Cdk4 Inhibitor - CAS 546102-60-7

PD 0332991, an unsymmetrical indolocarbazole compound, is cell-permeable and exhibits antiproliferative effects by functioning as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk4/D1 (IC 50 = 76 nM) . Although it can inhibit other Cdks, such as Cdk2/E and Cdk1/B, effectiveness requires higher concentrations (IC 50 = 520 nM and 2.1 μM, respectively) and demonstrates minimal activity against CaMKII, PKA, or GSK-3β (IC 50 ≥ 12.4 μM) . PD 0332991 efficiently inhibits tumor cell growth in HCT-116 and NCI-H460 cell lines with an IC 50 < 3.0 μM, primarily through blocking Rb phosphorylation and inducing G1 cell cycle arrest.

Others, CDK

Cell Cycle/Checkpoint, Others

546102-60-7

C20H10BrN3O2

404.2

O=C1C2=C3C(=C4C(=C2C(=O)N1)C=5C(N4)=CC=CC5)NC=6C3=CC=C(Br)C6

-20°C

Ice Packs

Small Compound