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背景介绍 AR-42 induces histone H3 acetylation, α-tubulin acetylation and p21 up-regulation, which have been considered as the hallmark indicators of HDAC inhibition. AR-42 has been found to modulate several apoptosis inhibitors as well as cell survival regulator, including Akt, Bcl-xL, Bax, Ku70 and surviving, and exert potent antitumor activity against multiple tumor types, such as human prostate and hepatic cancers, at least partially through PI3K/Akt pathway inhibition. AR-42 has been designated an orphan drug by the FDA for the treatment of meningioma and schwannoma of the central nervous system. Meningioma and schwannoma are rare, benign tumors that can present in different locations within the brain and the spinal cord and may cause substantial morbidity. 产品介绍 AR-42 (also known as OSU-HDAC42), a derivative of hydroxamate-tethered phenylbutyrate is a broad-spectrum deacetylase inhibitor of both histone and non-histone proteins. AR-42 treatment induces histone hyperacetylation and p21WAF/CIP1 overexpression, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells.
询价背景介绍 A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells. 产品介绍 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
询价背景介绍 A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells. 产品介绍 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
询价背景介绍 A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells. 产品介绍 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
询价背景介绍 A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Ki of 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood?brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically. 产品介绍 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
询价背景介绍 A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Ki of 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood?brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically. 产品介绍 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
询价背景介绍 A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Ki of 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood?brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically. 产品介绍 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
询价产品介绍 PI-103 is a multi-targeted inhibitor of PI3K for p110_x0003_, p110_x0004_, p110 , and p110 with reported IC50 values of 2 nM, 3 nM, 3 nM, and 15 nM respectively. PI-103 is less potent towards mTOR/DNA-PK with reported IC50 values of 30 nM and 23 nM respectively.
询价产品介绍 PI-103 is a multi-targeted inhibitor of PI3K for p110_x0003_, p110_x0004_, p110 , and p110 with reported IC50 values of 2 nM, 3 nM, 3 nM, and 15 nM respectively. PI-103 is less potent towards mTOR/DNA-PK with reported IC50 values of 30 nM and 23 nM respectively.
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