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Purvalanol B is a potent, selective, reversible and ATP-competitive inhibitor of CDK with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1 and CDK5-p35, respectively. Synonyms: NG 95; NG95; NG-95. Grades: >98%. CAS No. 212844-54-7. Molecular formula: C20H25ClN6O3. Mole weight: 432.91.
Purvalanol A, Free Base, 99+%
Purvalanol A is a cell-permeable, potent, and selective cyclin-dependent kinase (CDK) inhibitor. It inhibited CDK kinases with IC50 values of 4 nM for CDC2/cyclin B, 70 nM for CDK2/cyclin A, 35 nM for CDK2/cyclin E, 75 nM for CDK5/p35, and 850 nM for CDK4/cyclin D1. Gray N.S., et al. “Exploiting chemical libraries, structure and genomics in the search for kinase inhibitors.” Science 281: 533-538 (1998). Group: Biochemicals. Grades: Highly Purified. CAS No. 212844-53-6. Pack Sizes: 25mg, 50mg, 100mg. US Biological Life Sciences.
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NG 52
NG 52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p (IC50s = 7 and 2 μM, respectively). It is ineffective against the yeast kinases Kin28p, Srb10, and Cak1p. NG 52 is cell permeable and inhibits the growth of S. cerevisiae (GI50 = 30 μM). It is an analog of purvalanol A (Item No. 14579), a potent inhibitor of mammalian cyclin-dependent kinases. Synonyms: Compound 52; NG-52; NG52. Grades: >98%. CAS No. 212779-48-1. Molecular formula: C16H19ClN6O. Mole weight: 346.81.
Purvalanol A
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. These findings demonstrate that the coordinated inhibition of cell cycle progression and tyrosine kinase signaling by the multi-selective purvalanol A is effective in suppressing cancer progression associated with c-Src up-regulation. Synonyms: Purvalanol A, Purv; NG60; NG-60; NG 60. Grades: 0.98. CAS No. 212844-53-6. Molecular formula: C19H25ClN6O. Mole weight: 388.89.
VMY-1-103
VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma. Synonyms: VMY1-103; VMY 1-103. Grades: 98%. CAS No. 1209002-43-6. Molecular formula: C34H42ClN9O4S. Mole weight: 708.28.
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