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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA-PK-PIK-75
PIK-75

Chemical Structure : PIK-75

CAS No.: 372196-77-5

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PIK-75 (PIK-75 hydrochloride, PIK 75)

货号: PC-43460Not For Human Use, Lab Use Only.

PIK-75 is a potent, isoform-selective p110α inhibitor with IC50 of 0.3 nM, displays >100-fold selectivity over p110β, p110δ and PI3K C2b.

规格 价格 库存 数量
5 mg (Free Sample) ￥280 In stock
25 mg ￥1280 In stock
50 mg ￥1980 In stock
100 mg ￥3280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PIK-75 (PIK-75 hydrochloride) is a potent, isoform-selective p110α inhibitor with IC50 of 0.3 nM, displays >100-fold selectivity over p110β, p110δ and PI3K C2b.
PIK-75 blocks the phosphorylation of PKB induced by insulin on both Ser473 and Thr308 in CHO-IR cell (IC50=78 nM), inhibits PI3K activation associated with dramatic suppression of downstream signaling events, including AKT phosphorylation, IKK activation, and NF-kappaB transcription.
PIK-75 potently and dose dependently inhibits in vitro and in vivo production of TNF-alpha and IL-6, diminishes the induced expression of human endothelial cell adhesion molecules (E-selectin, ICAM-1, and VCAM-1), and blocks human monocyte-endothelial cell adhesion.
PIK-75 exhibits significant anti-tumor effectiveness in vivo.

物理化学性质&存储条件

分子量 488.74
分子式 C16H15BrClN5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Benzenesulfonic acid, 2-methyl-5-nitro-, 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide, hydrochloride (1:1)

参考文献

1. Chaussade C, et al. Biochem J. 2007 Jun 15;404(3):449-58.

2. Dagia NM, et al. Am J Physiol Cell Physiol. 2010 Apr;298(4):C929-41.

3. Zheng Z, et al. Mol Pharmacol. 2011 Oct;80(4):657-64.

4. Hayakawa M, et al. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.

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