Cayman
Showing 25501–25650 of 45550 results
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The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.
Brand:CaymanSKU:10641 - 10 mgAvailable on backorder
The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.
Brand:CaymanSKU:10641 - 25 mgAvailable on backorder
The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.
Brand:CaymanSKU:10641 - 5 mgAvailable on backorder
JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.
Brand:CaymanSKU:22905 - 1 mgAvailable on backorder
JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.
Brand:CaymanSKU:22905 - 10 mgAvailable on backorder
JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.
Brand:CaymanSKU:22905 - 25 mgAvailable on backorder
JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.
Brand:CaymanSKU:22905 - 5 mgAvailable on backorder
JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}
Brand:CaymanSKU:- JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}
Brand:CaymanSKU:- JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}
Brand:CaymanSKU:- JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}
Brand:CaymanSKU:-
JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}
Brand:CaymanSKU:-Available on backorder
JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}
Brand:CaymanSKU:-Available on backorder
JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}
Brand:CaymanSKU:-Available on backorder
JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}
Brand:CaymanSKU:- JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}
Brand:CaymanSKU:- JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}
Brand:CaymanSKU:- JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}
Brand:CaymanSKU:-
JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1674 reduces viability of LOX-IMVI cancer cells (EC50 = 0.03 µM) and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30784 - 1 mgAvailable on backorder
JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1674 reduces viability of LOX-IMVI cancer cells (EC50 = 0.03 µM) and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30784 - 5 mgAvailable on backorder
JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30786 - 1 mgAvailable on backorder
JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30786 - 10 mgAvailable on backorder
JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30786 - 25 mgAvailable on backorder
JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).
Brand:CaymanSKU:30786 - 5 mgAvailable on backorder
Immunogen: Human recombinant JMJD2A amino acids 1-350 • Host: Rabbit • Cross Reactivity: (+) JMJD2C, JMJD2B • Species Reactivity: (+) Human JMJD2A • Application(s): WB • JMJD2A is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.This JMJD2A polyclonal antibody was raised against an N-terminal recombinant fragment of JMJD2A. This fragment (amino acids 1-350) includes the JMJN and JMJC domains but not the two LAP/PHD zinc finger or Tudor domains of the 1,064 amino acid protein.
Brand:CaymanSKU:10382- 500 µl Jumonji Domain Containing 2A (JMJD2A) is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.{16409,17969,18035} This JMJD2A polyclonal antibody was raised against an N-terminal recombinant fragment of JMJD2A. This fragment includes amino acids 1-350 including the JMJN and JMJC domains but not the two LAP/PHD zinc finger or Tudor domains of the 1,064 amino acid protein.{16420,18036} JMJD2A is detected at 135 kDa by western blotting using a DLD1 cell lysate as a positive control. Also, the expression of JMJD2A varies by tissue, and northern blotting suggests skeletal muscle as a negative control and lung as a positive control tissue.{18036}
Brand:CaymanSKU:10382 - 500 µlAvailable on backorder
Immunogen: Human recombinant JMJD2A amino acids 1-350 • Host: Rabbit • Cross Reactivity: (+) JMJD2C, JMJD2B • Species Reactivity: (+) Human JMJD2A • Application(s): WB • JMJD2A is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.This JMJD2A polyclonal antibody was raised against an N-terminal recombinant fragment of JMJD2A. This fragment (amino acids 1-350) includes the JMJN and JMJC domains but not the two LAP/PHD zinc finger or Tudor domains of the 1,064 amino acid protein.
Brand:CaymanSKU:10382- 500 µlAvailable on backorder
Immunogen: human recombinant JMJD2D amino acids 1-354 • Host: Rabbit • Species Reactivity: (+) Human and mouse JMJD2D • Application(s): FC, ICC, IP, and WB • JMJD2D is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.
Brand:CaymanSKU:10383- 1 ea Jumonji Domain Containing 2D (JMJD2D) is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.{16420} This JMJD2D polyclonal antibody was raised against a N-terminal recombinant fragment of JMJD2D. JMJD2D is detected at 60 kDa by western blotting using a DLD1 cell lysate as a positive control.
Brand:CaymanSKU:10383 - 1 eaAvailable on backorder
Immunogen: human recombinant JMJD2D amino acids 1-354 • Host: Rabbit • Species Reactivity: (+) Human and mouse JMJD2D • Application(s): FC, ICC, IP, and WB • JMJD2D is a lysine specific demethylase with emerging roles in histone modification or epigenetic remodeling.
Brand:CaymanSKU:10383- 1 eaAvailable on backorder
Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}
Brand:CaymanSKU:10012699 - 1 mgAvailable on backorder
Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}
Brand:CaymanSKU:10012699 - 100 µgAvailable on backorder
Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}
Brand:CaymanSKU:10012699 - 5 mgAvailable on backorder
Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}
Brand:CaymanSKU:10012699 - 500 µgAvailable on backorder
JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:31781 - 1 mgAvailable on backorder
JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:31781 - 10 mgAvailable on backorder
JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:31781 - 25 mgAvailable on backorder
JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:31781 - 5 mgAvailable on backorder
JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}
Brand:CaymanSKU:11997 - 1 mgAvailable on backorder
JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}
Brand:CaymanSKU:11997 - 5 mgAvailable on backorder
JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}
Brand:CaymanSKU:11997 - 500 µgAvailable on backorder
Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.
Brand:CaymanSKU:10008131 - 1 mgAvailable on backorder
Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.
Brand:CaymanSKU:10008131 - 10 mgAvailable on backorder
Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.
Brand:CaymanSKU:10008131 - 5 mgAvailable on backorder
Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.
Brand:CaymanSKU:10008131 - 50 mgAvailable on backorder
JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}
Brand:CaymanSKU:- JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}
Brand:CaymanSKU:- JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}
Brand:CaymanSKU:-
Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}
Brand:CaymanSKU:-
JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}
Brand:CaymanSKU:30930 - 10 mgAvailable on backorder
JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}
Brand:CaymanSKU:30930 - 25 mgAvailable on backorder
JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}
Brand:CaymanSKU:30930 - 5 mgAvailable on backorder
JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}
Brand:CaymanSKU:30930 - 50 mgAvailable on backorder
JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}
Brand:CaymanSKU:- JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}
Brand:CaymanSKU:- JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}
Brand:CaymanSKU:- JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}
Brand:CaymanSKU:-
The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}
Brand:CaymanSKU:- The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}
Brand:CaymanSKU:- The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}
Brand:CaymanSKU:- The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}
Brand:CaymanSKU:-
JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}
Brand:CaymanSKU:-Available on backorder
JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}
Brand:CaymanSKU:-Available on backorder
JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}
Brand:CaymanSKU:-Available on backorder
JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}
Brand:CaymanSKU:-Available on backorder
JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}
Brand:CaymanSKU:27650 - 10 mgAvailable on backorder
JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}
Brand:CaymanSKU:27650 - 100 mgAvailable on backorder
JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}
Brand:CaymanSKU:27650 - 5 mgAvailable on backorder
JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}
Brand:CaymanSKU:27650 - 50 mgAvailable on backorder
JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.
Brand:CaymanSKU:21869 -Out of stock
JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.
Brand:CaymanSKU:21869 -Out of stock
JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.
Brand:CaymanSKU:21869 -Out of stock
JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.
Brand:CaymanSKU:21869 -Out of stock
Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of posttranscriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. Their catalytic activity is dependent on iron, 2-oxoglutarate (2-OG), and oxygen, and leads to the stabilization of a host of proteins, including the hypoxia-inducible transcription factors in response to oxygen availability.{29642} Inhibitors of PHD have been used to mimic a hypoxic response in order to study a range of oxygen-deprivation-related disorders, including anemia, ulcerative colitis, myocardial ischemia, stroke, and metabolic disorders. JNJ-42041935 is a selective, 2-OG competitive, and reversible inhibitor of PHD enzymes (pKis = 7.91, 7.29, and 7.65 for PHD1, 2, and 3, respectively).{29641} It is >100-fold selective for PHD compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes.{29641} In an inflammation-induced anemia model in rats, 100 µM/kg/day JNJ-42041935 significantly increased the number of circulating reticulocytes and red blood cells, increased blood hemoglobin and hematocrit, and restored mean corpuscular volume and mean cell hemoglobin of red bloods cells.{29641}
Brand:CaymanSKU:- Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of posttranscriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. Their catalytic activity is dependent on iron, 2-oxoglutarate (2-OG), and oxygen, and leads to the stabilization of a host of proteins, including the hypoxia-inducible transcription factors in response to oxygen availability.{29642} Inhibitors of PHD have been used to mimic a hypoxic response in order to study a range of oxygen-deprivation-related disorders, including anemia, ulcerative colitis, myocardial ischemia, stroke, and metabolic disorders. JNJ-42041935 is a selective, 2-OG competitive, and reversible inhibitor of PHD enzymes (pKis = 7.91, 7.29, and 7.65 for PHD1, 2, and 3, respectively).{29641} It is >100-fold selective for PHD compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes.{29641} In an inflammation-induced anemia model in rats, 100 µM/kg/day JNJ-42041935 significantly increased the number of circulating reticulocytes and red blood cells, increased blood hemoglobin and hematocrit, and restored mean corpuscular volume and mean cell hemoglobin of red bloods cells.{29641}
Brand:CaymanSKU:- Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of posttranscriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. Their catalytic activity is dependent on iron, 2-oxoglutarate (2-OG), and oxygen, and leads to the stabilization of a host of proteins, including the hypoxia-inducible transcription factors in response to oxygen availability.{29642} Inhibitors of PHD have been used to mimic a hypoxic response in order to study a range of oxygen-deprivation-related disorders, including anemia, ulcerative colitis, myocardial ischemia, stroke, and metabolic disorders. JNJ-42041935 is a selective, 2-OG competitive, and reversible inhibitor of PHD enzymes (pKis = 7.91, 7.29, and 7.65 for PHD1, 2, and 3, respectively).{29641} It is >100-fold selective for PHD compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes.{29641} In an inflammation-induced anemia model in rats, 100 µM/kg/day JNJ-42041935 significantly increased the number of circulating reticulocytes and red blood cells, increased blood hemoglobin and hematocrit, and restored mean corpuscular volume and mean cell hemoglobin of red bloods cells.{29641}
Brand:CaymanSKU:-
JNJ-42153605 is a positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2; EC50 = 17 nM in CHO cells expressing the human receptor).{48351} In vivo, JNJ-42153605 (3 mg/kg) inhibits mGluR2-mediated rapid eye movement (REM) sleep in rats. It also reverses phencyclidine-induced hyperlocomotion in mice (ED50 = 5.4 mg/kg).
Brand:CaymanSKU:21984 -Out of stock
JNJ-42153605 is a positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2; EC50 = 17 nM in CHO cells expressing the human receptor).{48351} In vivo, JNJ-42153605 (3 mg/kg) inhibits mGluR2-mediated rapid eye movement (REM) sleep in rats. It also reverses phencyclidine-induced hyperlocomotion in mice (ED50 = 5.4 mg/kg).
Brand:CaymanSKU:21984 -Out of stock