CDK

Roscovitine (Seliciclib) is a CDK inhibitor that preferentially inhibit multiple enzyme targets including CDK2, CDK7 and CDK9.

PF-06873600 is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with potential antineoplastic activity.

AT7519 is an inhibitor of multiple cyclin-dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.

A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.

abemaciclib (LY2835219) is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.

Atuveciclib, also known as BAY1143572, is a highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I.

Ro 3306 is an ATP-competitive, potent cyclin-dependent kinase (cdk) 1 inhibitor (Ki values are 35 and 110 nM for cdk1/cyclin B1 and cdk1/cyclin A respectively).

BMS-863233, also known as XL-413, is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity.

THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM

PHA-793887, a novel potent inhibitor of Cdk, target on kinds of cyclin-dependent kinase under low concentrations and poses high activity against several cancer cell lines.

SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. It specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.

PD 0332991 Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM respectively.

Kenpaullone is a potent inhibitor of CDK inhibitor (IC₅₀ values are 0.4, 0.68, 7.5, 0.85 µM for CDK1/cyclinB, CDK2/cyclinA, CDK2/cyclinE and CDK5/p25 respectively). Also inhibits GSK-3β and LCK (IC₅₀ values are 0.23 and 0.47 µM respectively) Displays reduced activity for other kinases (IC₅₀ values are 15, 20, 20, 9 µM for c-src, casein kinase 2, ERK1 and ERK2 respectively). Also Generates iPSCs. Displays antiproliferative properties.

PD 0332991 HCl is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.

PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication.

LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

Wogonin is an anti-inflammatory agent and an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase

BAY 1000394 is an orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity.

Flavopiridol (Alvocidib) is a cyclin-dependent kinase inhibitor under clinical development for the treatment of chronic lymphocytic leukemia.

LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.

Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively,

Dinaciclib (SCH 727965) is a potent and selective cyclin-dependent kinase (CDK) inhibitor, selectively inhibiting CDK1, CDK2, CDK5 and CDK9 with IC50 values of 3, 1, 1 and 4 nM respectively.

Palbociclib is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Purvalanol B is a cyclin-dependent kinase inhibitor. IC50 values are 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Selective over a range of other protein kinases (IC50 > 10,000 nM).

NU6102 is selective for CDK1 and CDK2 compared to CDK4/D1 (IC50=1.6 μM), DYRK1A (IC50=0.9 μM), PDK1 (IC50=0.8 μM) and ROCKII (IC50=0.6 μM).

NG52 is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 _mu_M), and the related Pho85p kinase (IC50 = 2 _mu_M).

Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics.

ON123300 is a potent multikinase inhibitor and may be potential useful for brain tumor chemotherapy. ON123300 strongly inhibits Ark5 and CDK4, as well as growth factor receptor tyrosine kinases such as ??-type platelet-derived growth factor receptor (PDGFR??).

MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.

(±)-BAY-1251152 is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

(-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.

BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor.

THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.

Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

GW779439X is an inhibitor of cyclin dependent kinase.

JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM.

PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor.

BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA).

BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader (PROTAC).

SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM).

AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively.

6-(Dimethylamino)purine is a dual inhibitor of protein kinase and CDK.