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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
2-Methyl-5,7-Dihydrothieno[3,4-D]Pyrimidine
2-Methyl-5,7-Dihydrothieno[3,4-D]Pyrimidine. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 5,7-Dihydro-2-Methylthieno(3,4-D)Pyrimidine; 5,7-Dihydro-2-Methylthieno[3,4-D]Pyrimidine. Product Category: Thiophenes. CAS No. 36267-71-7. Molecular formula: C7H8N2S. Mole weight: 152.21. Product ID: ACM36267717. Alfa Chemistry ISO 9001:2015 Certified.
5,6-Dihydro-4-hydroxy-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 5,6-DIHYDRO-4H-4-HYDROXY-6-METHYLTHIENO[2,3-B]THIOPYRAN-2-SULPHONAMIDE. Product Category: Heterocyclic Organic Compound. CAS No. 120298-37-5. Molecular formula: C8H11NO3S3. Mole weight: 265.37. Purity: 0.96. IUPACName: 4-hydroxy-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide. Canonical SMILES: CC1CC(C2=C(S1)SC(=C2)S(=O)(=O)N)O. Product ID: ACM120298375. Alfa Chemistry ISO 9001:2015 Certified.
5,6-Dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-4-one. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 5,6-DIHYDRO-4H-6-METHYLTHIENO[2,3-B]THIOPYRAN-4-ONE;5,6-Dihydro-6-methylthieno[2,3-b]thiopyran-4-one(DorzolamideIntermediate);5,6-DIHYDRO-6-METHYL-4-OXO-4H-THIENO[2,3-B]THIOPYRAN;5,6-Dihydro-4-hydroxy-6-methylthieno[2,3-b]thiopyran;5,6-Dihydro-6-methyl-4. Product Category: Heterocyclic Organic Compound. CAS No. 120279-85-8. Molecular formula: C8H8OS2. Mole weight: 184.28. Purity: 0.96. IUPACName: 6-methyl-5,6-dihydrothieno[2,3-b]thiopyran-4-one. Canonical SMILES: CC1CC(=O)C2=C(S1)SC=C2. Density: 1.3. ECNumber: 601-693-8. Product ID: ACM120279858. Alfa Chemistry ISO 9001:2015 Certified.
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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