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Pifithrin-μ

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Chemical Structure| 64984-31-2 同义名 : 2-Phenylethynesulfonamide;PFTμ;PFT-µ;Pifithrin-µ;NSC 303580
CAS号 : 64984-31-2
货号 : A370437
分子式 : C8H7NO2S
纯度 : 99%+
分子量 : 181.212
MDL号 : MFCD00181531
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(579.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p53
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.52mL

1.10mL

0.55mL

27.59mL

5.52mL

2.76mL

55.18mL

11.04mL

5.52mL
参考文献

[1]Kaiser M, Kuhnl A, et al. Antileukemic activity of the HSP70 inhibitor pifithrin-μ in acute leukemia. Blood Cancer J. 2011 Jul;1(7):e28.

[2]Strom E, Sathe S, et al. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat Chem Biol. 2006 Sep;2(9):474-9. Epub 2006 Jul 23.

[3]Kaiser M, Kühnl A, Reins J, Fischer S, Ortiz-Tanchez J, Schlee C, Mochmann LH, Heesch S, Benlasfer O, Hofmann WK, Thiel E, Baldus CD. Antileukemic activity of the HSP70 inhibitor pifithrin-μ in acute leukemia. Blood Cancer J. 2011 Jul;1(7):e28. doi: 10.1038/bcj.2011.28. Epub 2011 Jul 15. PMID: 22829184; PMCID: PMC3255249.

[4]Monma H, Harashima N, Inao T, Okano S, Tajima Y, Harada M. The HSP70 and autophagy inhibitor pifithrin-μ enhances the antitumor effects of TRAIL on human pancreatic cancer. Mol Cancer Ther. 2013 Apr;12(4):341-51. doi: 10.1158/1535-7163.MCT-12-0954. Epub 2013 Jan 31. PMID: 23371857.