CDK

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.

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.

Cat. No.

A54149

CAS No.

222036-17-1

GW8510

GW8510 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) that also targets ribonucleotide reductase M2 (RRM2). This compound demonstrates significant neuroprotective effects and possesses anticancer properties. It is utilized in scientific research to explore mechanisms of cell proliferation and apoptosis in various cancer models, making it a valuable tool for studying the role of CDK2 in cancer and neurodegenerative diseases.

Cat. No.

A54152

CAS No.

2871872-79-4

DS96432529

DS96432529 is a potent CDK8 inhibitor that exhibits bone anabolic properties. This compound selectively inhibits cyclin-dependent kinase 8, leading to enhanced bone formation and potential therapeutic applications in osteoporosis and other bone-related disorders. Its oral bioavailability makes it a valuable tool for in vivo studies focusing on bone metabolism and development.

Cat. No.

A54155

CAS No.

2488073-20-5

CDK2-IN-23

CDK2-IN-23 is a highly potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.29 nM. This compound demonstrates significant pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models, making it a valuable tool in cancer research. Its selectivity and potency provide a promising avenue for studying CDK2's role in tumorigenesis and evaluating therapeutic strategies in oncology.

Cat. No.

A54156

CAS No.

204188-41-0

CDK9 inhibitor HH1

CDK9 inhibitor HH1 selectively targets cyclin-dependent kinase 9 (CDK9), a key regulator of transcriptional control. This compound effectively inhibits CDK9 activity, leading to decreased transcription of oncogenes associated with cancer progression. HH1 serves as a valuable reagent for investigating therapeutic strategies in cancer research and studying the role of CDK9 in gene expression regulation.

Cat. No.

A54157

CAS No.

2648453-53-4

JH-XVI-178

JH-XVI-178 is a potent and selective inhibitor targeting cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 1 nM and 2 nM, respectively. This compound exhibits low clearance rates and moderate oral pharmacokinetic characteristics, making it suitable for in vivo studies. JH-XVI-178 is valuable for research in transcriptional regulation and cancer biology, particularly in contexts where CDK8 and CDK19 play critical roles in oncogenic signaling pathways.

Cat. No.

A54158

CAS No.

2088715-91-5

MFH290

MFH290 is a selective covalent inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/13). By forming a covalent bond with Cys-1039 of CDK12, MFH290 effectively inhibits the phosphorylation of serine-2 in the C-terminal domain of RNA polymerase II, thus modulating transcriptional regulation. This compound is primarily utilized in cancer research to explore therapeutic strategies targeting CDK12/13-related pathways.

Cat. No.

A54160

CAS No.

2748220-93-9

YKL-5-124 TFA

YKL-5-124 TFA is a selective and irreversible inhibitor of Cyclin-dependent kinase 7 (CDK7), with IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound demonstrates over 100-fold selectivity for CDK7 compared to CDK9 and CDK2, and it shows no activity against CDK12 and CDK13. YKL-5-124 TFA effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on RNA polymerase II phosphorylation, making it a valuable tool for research in cancer biology and transcription regulation.

Cat. No.

A54162

CAS No.

2227392-55-2

BSJ-01-175

BSJ-01-175 is a potent covalent inhibitor of CDK12 and CDK13, targeting cyclin-dependent kinases involved in cell cycle regulation. This compound exhibits strong selectivity and effectively inhibits RNA polymerase II phosphorylation, leading to the downregulation of CDK12-targeted genes in cancer cells. BSJ-01-175 is valuable for research in cancer biology and therapeutic development aimed at CDK-mediated signaling pathways.

Cat. No.

A54163

CAS No.

83-30-7

2,4,6-Trihydroxybenzoic acid

2,4,6-Trihydroxybenzoic acid is a specific inhibitor of cyclin-dependent kinases (CDKs). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound is utilized in studies aimed at elucidating the role of CDKs in cell cycle regulation and tumorigenesis.

Cat. No.

A54167

CAS No.

2640038-22-6

CDK2-IN-30

CDK2-IN-30 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 value of ≤20 nM. By modulating CDK2 activity, this compound plays a critical role in regulating cell cycle progression. CDK2-IN-30 is utilized in cancer research to explore therapeutic strategies targeting cell cycle dysregulation, providing valuable insights into tumorigenesis and potential treatment pathways.

Cat. No.

A54168

CAS No.

267654-00-2

BML-259

BML-259 is a potent inhibitor of cyclin-dependent kinase 5 (Cdk5), exhibiting IC50 values of 64 nM and 98 nM for Cdk5 and Cdk2, respectively. This compound is valuable in research focused on neurodegenerative diseases and neuronal signaling pathways since Cdk5 plays a critical role in neuronal development and function. Its selective inhibition can enhance understanding of Cdk5-related mechanisms and potential therapeutic applications.

Cat. No.

A54169

CAS No.

2020052-55-3

CDK12-IN-E9

CDK12-IN-E9 is a potent and selective covalent inhibitor of cyclin-dependent kinase 12 (CDK12), with additional non-covalent inhibitory activity towards CDK9. This compound effectively engages its target while minimizing interaction with ABC transporter-mediated efflux mechanisms. Furthermore, CDK12-IN-E9 demonstrates a weak binding affinity to the CDK7/CyclinH complex, exhibiting an IC50 greater than 1 μM. It holds significant potential for research applications in studying transcriptional regulation and cancer biology.

Cat. No.

A54170

CAS No.

3034411-38-3

ZNL-05-044

ZNL-05-044 is a potent inhibitor of cyclin-dependent kinase 11 (CDK11), demonstrating IC50 values of 0.23 μM for CDK11A and 0.27 μM for CDK11B, as assessed using the NanoBRET assay. This compound induces G2/M cell cycle arrest and disrupts RNA splicing mechanisms. ZNL-05-044 is valuable for research applications focusing on cell cycle regulation and the role of CDK11 in RNA processing.

Cat. No.

A54171

CAS No.

2375554-02-0

Senexin C

Senexin C is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8/19). It exhibits a favorable pharmacokinetic profile, promoting tumor-specific enrichment and eliciting tumor pharmacodynamic responses. Senexin C effectively inhibits the proliferation of MV4-11 leukemia cells, demonstrating good tolerability, making it a valuable tool for research into cancer therapeutics and cell cycle regulation.

Cat. No.

A54172

CAS No.

1132609-87-0

PKCζ-IN-1

PKCζ-IN-1 is a selective inhibitor of Protein Kinase C zeta (PKCζ) and Cyclin-Dependent Kinase 2 (CDK2). It exhibits an IC50 value of 5.18 nM for PKCζ and 1.04 μM for CDK2, demonstrating a remarkable 200-fold selectivity. PKCζ-IN-1 effectively reduces CDK2 activity while simultaneously inhibiting PKCζ, making it a valuable tool for research in cellular signaling pathways and cancer biology.