cdk-2

CDK HDAC-IN-2 is a potent dual HDAC CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK HDAC-IN-2 can arrest the cell cycle in the G2 M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: <8 nM).

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1 2.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3 1 1 4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

Olomoucine is an ATP-competitive inhibitor of Cdk2 cyclin A, Cdc2 CyclinB, CDK2 CyclinE, CDK5 p35, and ERK1 p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.

CVT-313 (NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7 CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

LDC000067 (LDC067) is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.

CDK2, a eukaryotic S/T protein kinase family member, catalyzes the phosphoryl transfer from ATP γ-phosphate to the hydroxyl of serine or threonine (denoted as S0/T0) in a protein substrate.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

NG 52 (NG-52) is a cell-permeable, reversible, and ATP-compatible inhibitor of the cell cycle-regulating kinase Cdc28p and the related Pho85p kinase.

WHI-P180 (Janex 3) is a potent inhibitor of EGFR and Cdk2, with IC50 values of 4.0 µM and 1.0 µM, respectively.

AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM).

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.

PHA-767491 hydrochloride (CAY-10572 hydrochloride) is an effective ATP-competitive dual Cdc7 CDK9 inhibitor (IC50: 10 34 nM). It has ~20-fold selectivity against GSK3-β and CDK1 2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.

Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec