CDK

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.

A54150

CAS No.

3036606-92-2

CDK2 degrader 6

CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers.

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.

A54164

CAS No.

2862772-71-0

CDK2 degrader 3

CDK2 Degrader 3 is a selective degrader of cyclin-dependent kinase 2 (CDK2) that promotes degradation of the target protein. This compound induces G1 cell cycle arrest specifically in CCNE1-amplified cancer cells, making it a valuable tool for studying cell cycle regulation. CDK2 Degrader 3 is particularly relevant for research applications related to breast cancer.

Cat. No.

A54165

CAS No.

3103763-70-5

JWZ-5-13

JWZ-5-13 is a potent CDK7 PROTAC degrader that selectively targets cyclin-dependent kinase 7 for ubiquitin-proteasome system-mediated degradation. It exhibits significant antiproliferative effects on various cancer cell lines, making it an essential tool for studying pathways involved in malignancies such as ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia, and non-small cell lung cancer. This compound facilitates the exploration of targeted protein degradation in cancer biology, offering insights into therapeutic strategies.

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.

Cat. No.

A54173

CAS No.

101622-51-9

Olomoucine

Olomoucine is a potent ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) including CDC2/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, with IC50 values of 7 μM, as well as CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). By targeting these kinases, Olomoucine effectively regulates cell cycle progression and exhibits antitumor activity against melanin-producing tumor cells. This compound is valuable for research into cell cycle regulation and cancer therapy.

Cat. No.

A54174

CAS No.

2488892-09-5

TMX-2172

TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer.

Cat. No.

A54175

CAS No.

2519823-37-9

BSJ-5-63

BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer.

Cat. No.

A54177

CAS No.

2923574-11-0

CDK2 degrader 5

CDK2 Degrader 5 is a targeted degrader for cyclin-dependent kinase 2 (CDK2), achieving a maximum degradation (Dmax) of over 50% and up to 80% in the HiBiT Assay. This compound is integral for probing CDK2's role in cell cycle regulation and cancer biology, making it a valuable tool for researchers investigating therapeutic strategies in oncology. Its selective degradation mechanism allows for a deeper understanding of CDK2 functions in various cellular contexts.

Cat. No.

A54179

CAS No.

186692-45-5

(S)-Roscovitine

Synonyms: (S)-Seliciclib; (S)-CYC202

(S)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating the ability to cross the blood-brain barrier effectively. This compound exhibits neuroprotective properties, making it a valuable tool in the study of neurodegenerative conditions and stroke research. Its ability to modulate CDK activity is pivotal for investigating cell cycle regulation and potential therapeutic strategies in neurological disorders.

Cat. No.

A54180

CAS No.

2761858-59-5

CDK1-IN-1

CDK1-IN-1 is a potent inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 value of 161.2 nM in complex with cyclin B. This compound demonstrates significant antiproliferative activity, selectively targeting cancer cells and inducing apoptosis through a p53-dependent mechanism via the intrinsic apoptotic pathway. CDK1-IN-1 is a promising candidate for targeted antitumor therapies in oncology research.

Cat. No.

A54182

CAS No.

2078047-99-9

CDK4/6-IN-15

CDK4/6-IN-15 is a selective inhibitor targeting cyclin-dependent kinases 4 and 6 (CDK4/6). This compound effectively suppresses the proliferation of cancer cells by inducing a G1 phase cell cycle arrest and inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine 780. CDK4/6-IN-15 is valuable in research focused on cancer biology and therapeutic interventions that modulate cell cycle dynamics.