Cell Cycle

BMS-265246 is a potent new pyra- zolopyridine inhibitor of cdk2/cyclin E and cdk1/cyclin B, as well as cdk4/cyclin D.

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.

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.

GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs) (Ki = 1, 3, and 1 nM for CDK1, CDK2, and CDK4, respectively) with excellent in vitro cellular potency that inhibits the growth of various human tumor cell lines.

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.

Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.

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.

CGP60474 is a potent inhibitor of cyclin-dependent kinase (CDK).

CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.

MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.

GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively).

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.

Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki value of 2.6 uM.

Y-33075 is ROCK (Rho-associated coiled coil-forming protein kinase) inhibitor.

Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.

TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.

Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities.

Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.

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

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.

GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively).

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).

MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines.

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).

AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors.

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.

ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.

NSC 23766 is a selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50 ~ 50 μM) without affecting Cdc42 or RhoA activation.

Kobe2602 is an analog of Kobe0065. Exhibits potent activity to competitively inhibit the binding of H-Ras??GTP to c-Raf-1 RBD with a Ki value of 149 ?? 55 μM.

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??).

EHT 1610 is a highly potent and selective inhibitor of dual-specificity tyrosine-phosphorylation-regulated kinases (DYRK), exhibiting IC₅₀ values of 0.36 nM for DYRK1A and 0.59 nM for DYRK1B. EHT 1610 demonstrates significant antileukemic activity, associated with modulation of cell cycle progression and induction of apoptotic pathways in target cells.

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

SR 3677  is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively).

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

EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.

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

BMS-5 is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.

CASIN is a novel and potent Cdc42 inhibitor.

ID-8 is a DYRK inhibitor. ID 8 also stimulates proliferation at a steady rate (observed in serum-free media supplemented with 10 μM over a 30 day period).

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

KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

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.

KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity.

KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.