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.

BS-181 is a potential anti-tumor agent as CDK7 inhibitor.

Indirubin, the active constituent of a Chinese antileukaemia medicine, is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.

SNS-032 (BMS-387032) is a highly selective and potent inhibitor of cyclin-dependent kinases (Cdks) 2, 7, and 9, with in vitro growth inhibitory effects and ability to induce apoptosis in malignant B cells.

Flavopiridol HCl is an inhibitor of cyclin-dependent kinases. The (-)-cis form induces apoptosis in particular tumor cells.

PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity.

AZD5438 is a potent inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 (IC50 values are 16, 6 and 20 nM respectively).

YX-2-107 is a CDK6-degrading PROTAC with an IC50 of 4.4 nM, designed for selective degradation of CDK6. This compound effectively inhibits retinoblastoma (RB) phosphorylation and reduces FOXM1 expression in vitro. YX-2-107 has potential applications in research related to Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), demonstrating its ability to attenuate disease progression in rat models.

CPS2 is a highly potent and selective PROTAC that irreversibly degrades cyclin-dependent kinase 2 (CDK2) with an IC50 of 24 nM. This compound is valuable for exploring the role of CDK2 in cell cycle regulation and has applications in the study of acute myeloid leukemia. Its unique mechanism provides a powerful tool for researchers investigating targeted protein degradation in cancer therapies.

CP-10 is a PROTAC designed to selectively target and degrade cyclin-dependent kinase 6 (CDK6) through its binding to Cereblon. Demonstrating a DC50 of 2.1 nM, this compound effectively inhibits the proliferation of various hematopoietic cancer cell lines, including multiple myeloma, and is capable of degrading both mutated and overexpressed forms of CDK6. Its specific activity makes CP-10 a valuable tool for research into CDK6-related malignancies and potential therapeutic strategies.

SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways.

DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

BSJ-02-162 is a potent PROTAC degrader targeting CDK4/6 through the utilization of a thalidomide-based E3 ligase ligand and a selective CDK4/6 inhibitor. This compound effectively recruits ubiquitin ligases to facilitate the targeted degradation of CDK4/6, thereby modulating cellular responses to cell cycle regulation. BSJ-02-162 is designed for research applications exploring cancer therapies and the mechanisms of protein homeostasis within tumor cells.

CDK2 degrader 1 is a selective molecular glue degrader targeting cyclin-dependent kinase 2 (CDK2). It effectively induces ubiquitination and proteasomal degradation of CDK2 by binding to cereblon, achieving a Dmax greater than 80% and a Ki greater than 1 μM. This compound is utilized in cancer research, providing insights into tumor biology and potential therapeutic strategies.

(S)-CR8 is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating potent inhibitory activity with IC50 values of 0.060 μM for CDK2/cyclin E, 0.080 μM for CDK2/cyclin A, 0.11 μM for CDK9/cyclin T, 0.12 μM for CDK5/p25, and 0.15 μM for CDK1/cyclin B. This compound effectively reduces the survival of SH-SY5Y cells, with an IC50 of 0.40 μM, making it a valuable tool for studying cell cycle regulation and potential therapeutic strategies in cancer research.

Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders.

NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways.

(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis.

Tambiciclib is a potent and selective CDK9 inhibitor with an IC50 of 1 nM, exhibiting over 200-fold selectivity against other cyclin-dependent kinases and significant selectivity over DYRK1A/B and a wide range of kinases. This compound has demonstrated effective in vitro and in vivo antileukemic activity in acute myeloid leukemia (AML) models by inhibiting RNA Polymerase II phosphorylation, leading to downregulation of MCL1 and MYC, and subsequent induction of apoptosis. Tambiciclib is suitable for research applications focused on AML and related oncological studies.

VMY-1-103 is a selective inhibitor of the cyclin-dependent kinase (CDK) complex, effectively arresting the cell cycle at the G1 phase. It has been demonstrated to reduce mitochondrial membrane potential, induce p53 phosphorylation, and trigger PARP cleavage, ultimately activating caspase-3 and initiating apoptosis in LNCaP prostate cancer cells. This compound is valuable for research applications focused on cancer biology and the mechanisms of cell cycle regulation and apoptosis.

PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics.

KDM1/CDK1-IN-1 is a potent inhibitor of both KDM1 and CDK1, exhibiting IC50 values of 0.096 μM and 0.078 μM, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in HOP-92 cancer cells. Additionally, KDM1/CDK1-IN-1 demonstrates significant cytotoxic effects against a range of cell lines, including CCRF-CEM, HOP-92, and Hep-G2, with IC50 values of 16.34 μM, 3.45 μM, and 7.79 μM, respectively. Its ability to target critical regulators of the cell cycle makes KDM1/CDK1-IN-1 valuable for cancer research applications.

CDK1/Cyc B-IN-1 is a selective inhibitor of the CDK1/cyclin B complex, demonstrating an IC50 of 97 nM. This compound effectively induces apoptosis and facilitates G2/M phase cell cycle arrest, making it a valuable tool for studying cell proliferation. CDK1/Cyc B-IN-1 exhibits broad-spectrum cytotoxic activity against various cancer cell lines, supporting its potential in cancer research applications.

RGB-286147 is a selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs), exhibiting IC50 values between 9 to 839 nM. This compound demonstrates minimal activity against non-CDK/CRK kinases. RGB-286147 induces apoptosis in cancer cells and shows significant anti-tumor effects, making it a valuable tool for research in cancer biology and therapeutic development targeting CDK pathways.

LA-CB1 is a CDK4/6 degrader that promotes the degradation of cyclin-dependent kinases 4 and 6 through the ubiquitin-proteasome pathway. This action disrupts the CDK4/6-Cyclin D1-Rb-E2F signaling axis, leading to G0/G1 cell cycle arrest and apoptosis. LA-CB1 demonstrates potent anti-proliferative effects against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In models of triple-negative breast cancer, LA-CB1 significantly inhibits tumor growth in a dose-dependent manner, making it a valuable compound for research in breast cancer therapeutics.

CDK6/PIM1-IN-1 is a potent dual inhibitor targeting CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively, and an additional inhibition of CDK4 at an IC50 of 3.6 nM. This reagent significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 demonstrates strong anti-AML activity, making it a valuable tool for research in cancer biology and therapeutic development.