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CAS No.: 64984-31-2

Synonyms: PFTμ;2-Phenylethynesulfonamide;NSC 303580

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

描述Hot shock protein 70(HSP70) is an ATP-dependent chaperone that can be induced by cellular stress and its aberrant activation is commonly observed in various malignancies. Pifithrin-μ is an inhibitor of inducible HSP70. It strongly inhibited cell viability with IC₅₀ values of 2.5, 6.1, 4.4, 6.1, 12.7, 8.4 and 11.2 μM in NALM-6, TOM-1, BE-13, Jurkat, KG-1a, K562 and K562-r cells, respectively. In NALM-6 and KG-1a cell lines, incubation with Pifithrin-μ (4 and 5 μM for NALM-6; 40 and 60 μM for KG-1a) for 24h caused a remarkably reduced proportion of cells in S phase. Around 22% of NALM-6 cells were observed in the sub-G0/1 fraction after incubation with 5μM Pifithrin-μ, while only 2% of KG-1a cells were within this fraction after 60 μM Pifithrin-μ treatment. Incubation of NALM-6 cells with Pifithrin-μ at 4, 5 and 6.5 μM resulted in 34, 59 and 80% apoptotic cells above spontaneous apoptosis, respectively. Moreover, the intracellular AKT and ERK1/2 levels in NALM-6 cells was decreased by 10-h incubation of 10μM Pifithrin-μ^[3]. In nude mice inoculated with human pancreatic cancer MiaPaca-2 cells, intraperitoneal injection with Pifithrin-μ (25mg/kg, 100μL) significantly enhanced the inhibitory effect of TRAIL on MiaPaca-2 tumor growth^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human T293 cells	15 μM	Function assay	48 h	Binding affinity to p53 transfected in human T293 cells assessed as reduction in p53 bound-Bcl-2 at 15 uM after 48 hrs	16862141
Saos-2 cells	10 μM	Function assay	48 h	Binding affinity to p53 transfected in human Saos-2 cells harboring pLV-53 assessed as reduction of p53 protein in mitochondria at 10 uM after 48 hrs	16862141
WI38 cells	10 μM	Function assay	24 h	Inhibition of p53-mediated apoptosis in human WI38 cells assessed as cell survival at 10 uM after 24 hrs by methylene blue assay	16862141

动物研究
剂量	Mice: 1 mg/kg or 5 mg/kg^[3] (i.p.), 40 mg/kg^[2] (i.p.)
给药途径	i.p.

实验方案

技术信息

CAS号	64984-31-2	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C8H7NO2S	运输	蓝冰
分子量	181.21	别名	PFTμ;2-Phenylethynesulfonamide;NSC 303580;PFTmu;Pifithrin-µ;PFT-µ

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