPCR-like receptor that, with Patched, mediates hedgehog (Hh) signaling to regulate gene expression through the Gli transcription factors.{21774} LY2940680 is an antitumor agent that binds to the human Smo receptor and inhibits Sonic Hh-induced Gli1 expression (IC50 = ~2.4 nM in vitro).{27679,27681,27680} The potential anticancer activity of LY2940680 is currently under clinical investigation.  

     

    Brand:
    Cayman
    SKU:-
  • LY2955303 is a potent antagonist of retinoic acid receptor γ (RARγ; Ki = 1.1 nM).{42717} It is selective for RARγ over RARα and RARβ (Kis = >1,700 and >2,980 nM, respectively). LY2955303 reduces differential weight bearing between the contralateral and ipsilateral limbs in a rat model of monoiodoacetate-induced osteoarthritis (ED50 = 0.72 mg/kg).  

     

    Brand:
    Cayman
    SKU:25833 - 1 mg

    Available on backorder

  • LY2955303 is a potent antagonist of retinoic acid receptor γ (RARγ; Ki = 1.1 nM).{42717} It is selective for RARγ over RARα and RARβ (Kis = >1,700 and >2,980 nM, respectively). LY2955303 reduces differential weight bearing between the contralateral and ipsilateral limbs in a rat model of monoiodoacetate-induced osteoarthritis (ED50 = 0.72 mg/kg).  

     

    Brand:
    Cayman
    SKU:25833 - 10 mg

    Available on backorder

  • LY2955303 is a potent antagonist of retinoic acid receptor γ (RARγ; Ki = 1.1 nM).{42717} It is selective for RARγ over RARα and RARβ (Kis = >1,700 and >2,980 nM, respectively). LY2955303 reduces differential weight bearing between the contralateral and ipsilateral limbs in a rat model of monoiodoacetate-induced osteoarthritis (ED50 = 0.72 mg/kg).  

     

    Brand:
    Cayman
    SKU:25833 - 25 mg

    Available on backorder

  • LY2955303 is a potent antagonist of retinoic acid receptor γ (RARγ; Ki = 1.1 nM).{42717} It is selective for RARγ over RARα and RARβ (Kis = >1,700 and >2,980 nM, respectively). LY2955303 reduces differential weight bearing between the contralateral and ipsilateral limbs in a rat model of monoiodoacetate-induced osteoarthritis (ED50 = 0.72 mg/kg).  

     

    Brand:
    Cayman
    SKU:25833 - 5 mg

    Available on backorder

  • LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme).{53427} It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.  

     

    Brand:
    Cayman
    SKU:29729 - 1 mg

    Available on backorder

  • LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme).{53427} It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.  

     

    Brand:
    Cayman
    SKU:29729 - 10 mg

    Available on backorder

  • LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme).{53427} It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.  

     

    Brand:
    Cayman
    SKU:29729 - 5 mg

    Available on backorder

  • LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme).{53427} It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.  

     

    Brand:
    Cayman
    SKU:29729 - 500 µg

    Available on backorder

  • LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}  

     

    Brand:
    Cayman
    SKU:21504 -

    Out of stock

  • LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}  

     

    Brand:
    Cayman
    SKU:21504 -

    Out of stock

  • LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}  

     

    Brand:
    Cayman
    SKU:21504 -

    Out of stock

  • LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}  

     

    Brand:
    Cayman
    SKU:21504 -

    Out of stock

  • LY303511 is a close structural analog of LY294002 (Item No. 70920), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor.{32629} LY303511, however, does not inhibit PI3K-dependent phosphorylation of Akt but instead has been shown to inhibit mTOR-dependent phosphorylation of S6K.{32629} It can reduce cell proliferation in human lung epithelial adenocarcinoma cells, blocking G2/M progression and inhibiting casein kinase 2 activity.{32629} LY303511 demonstrates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitizing activity in HeLa cells that are refractory to TRAIL-induced apoptosis.{32630} LY303511 is also reported to block voltage-gated potassium (Kv) channels.{32631}  

     

    Brand:
    Cayman
    SKU:-
  • LY303511 is a close structural analog of LY294002 (Item No. 70920), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor.{32629} LY303511, however, does not inhibit PI3K-dependent phosphorylation of Akt but instead has been shown to inhibit mTOR-dependent phosphorylation of S6K.{32629} It can reduce cell proliferation in human lung epithelial adenocarcinoma cells, blocking G2/M progression and inhibiting casein kinase 2 activity.{32629} LY303511 demonstrates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitizing activity in HeLa cells that are refractory to TRAIL-induced apoptosis.{32630} LY303511 is also reported to block voltage-gated potassium (Kv) channels.{32631}  

     

    Brand:
    Cayman
    SKU:-
  • LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}  

     

    Brand:
    Cayman
    SKU:22938 - 10 mg

    Available on backorder

  • LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}  

     

    Brand:
    Cayman
    SKU:22938 - 25 mg

    Available on backorder

  • LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}  

     

    Brand:
    Cayman
    SKU:22938 - 5 mg

    Available on backorder

  • Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:25988 - 10 mg

    Available on backorder

  • LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:25988 - 25 mg

    Available on backorder

  • LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:25988 - 5 mg

    Available on backorder

  • LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:25988 - 50 mg

    Available on backorder

  • LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.  

     

    Brand:
    Cayman
    SKU:25276 - 1 mg

    Available on backorder

  • LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.  

     

    Brand:
    Cayman
    SKU:25276 - 10 mg

    Available on backorder

  • LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.  

     

    Brand:
    Cayman
    SKU:25276 - 25 mg

    Available on backorder

  • LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.  

     

    Brand:
    Cayman
    SKU:25276 - 5 mg

    Available on backorder

  • LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}  

     

    Brand:
    Cayman
    SKU:11738 - 1 mg

    Available on backorder

  • LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}  

     

    Brand:
    Cayman
    SKU:11738 - 10 mg

    Available on backorder

  • LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}  

     

    Brand:
    Cayman
    SKU:11738 - 5 mg

    Available on backorder

  • LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.  

     

    Brand:
    Cayman
    SKU:27936 - 1 mg

    Available on backorder

  • LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.  

     

    Brand:
    Cayman
    SKU:27936 - 10 mg

    Available on backorder

  • LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.  

     

    Brand:
    Cayman
    SKU:27936 - 25 mg

    Available on backorder

  • LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.  

     

    Brand:
    Cayman
    SKU:27936 - 5 mg

    Available on backorder

  • The protein kinase C (PKC) isoforms PKCβ1 and PKCβ2 have central roles in cell signaling in diabetes, diffuse large B-cell lymphoma, and cardiovascular diseases.{21723,21721,21722,21725} LY333531 is a selective and potent inhibitor of PKCβ1 and PKCβ2 (IC50 = 4.7 and 5.9 nM, respectively).{21724} For comparison, its IC50 values for PKC isoforms α, γ, δ, ε, ζ, and η are 360, 300, 250, 600, >100,000, and 52 nM, respectively.{21724} LY333531 is effective in vivo.{21723,21721}  

     

    Brand:
    Cayman
    SKU:-
  • The protein kinase C (PKC) isoforms PKCβ1 and PKCβ2 have central roles in cell signaling in diabetes, diffuse large B-cell lymphoma, and cardiovascular diseases.{21723,21721,21722,21725} LY333531 is a selective and potent inhibitor of PKCβ1 and PKCβ2 (IC50 = 4.7 and 5.9 nM, respectively).{21724} For comparison, its IC50 values for PKC isoforms α, γ, δ, ε, ζ, and η are 360, 300, 250, 600, >100,000, and 52 nM, respectively.{21724} LY333531 is effective in vivo.{21723,21721}  

     

    Brand:
    Cayman
    SKU:-
  • LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.  

     

    Brand:
    Cayman
    SKU:29481 - 1 mg

    Available on backorder

  • LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.  

     

    Brand:
    Cayman
    SKU:29481 - 10 mg

    Available on backorder

  • LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.  

     

    Brand:
    Cayman
    SKU:29481 - 5 mg

    Available on backorder

  • LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}  

     

    Brand:
    Cayman
    SKU:-
  • LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}  

     

    Brand:
    Cayman
    SKU:-
  • LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}  

     

    Brand:
    Cayman
    SKU:-
  • LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).  

     

    Brand:
    Cayman
    SKU:29496 - 10 mg

    Available on backorder

  • LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).  

     

    Brand:
    Cayman
    SKU:29496 - 25 mg

    Available on backorder

  • LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).  

     

    Brand:
    Cayman
    SKU:29496 - 5 mg

    Available on backorder

  • LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).  

     

    Brand:
    Cayman
    SKU:29496 - 50 mg

    Available on backorder

  • LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}  

     

    Brand:
    Cayman
    SKU:24215 - 1 mg

    Available on backorder

  • LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}  

     

    Brand:
    Cayman
    SKU:24215 - 10 mg

    Available on backorder

  • LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}  

     

    Brand:
    Cayman
    SKU:24215 - 5 mg

    Available on backorder

  • Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}  

     

    Brand:
    Cayman
    SKU:-
  • Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}  

     

    Brand:
    Cayman
    SKU:-
  • Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}  

     

    Brand:
    Cayman
    SKU:-
  • Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}  

     

    Brand:
    Cayman
    SKU:-
  • LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}  

     

    Brand:
    Cayman
    SKU:-
  • LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}  

     

    Brand:
    Cayman
    SKU:-
  • LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}  

     

    Brand:
    Cayman
    SKU:-
  • LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}  

     

    Brand:
    Cayman
    SKU:32775 - 1 mg

    Available on backorder

  • LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}  

     

    Brand:
    Cayman
    SKU:32775 - 10 mg

    Available on backorder

  • LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}  

     

    Brand:
    Cayman
    SKU:32775 - 5 mg

    Available on backorder

  • LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}  

     

    Brand:
    Cayman
    SKU:28741 - 10 mg

    Available on backorder

  • LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}  

     

    Brand:
    Cayman
    SKU:28741 - 25 mg

    Available on backorder

  • LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}  

     

    Brand:
    Cayman
    SKU:28741 - 5 mg

    Available on backorder

  • LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}  

     

    Brand:
    Cayman
    SKU:28741 - 50 mg

    Available on backorder

  • γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}  

     

    Brand:
    Cayman
    SKU:-
  • γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}  

     

    Brand:
    Cayman
    SKU:-
  • γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}  

     

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    Cayman
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  • γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}  

     

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    Cayman
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  • LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}  

     

    Brand:
    Cayman
    SKU:70230 - 1 mg

    Available on backorder

  • LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}  

     

    Brand:
    Cayman
    SKU:70230 - 10 mg

    Available on backorder

  • LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}  

     

    Brand:
    Cayman
    SKU:70230 - 5 mg

    Available on backorder

  • LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}  

     

    Brand:
    Cayman
    SKU:70230 - 50 mg

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  • Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}  

     

    Brand:
    Cayman
    SKU:70945 - 1 mg

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  • Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}  

     

    Brand:
    Cayman
    SKU:70945 - 10 mg

    Available on backorder

  • Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}  

     

    Brand:
    Cayman
    SKU:70945 - 5 mg

    Available on backorder

  • Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}  

     

    Brand:
    Cayman
    SKU:30650 - 10 mg

    Available on backorder

  • Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}  

     

    Brand:
    Cayman
    SKU:30650 - 25 mg

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  • Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}  

     

    Brand:
    Cayman
    SKU:30650 - 5 mg

    Available on backorder

  • Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}  

     

    Brand:
    Cayman
    SKU:30650 - 50 mg

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  • Lydicamycin is an antibiotic first isolated from Streptomyces. It is particularly cytotoxic against S. aureus, including the methicillin resistant 535 strain (MICs = 3.1-6.2 µg/ml).{32121} Lydicamycin also inhibits the growth of C. neoformans (MIC = 25 µg/ml) but is ineffective against Gram-negative bacteria.{32121}  

     

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    Cayman
    SKU:20584 -

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  • Lydicamycin is an antibiotic first isolated from Streptomyces. It is particularly cytotoxic against S. aureus, including the methicillin resistant 535 strain (MICs = 3.1-6.2 µg/ml).{32121} Lydicamycin also inhibits the growth of C. neoformans (MIC = 25 µg/ml) but is ineffective against Gram-negative bacteria.{32121}  

     

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    Cayman
    SKU:20584 -

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  • LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities.{39094, 39095} It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential.{39094} LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.{39095}  

     

    Brand:
    Cayman
    SKU:21976 -

    Out of stock

  • LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities.{39094, 39095} It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential.{39094} LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.{39095}  

     

    Brand:
    Cayman
    SKU:21976 -

    Out of stock

  • LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities.{39094, 39095} It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential.{39094} LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.{39095}  

     

    Brand:
    Cayman
    SKU:21976 -

    Out of stock

  • LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities.{39094, 39095} It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential.{39094} LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.{39095}  

     

    Brand:
    Cayman
    SKU:21976 -

    Out of stock

  • LYN-1604 is an activator of unc-51-like kinase 1 (ULK1; EC50 = 18.94 nM).{36916} It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC50 = 1.66 μM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA; Item No. 13242). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24007 - 1 mg

    Available on backorder

  • LYN-1604 is an activator of unc-51-like kinase 1 (ULK1; EC50 = 18.94 nM).{36916} It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC50 = 1.66 μM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA; Item No. 13242). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24007 - 10 mg

    Available on backorder

  • LYN-1604 is an activator of unc-51-like kinase 1 (ULK1; EC50 = 18.94 nM).{36916} It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC50 = 1.66 μM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA; Item No. 13242). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24007 - 5 mg

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  • Lys05 is an inhibitor of autophagy.{51043} It induces p62 accumulation and increases the ratio of LC3-II to LC3-I in C8161 melanoma cells in a concentration-dependent manner. Lys05 (76 mg/kg) increases the number of autophagic vesicles per cell in tumors in a C8161 mouse xenograft model and reduces tumor volume and growth in a 1205Lu melanoma mouse xenograft model. It also reduces tumor growth rate, volume, and weight in an HT-29 colon cancer mouse xenograft model when administered at doses greater than or equal to 10 mg/kg but increases bowel thickness and obstruction when administered at 80 mg/kg.  

     

    Brand:
    Cayman
    SKU:27334 - 10 mg

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  • Lys05 is an inhibitor of autophagy.{51043} It induces p62 accumulation and increases the ratio of LC3-II to LC3-I in C8161 melanoma cells in a concentration-dependent manner. Lys05 (76 mg/kg) increases the number of autophagic vesicles per cell in tumors in a C8161 mouse xenograft model and reduces tumor volume and growth in a 1205Lu melanoma mouse xenograft model. It also reduces tumor growth rate, volume, and weight in an HT-29 colon cancer mouse xenograft model when administered at doses greater than or equal to 10 mg/kg but increases bowel thickness and obstruction when administered at 80 mg/kg.  

     

    Brand:
    Cayman
    SKU:27334 - 25 mg

    Available on backorder

  • Lys05 is an inhibitor of autophagy.{51043} It induces p62 accumulation and increases the ratio of LC3-II to LC3-I in C8161 melanoma cells in a concentration-dependent manner. Lys05 (76 mg/kg) increases the number of autophagic vesicles per cell in tumors in a C8161 mouse xenograft model and reduces tumor volume and growth in a 1205Lu melanoma mouse xenograft model. It also reduces tumor growth rate, volume, and weight in an HT-29 colon cancer mouse xenograft model when administered at doses greater than or equal to 10 mg/kg but increases bowel thickness and obstruction when administered at 80 mg/kg.  

     

    Brand:
    Cayman
    SKU:27334 - 5 mg

    Available on backorder

  • Lys05 is an inhibitor of autophagy.{51043} It induces p62 accumulation and increases the ratio of LC3-II to LC3-I in C8161 melanoma cells in a concentration-dependent manner. Lys05 (76 mg/kg) increases the number of autophagic vesicles per cell in tumors in a C8161 mouse xenograft model and reduces tumor volume and growth in a 1205Lu melanoma mouse xenograft model. It also reduces tumor growth rate, volume, and weight in an HT-29 colon cancer mouse xenograft model when administered at doses greater than or equal to 10 mg/kg but increases bowel thickness and obstruction when administered at 80 mg/kg.  

     

    Brand:
    Cayman
    SKU:27334 - 50 mg

    Available on backorder

  • Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).{18521,16614} LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 µM.{18521} It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.{16614} LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.  

     

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    Cayman
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