PU-141

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PU-141 是一种有效的选择性 CBP/p300 抑制剂，可抑制 SK-N-SH 细胞生长，GI50 为 0.48 uM。

PU-141 is a potent, selective CBP/p300 inhibitor that inhibits SK-N-SH cell growth with GI50 of 0.48 uM; blocks growth of SK-N-SH neuroblastoma xenografts in mice, also reduces histone lysine acetylation in vivo at concentrations that block neoplastic xenograft growth.

PU141 inhibits cell growth at micromolar concentrations in A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma).PU141 causes both histone hypoacetylation and growth inhibition in vitro. PU141 (25 μM) leads to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation, whereas H3K9 and H4K16 acetylation levels remaine stable after co-treatment of HDAC and HAT inhibitor. The impact on histone acetylation is similar in both SK-N-SH and HCT116 cells.:Cell Viability Assay Cell Line:A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)Concentration:0, 10, 20, 30, 40, 50, and 60 μM Incubation Time:Result:Inhibited cell growth at micromolar concentrations in all screened cell lines. The highest cellular antiproliferative activity was detected for the neuroblastoma SK-N-SH cell line. Western Blot Analysis Cell Line:SK-N-SH neuroblastoma and HCT116 colon carcinoma cells Concentration:25 μM Incubation Time:3 hours Result:Led to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation.

PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo. Animal Model:Male NMRI:nu/nu mice bearing a xenograft model Dosage:12.5 and 25 mg/kg Administration:Administered once intraperitoneally (i.p.) as a detergent containing saline microemulsion; for 24 days Result:Led to significant tumor volume reduction (19%) at 25 mg/kg.

PU141 | PU 141

Chromatin/Epigenetic

HAT

HAT

——

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168334-34-7

310.294

C14H9F3N2OS

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (322.28 mM)

O=C1N(CC2=CC=C(C(F)(F)F)C=C2)SC3=NC=CC=C31

2-(4-(trifluoromethyl)benzyl)isothiazolo[5,4-b]pyridin-3(2H)-one

(-20℃)

With Ice Pack

≥ 2 years