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| Product | Description | |
|---|---|---|
| PF-3758309 | PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 ( K d = 2.7 nM; K i =18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PF-03758309. CAS No. 898044-15-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13007. |  |
| p21-Activated Kinase Inhibitor II, PF-3758309 (PAK Inhibitor II, PF3758309, (S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide) | A cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (Ki innM/[ATP] inuM = 13.7/200, 18.7/40, 18.1/80. 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 kinase assays; IC50 = 190 and 99nM against PAK1 and PAK3, respectively) by directly targeting the kinase ATP-binding site in a reversible manner (Kd = 4.5nM using rhPAK4300-591 kinase domain). Inhibits PAK4-dependent cellular signaling (IC50 = 24.2nM against TNFalpha-stimulated NF-kappa-B activity in HEK293T) and proliferation (IC50 = 0.24 and 27nM, respectively, against HCT116 and A549 colonies formation) in vitro and the growth of human tumors in nude mice in vivo (10 to 25mg/kg; b.i.d. p.o). Group: Biochemicals. Grades: Highly Purified. CAS No. 898044-15-0. Pack Sizes: 5mg. Molecular Formula: C??H??N?OS. US Biological Life Sciences. |  Worldwide |
| PF-03758309 | PF-3758309, also known as PF-03758309, is a PAK4 inhibitor, is also an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PAK4 inhibitor PF-03758309 binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival. Synonyms: PF03758309; PF 03758309; PF-3758309; PF3758309; PF 3758309. Grades: >98%. CAS No. 898044-15-0. Molecular formula: C25H30N8OS. Mole weight: 490.63. |  |
| PF 3758309 dihydrochloride | PF 3758309 dihydrochloride is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 (IC50 = 1.3 nM; Kd = 2.7 nM). PF 3758309 inhibits phosphorylation of a natural PAK4 substrate in cells with an IC50 ~1 nM and inhibits anchorage-independent growth (expected biology for PAK4 inhibition) at 240 pM. Synonyms: N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide dihydrochloride; PF 3758309 dihydrochloride; PF3758309 dihydrochloride; PF-3758309 dihydrochloride. Grades: ≥98% by HPLC. Molecular formula: C25H30N8OS.2HCl. Mole weight: 563.55. | |
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