Purvalanol A

• CAT Number: I002639
• CAS Number: 212844-53-6
• Molecular Formula: C19H25ClN6O
• Molecular Weight: 388.9
• Purity: ≥95%
• Target: Cyclin-Dependent Kinases
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: (2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol
• InChI: InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1
• InChIKey: PMXCMJLOPOFPBT-HNNXBMFYSA-N
• SMILES: CC(C)C(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NC3=CC(=CC=C3)Cl

Purvalanol A (Cat No.:I002639) is a highly potent and selective inhibitor of cyclin-dependent kinases (CDKs). It exhibits strong inhibitory activity against various CDK-cyclin complexes, with IC50 values of 4 nM for cdc2/cyclin B, 70 nM for Cdk2/cyclin A, 35 nM for Cdk2/cyclin E, 850 nM for Cdk4/cyclin D1, and 75 nM for Cdk5-p35. Purvalanol A is cell-permeable and effectively blocks the activity of CDKs, making it a valuable tool in cell cycle and kinase-related research.

Reference

1:Placental passage of olomoucine II, but not purvalanol A, is affected by p-glycoprotein (ABCB1), breast cancer resistance protein (ABCG2) and multidrug resistance-associated proteins (ABCCs). Hofman J, Kučera R, Neumanova Z, Klimes J, Ceckova M, Staud F.Xenobiotica. 2016;46(5):416-23. doi: 10.3109/00498254.2015.1086039. Epub 2015 Sep 12. PMID: 26364927 2:Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro. Cihalova D, Hofman J, Ceckova M, Staud F.PLoS One. 2013 Dec 23;8(12):e83467. doi: 10.1371/journal.pone.0083467. eCollection 2013. PMID: 24376706 Free PMC Article3:Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Obakan P, Arısan ED, Özfiliz P, Çoker-Gürkan A, Palavan-Ünsal N.Mol Biol Rep. 2014 Jan;41(1):145-54. doi: 10.1007/s11033-013-2847-1. Epub 2013 Nov 5. PMID: 24190492 4:Olomoucine II, but not purvalanol A, is transported by breast cancer resistance protein (ABCG2) and P-glycoprotein (ABCB1). Hofman J, Kučera R, Cihalova D, Klimes J, Ceckova M, Staud F.PLoS One. 2013 Oct 8;8(10):e75520. doi: 10.1371/journal.pone.0075520. eCollection 2013. PMID: 24116053 Free PMC Article5:Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone. Hofman J, Ahmadimoghaddam D, Hahnova L, Pavek P, Ceckova M, Staud F.Pharmacol Res. 2012 Mar;65(3):312-9. doi: 10.1016/j.phrs.2011.11.017. Epub 2011 Dec 6. PMID: 22173067 6:Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. Hikita T, Oneyama C, Okada M.Genes Cells. 2010 Oct;15(10):1051-62. doi: 10.1111/j.1365-2443.2010.01439.x. Epub 2010 Sep 5. PMID: 20825494 Free Article7:Two specific drugs, BMS-345541 and purvalanol A induce apoptosis of HTLV-1 infected cells through inhibition of the NF-kappaB and cell cycle pathways. Agbottah E, Yeh WI, Berro R, Klase Z, Pedati C, Kehn-Hall K, Wu W, Kashanchi F.AIDS Res Ther. 2008 Jun 10;5:12. doi: 10.1186/1742-6405-5-12. PMID: 18544167 Free PMC Article8:Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II. Iizuka D, Ogura A, Kuwabara M, Inanami O.Anticancer Drugs. 2008 Jul;19(6):565-72. doi: 10.1097/CAD.0b013e3282fe330e. PMID: 18525315 9:Purvalanol A enhances cell killing by inhibiting up-regulation of CDC2 kinase activity in tumor cells irradiated with high doses of X rays. Iizuka D, Inanami O, Kashiwakura I, Kuwabara M.Radiat Res. 2007 May;167(5):563-71. PMID: 17474786 10:Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus. Maćkowiak M, Kolasiewicz W, Markowicz-Kula K, Wedzony K.Pharmacol Rep. 2005 Nov-Dec;57(6):845-9. PMID: 16382206 Free Article