Cdk4 Inhibitor

• Target:

  Others|||CDK

• Related Pathways:

  Cell Cycle/Checkpoint|||Others

• Bioactivity:

  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-3? (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.

• Smiles:

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

• Molecular Formula:

  C20H10BrN3O2

• Molecular Weight:

  404.2

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  546102-60-7