CDK

Cat. No.

A51291

CAS No.

2319747-14-1

LDC4297 hydrochloride

LDC4297 hydrochloride is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), exhibiting an IC50 of 0.13 nM. This compound effectively inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM and demonstrates broad antiviral activity against multiple families of viruses, including Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae, with EC50 values ranging from 0.02 to 1.21 μM. LDC4297 hydrochloride is valuable for research into viral infections and the underlying mechanisms of CDK7 in cellular pathways.

Cat. No.

A51806

CAS No.

748146-89-6

CDK9-IN-30

CDK9-IN-30 is a selective inhibitor of Cyclin-dependent kinase 9 (CDK9), primarily targeting its role in transcription regulation. This compound exhibits potent antiviral activity by disrupting HIV-1 replication, making it a valuable tool for studying HIV-1 pathogenesis and exploring therapeutic strategies. Its inhibition of CDK9 can also provide insights into broader cellular processes related to transcriptional regulation and oncogenesis.

Cat. No.

A53351

CAS No.

252725-86-3

CDK9-IN-34

CDK9-IN-34 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 value of 0.25 μM. It demonstrates significant cytotoxic effects on cancer cell lines HCT116, MCF7, and K652, with IC50 values of 1.43 μM, 3.01 μM, and 50.27 μM, respectively. Additionally, CDK9-IN-34 exhibits antiviral properties against coronavirus 229E, displaying an IC50 of 145.92 μM. This compound serves as a valuable tool for investigating the roles of CDK9 in cancer and viral pathogenesis.

Cat. No.

A53660

CAS No.

2349329-01-5

MG16

MG16 is a prodrug of 10-Methoxycamptothecin, primarily targeting CDK6 and ASK1. It effectively induces cell cycle arrest and apoptosis in cancer cells, demonstrating significant anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer. This compound is valuable for research applications focused on cancer therapeutics and the exploration of cell cycle regulation.

Cat. No.

A53679

CAS No.

3054009-82-1

KI-CDK9d-32

KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A53682

CAS No.

2571068-74-9

YK-2168

YK-2168 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 5.9 nM. By inhibiting the phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain, YK-2168 effectively induces apoptosis in tumor cells and suppresses the expression of CDK9-regulated genes, including MYC and Mcl1. This reagent is valuable for research applications in cancer biology, particularly in the study of leukemia and tumor growth inhibition in CDX mouse models.

Cat. No.

A53702

CAS No.

2416873-72-6

KI-ARv-03

KI-ARv-03 is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC₅₀ of 0.15 μM in the presence of 45 μM ATP, with over 130-fold selectivity for CDK9 relative to other CDKs. This compound effectively reduces androgen receptor (AR)-driven transcription and cellular proliferation in prostate cancer models. KI-ARv-03 is applicable in the study of various malignancies, including leukemia, pancreatic cancer, alveolar rhabdomyosarcoma, and castration-resistant prostate cancer. Additionally, it serves as a ligand for PROTAC synthesis, specifically for generating PROTAC KI-CDK9d-32.

Cat. No.

A53813

CAS No.

3083904-06-4

CDK2/MDM2-IN-1

CDK2/MDM2-IN-1 is a potent dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM for CDK2. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit key regulatory proteins positions it as a promising candidate for studies focused on cell cycle regulation and apoptosis.

Cat. No.

A54125

CAS No.

571189-11-2

Palbociclib hydrochloride

Synonyms: PD-0332991 hydrochloride

Palbociclib hydrochloride is a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6, with IC50 values of 11 nM and 16 nM, respectively. This compound demonstrates significant anti-proliferative activity, effectively inducing cell cycle arrest in malignant cells. Palbociclib hydrochloride is utilized in research focused on HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma, making it a valuable tool for understanding tumor biology and therapeutic responses.

Cat. No.

A54126

CAS No.

1957203-01-8

YKL-5-124

YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control.

Cat. No.

A54128

CAS No.

2443816-41-7

Romaciclib monohydrochloride

Synonyms: SEL120-34A monohydrochloride

Romaciclib monohydrochloride is a selective CDK inhibitor that targets CDK8 and CDK19. This compound exhibits potent inhibition of CDK8/CycC and CDK19/CycC kinase activities with IC50 values of 4.4 nM and 10.4 nM, respectively. Additionally, it weakly inhibits CDK9 with an IC50 of 1070 nM, while having no significant activity against other CDK isoforms. Romaciclib monohydrochloride is known to inhibit the phosphorylation of STAT1 at S727 and STAT5 at S726, demonstrating potential anti-tumor activity valuable for cancer research applications.

Cat. No.

A54129

CAS No.

2416874-75-2

KB-0742 dihydrochloride

KB-0742 dihydrochloride is a selective and orally bioactive inhibitor of CDK9, exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. This compound demonstrates over 50-fold selectivity for CDK9 compared to other CDK kinases, making it a valuable tool for precision research. KB-0742 dihydrochloride possesses strong anti-tumor activity, facilitating investigations into its efficacy in cancer biology and therapeutic applications.

Cat. No.

A54130

CAS No.

1637781-04-4

Dalpiciclib

Synonyms: SHR-6390

Dalpiciclib is a highly selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), demonstrating IC50 values of 12.4 nM and 9.9 nM, respectively. This orally active compound exhibits significant antitumor activity, particularly in breast cancer and esophageal squamous cell carcinoma. Dalpiciclib is utilized in research applications focused on tumor suppression and cell cycle regulation.

Cat. No.

A54134

CAS No.

1226443-41-9

HQ461

HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway.

Cat. No.

A54135

CAS No.

2416873-83-9

KB-0742

KB-0742 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. With over 50-fold selectivity against other CDK kinases, KB-0742 demonstrates significant anti-tumor activity. This compound is particularly valuable for research involving transcriptional regulation, cancer biology, and therapeutic strategies targeting CDK9-associated pathways.

Cat. No.

A54136

CAS No.

2891598-76-6

Dalpiciclib hydrochloride

Synonyms: SHR-6390 hydrochloride

Dalpiciclib hydrochloride is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 12.4 nM and 9.9 nM, respectively. This compound exhibits significant antitumor activity, particularly in the context of breast cancer and esophageal squamous cell carcinoma. Dalpiciclib hydrochloride is valuable for research focused on cell cycle regulation and cancer therapeutics.

Cat. No.

A54137

CAS No.

2062200-97-7

XL413 monohydrochloride

Synonyms: BMS-863233 monohydrochloride

XL413 monohydrochloride is a potent and selective inhibitor of the Cdc7 kinase, operating through an ATP-competitive mechanism with an IC50 of 3.4 nM. In addition to its primary activity, XL413 exhibits significant inhibitory effects on CK2 and PIM1, with respective IC50 values of 215 nM and 42 nM, as well as an EC50 of 118 nM on pMCM. This compound is valuable for exploring cell cycle regulation and kinase signaling pathways in various research applications.

Cat. No.

A54138

CAS No.

2923012-24-0

Atuveciclib

Synonyms: BAY-1143572

Atuveciclib is a highly selective oral inhibitor of PTEFb/CDK9, demonstrating potent activity with an IC50 of 13 nM against the CDK9/CycT1 complex. This compound effectively disrupts transcriptional regulation, making it a valuable tool in cancer research and studies related to transcriptional control. Atuveciclib may be employed in investigations aimed at understanding the roles of CDK9 in various diseases, including cancer and other pathologies linked to aberrant transcriptional activity.

Cat. No.

A54139

CAS No.

2775311-17-4

GFB-12811

GFB-12811 is a highly selective inhibitor of cyclin-dependent kinase 5 (CDK5) with an IC50 of 2.3 nM. Its potent action allows for effective modulation of CDK5 activity, making it a valuable tool for studying neurodegenerative diseases and related signaling pathways. This compound is suitable for research investigating the role of CDK5 in neuronal function and pathology.

Cat. No.

A54143

CAS No.

2138499-06-4

Abemaciclib metabolite M20

Synonyms: LSN3106726

Abemaciclib metabolite M20 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This compound exhibits potent anti-proliferative activity in various cancer cell lines, contributing to its potential use in cancer therapy. Research applications include studying cell cycle regulation and exploring therapeutic strategies for tumors driven by CDK4/6 activity.

Cat. No.

A54144

CAS No.

865317-30-2

CDK5 inhibitor 20-223

Synonyms: CP668863

CDK5 inhibitor 20-223 is a potent inhibitor of cyclin-dependent kinases 2 and 5, exhibiting IC50 values of 6.0 nM and 8.8 nM, respectively. This compound demonstrates significant anti-colorectal cancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selective inhibition of CDK2 and CDK5 provides insights into their roles in cell cycle regulation and oncogenesis.

Cat. No.

A54145

CAS No.

3055472-38-0

CPD-39

CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics.

Cat. No.

A54146

CAS No.

2704316-82-3

Abemaciclib metabolite M18 hydrochloride

Synonyms: LSN3106729 hydrochloride

Abemaciclib metabolite M18 hydrochloride functions as a CDK4/6 inhibitor, exhibiting significant antitumor activity. This compound has been utilized in the design of PROTAC (Proteolysis Targeting Chimera) CDK4/6 degraders in conjunction with a CRBN ligand. Its role in targeted protein degradation research makes it a valuable tool for investigating cell cycle regulation and cancer therapeutics.

Cat. No.

A54147

CAS No.

2244987-03-7

CDK12-IN-2

CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation.

Cat. No.

A54148

CAS No.

2639542-32-6

CDK5-IN-3

CDK5-IN-3 is a highly selective inhibitor of CDK5, demonstrating IC50 values of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. This compound is valuable for investigations into the role of CDK5 in cellular processes and is particularly relevant for research focused on autosomal dominant polycystic kidney disease (ADPKD). Its potency and specificity make CDK5-IN-3 an essential tool for elucidating the molecular mechanisms underlying CDK5-related pathologies.