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.
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.
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.
别名
Cyclin-dependent kinase 4 Inhibitor
化学信息
分子量
404.2
分子式
C20H10BrN3O2
CAS No.
546102-60-7
储存&溶解度
存储
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
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