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PHA-848125 is a potent, ATP-competitive Cdk2/cyclin A inhibitor (IC50 = 45 nM). PHA-848125 also inhibits additional cdk proteins, but to significantly lesser extent; the activities of Cdk7/cyclin H (IC50 = 0.15 µM), Cdk4/cyclin D1 (IC50 = .0.16 µM), Cdk5/p35 (IC50 = 0.265 µM), as well as Cdk2/cyclin E (IC50 = 0.363 µM) and Cdk1/cyclin B (IC50 = 0.398 µM). Trk A (NTRK1) is also inhibited by PHA-848125 with similar potency to the Cdk′s. PHA-848125 also impairs phosphorylation of the retinoblastoma (Rb) protein at Cdk2 and Cdk4 specific sites, reduces retinoblastoma protein and cyclin A levels, and increases p21(Cip1), p27(Kip1) and p53 expression.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PHA-848125, 5 mg | sc-364581 | 5 mg | $304.00 | |||
PHA-848125, 10 mg | sc-364581A | 10 mg | $555.00 |