Purvalanol A

Additional information:
Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activation of CDKs contributes to the c-Src transformation. Purvalanol A suppressed the c-Src activity as effectively as the Src-selective inhibitor PP2, and that it reverted the transformed morphology to a nearly normal shape with less cytotoxicity than PP2. Purvalanol A induced a strong G2-M arrest, whereas PP2 weakly acted on the G1-S transition. Furthermore, when compared with PP2, purvalanol A more effectively suppressed the growth of human colon cancer HT29 and SW480 cells, in which Src family kinases and CDKs are activated.|Product information|CAS Number: 212844-53-6|Molecular Weight: 388.89|Formula: C19H25ClN6O|Synonym:|NG-60|Purvalanol A|Purv|NG60|NG 60|Chemical Name: (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol|Smiles: CC(C)N1C=NC2=C1N=C(N[C@@H](CO)C(C)C)N=C2NC1=CC(Cl)=CC=C1|InChiKey: PMXCMJLOPOFPBT-HNNXBMFYSA-N|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|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Glipizide} medchemexpress|{Glipizide} Potassium Channel|{Glipizide} Protocol|{Glipizide} In Vivo|{Glipizide} custom synthesis|{Glipizide} Autophagy} |Drug Formulation: To be determined.{{SARS-CoV-2 S Protein RBD (HEK293)} site|{SARS-CoV-2 S Protein RBD (HEK293)} Biological Activity|{SARS-CoV-2 S Protein RBD (HEK293)} Purity|{SARS-CoV-2 S Protein RBD (HEK293)} custom synthesis|{SARS-CoV-2 S Protein RBD (HEK293)} Epigenetic Reader Domain} |HS Tariff Code: 382200|How to use|In Vitro:|Purvalanol A inhibits cdc28 (S.PMID:24463635 cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI50 of 347 nM[1]. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26, 84 μM. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions.|References:|Obakan P, Arısan ED, Ozfiliz P, Coker-Gürkan A, Palavan-Ãœnsal N. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep. 2013 Nov 5. [Epub ahead of print] PubMed PMID: 24190492.Hikita T, Oneyama C, Okada M. Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. Genes Cells. 2010 Oct;15(10):1051-62. doi: 10.1111/j.1365-2443.2010.01439.x. Epub 2010 Sep 5. PubMed PMID: 20825494.Products are for research use only. Not for human use.|