Cell Cycle/Checkpoint
The cell cycle is consisted of 4 main phases: Gap 1 (G1), DNA replication (S), Gap 2 (G2), and mitosis (M). There are “checkpoints” mechanism regulates the transition between these phases, at the G1/S boundary, in the S-phase and during G2/M phases. Cell can only pass through these checkpoints when signaling factors are activated and free of DNA damage. Important proteins that control cell cycle events and checkpoints are cullins, cyclins, cyclin-dependent kinases (Cdks), p53 and their inhibitors etc. Cdks family (Cdk2, Cdk3, Cdk4 and Cdk6) are Ser/Thr kinases that regulate cell cycle progression in association with cyclin binding partners (cyclin D, cyclin E and cyclin A) during all four phases. p53 halts the cell cycle if the DNA is damaged and allowing time for DNA repair to progress; it can also initiate apoptosis if DNA damage is too severe to be repaired.
- B6192 ON123300Summary: 多靶点激酶抑制剂,抑制CDK4,Ark5,PDGFRβ,FGFR1,RET和Fyn。
- B6180 FRAX1036Summary: p21活化激酶I(PAK1)抑制剂
- B6165 FRAX486Summary: p21活化激酶(PAK)抑制剂
- B6103 CasinSummary: GTPase Cdc42抑制剂
- B6101 BohemineSummary: CDK抑制剂
- B6093 ISRIBSummary: PERK信号传导抑制剂
- A8739 CCT251545 analogue, Compound 51Summary: CDK8/CDK19的强效选择性抑制剂,具有口服活性
- A8736 THZ531Target: Cyclin-Dependent KinasesSummary: CDK12 和CDK13共价抑制剂
- B6076 MyoseverinSummary: 微管结合分子
- B6075 MonastrolSummary: Eg5 抑制剂