PU141

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PU141 

PU141 是一种选择性的 HAT 抑制剂。PU141 选择性作用于 CBP 和 p300。PU141 可诱导细胞组蛋白低乙酰化并抑制多种肿瘤细胞系生长。具有抗肿瘤活性。

PU141

PU141 Chemical Structure

CAS No. : 168334-34-7

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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[1].

IC50 & Target

CBP/p300[1]
体外研究
(In Vitro)

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)[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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.

体内研究
(In Vivo)

PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NMRI:nu/nu mice bearing a xenograft model[1]
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.

分子量

310.29

Formula

C14H9F3N2OS
CAS 号

168334-34-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. M Gajer,et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis.2015 Feb 9;4(2):e137.

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