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PIK-75

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Chemical Structure| 372196-67-3 同义名 : -
CAS号 : 372196-67-3
货号 : A874217
分子式 : C16H14BrN5O4S
纯度 : 98%+
分子量 : 452.283
MDL号 : MFCD12407411
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 : -
动物实验配方：
生物活性
描述 PIK-75 is a reversible selective inhibitor of DNA-PK and p110α, with inhibition IC50s of 2 nM, 5.8 nM and 76 nM for DNA-PK, p110α and p110γ, respectively. p110α was inhibited 200-fold more strongly than p110β by PIK-75 (IC50=1.3 μM)[1][2].PIK-75 also inhibited p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR, and PI4KIIIβ, with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, and ~50 μM, respectively. PIK-75 blocked the phosphorylation of AKT-Thr 308 in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively[1].At a concentration range of 1-1000 nM, acting for 5 min, PIK-75 blocked insulin-induced phosphorylation of AKT on Ser473 and Thr308 in CHO-IR cells in a dose-dependent manner with an IC50 of 78 nM[2].At a concentration of less than 1 μM, acting for 48 hours, PIK-75 inhibits the proliferation and survival of pancreatic cancer cells through apoptosis, and also reduces colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.06mL

2.21mL

1.11mL

22.11mL

4.42mL

2.21mL
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.