产品
编 号:F201348
分子式:C14H9F3N2OS
分子量:310.29
产品类型
结构图
CAS No: 168334-34-7
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产品详情
生物活性:
PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
体内研究:
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.
体外研究:
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.