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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-p21-activated Kinase (PAK)-PF-3758309
PF-3758309

Chemical Structure : PF-3758309

CAS No.: 898044-15-0

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PF-3758309 (PF 3758309;PF03758309)

货号: PC-43316Not For Human Use, Lab Use Only.

PF-3758309 (PF03758309) is a potent, ATP-competitive p21-activated kinase (PAK) inhibitor with Ki of 18.7 nM, shows similar enzymatic potency against other group B PAKs (PAK5 Ki=18.1 nM, PAK6 Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), less active against PAK2 and PAK3 (IC50=190 nM and 99 nM).

规格 价格 库存 数量
10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2280 In stock
100 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

PF-3758309 (PF03758309) is a potent, ATP-competitive p21-activated kinase (PAK) inhibitor with Ki of 18.7 nM, shows similar enzymatic potency against other group B PAKs (PAK5 Ki=18.1 nM, PAK6 Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), less active against PAK2 and PAK3 (IC50=190 nM and 99 nM).
PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM).
PF-3758309 inhibits PAK4-dependent pathways in proteomic studies and regulates functional activities related to cell proliferation and survival; blocks the growth of multiple human tumor xenografts.

物理化学性质&存储条件

分子量 490.6237
分子式 C25H30N8OS
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

Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-

参考文献

1. Murray BW, et al. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51.

2. Bradshaw-Pierce EL, et al. Front Pharmacol. 2013 Mar 22;4:22.

3. Ryu BJ, et al. Mol Cell Biochem. 2014 Apr;389(1-2):69-77.

4. Chow HY, et al. Cancer Res. 2012 Nov 15;72(22):5966-75.

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