PIK-75 HCl

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Chemical Structure| 372196-77-5 同义名 : PIK-75; PIK-75 (hydrochloride); PIK-75 hydrochloride
CAS号 : 372196-77-5
货号 : A111266
分子式 : C16H15BrClN5O4S
纯度 : 99%+
分子量 : 488.74
MDL号 : MFCD12546130
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 10 mg/mL(20.46 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
生物活性
靶点

  • p110γ

    p110γ, IC50:76 nM

  • p110α

    p110α, IC50:5.8 nM

  • p110δ

    p110δ, IC50:0.51 μM

  • DNA-PK

    DNA-PK, IC50:2 nM
描述 PIK-75 hydrochloride is a reversible inhibitor selectively targeting DNA-PK and p110α, with IC50 values of 2, 5.8, and 76 nM for DNA-PK, p110α, and p110γ, respectively. Notably, PIK-75 hydrochloride exhibits over 200-fold greater potency against p110α compared to p110β (IC50=1.3 μM)[1][2]. PIK-75 hydrochloride triggers apoptosis[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human MV4-11 cells Cytotoxic assay 72 h Cytotoxicity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay, IC50=0.003 μM 26349627
human NZB5 cells Proliferation assay Antiproliferative activity against human NZB5 cells, IC50=0.069 μM 17869522
human NZOV9 cells Proliferation assay Antiproliferative activity against human NZOV9 cells, IC50=0.066 μM 17869522
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.23mL

2.05mL

1.02mL

20.46mL

4.09mL

2.05mL
参考文献

[1]Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[2]Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58.

[3]Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69.