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Chemical Structure : PF-3758309
CAS No.: 898044-15-0
Catalog No.: 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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $138 | In stock | |
| 50 mg | $228 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 490.6237 | |
| Formula | C25H30N8OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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]- |
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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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