CDK

Cat. No.

A54183

CAS No.

2704316-81-2

Abemaciclib metabolite M18

Synonyms: LSN3106729

Abemaciclib metabolite M18 is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), key regulators of the cell cycle. This compound exhibits significant antitumor activity and has been utilized in the formulation of PROTAC-based degraders targeting CDK4/6 alongside a CRBN ligand. Its application in cancer research highlights its potential for therapeutic development in various malignancies.

Cat. No.

A54184

CAS No.

3053716-46-1

ZLC491

ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype.

Cat. No.

A54185

CAS No.

2376577-06-7

M2N12

M2N12 is a potent and highly selective inhibitor of the cell division cycle 25C protein phosphatase (Cdc25C), demonstrating an IC50 value of 0.09 μM. Additionally, M2N12 exhibits significant activity against Cdc25A and Cdc25B with IC50 values of 0.53 μM and 1.39 μM, respectively. This compound shows anti-tumor efficacy and is suitable for various cancer research applications, enabling investigations into cell cycle regulation and its implications in oncology.

Cat. No.

A54186

CAS No.

2768712-71-4

CDK9-IN-13

CDK9-IN-13 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 value of less than 3 nM. This compound effectively modulates transcriptional regulation by inhibiting CDK9's role in phosphorylating the RNA polymerase II elongation complex. Given its high potency, CDK9-IN-13 is a valuable tool for investigating the role of CDK9 in various cellular processes and its potential implications in cancer and other diseases.

Cat. No.

A54187

CAS No.

2044686-42-0

TP-1287

TP-1287 is a prodrug of Alvocidib and functions as an orally active inhibitor of cyclin-dependent kinase 9 (CDK9). By inhibiting CDK9, TP-1287 disrupts transcriptional regulation and induces apoptosis in cancer cells. This reagent is valuable for research on cancer therapeutics and exploring the role of CDK9 in various cellular processes.

Cat. No.

A54188

CAS No.

3030279-55-8

CDK2 degrader 7

CDK2 Degrader 7 is an orally active compound that targets cyclin-dependent kinase 2 (CDK2) for selective degradation. It exhibits effective biological activity with DC50 values of 13 nM in MKN1 cells and 17 nM in TOV21G cells, leading to G1 phase arrest in MKN1 cells. Additionally, CDK2 Degrader 7 demonstrates efficacy in achieving tumor stasis in xenograft models of HCC1569 with CCNE1 amplification. This reagent is valuable for investigating the therapeutic potential in CCNE1-amplified cancers.

Cat. No.

A54189

CAS No.

2531748-80-6

CDK2/4/6-IN-2

CDK2/4/6-IN-2 is a selective inhibitor of cyclin-dependent kinases 2, 4, and 6, exhibiting IC50 values under 1 μM. This compound effectively inhibits cell proliferation and reduces the phosphorylation of the retinoblastoma protein at Ser807/811 in breast cancer cells. CDK2/4/6-IN-2 is suitable for research in cancer biology, particularly in studies focused on breast cancer.

Cat. No.

A54190

CAS No.

2488761-18-6

TMX-3013

TMX-3013 is a selective inhibitor of cyclin-dependent kinases (CDKs), effectively targeting CDK1, CDK2, CDK4, CDK5, and CDK6 with IC50 values of 0.9 nM,

Cat. No.

A54191

CAS No.

2651196-71-1

CDK12-IN-6

CDK12-IN-6 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), demonstrating an IC50 of 1.19 μM at elevated ATP concentrations (2 mM). It exhibits strong specificity, showing no significant inhibition of CDK2/Cyclin E or CDK9/Cyclin T1 at concentrations exceeding 20 μM. This compound is valuable for research into transcription regulation and therapeutic strategies targeting CDK12-related pathways in cancer.

Cat. No.

A54192

CAS No.

2488892-01-7

TMX-2039

TMX-2039 is a potent pan-CDK inhibitor that targets multiple cyclin-dependent kinases, including cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) as well as transcriptional CDKs (CDK7 and CDK9), exhibiting IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. This compound is particularly notable for its utility in the development of PROTACs, facilitating targeted protein degradation and expanding therapeutic strategies in oncology and beyond. TMX-2039 is an essential tool for researchers investigating cell cycle regulation and transcriptional control pathways.

Cat. No.

A54194

CAS No.

2326428-25-3

CDK7-IN-4

CDK7-IN-4 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7), a crucial regulator of cell cycle progression and transcriptional control. This compound exhibits significant anticancer activity by selectively inhibiting the proliferation of various cancer cell lines, including those derived from colon, breast, lung, ovary, and stomach tumors, in a dose-dependent manner. CDK7-IN-4 serves as a valuable tool for research into cancer therapeutics and the underlying mechanisms of CDK7-related oncogenesis.

Cat. No.

A54195

CAS No.

3030271-16-7

CDK2 degrader 2

CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms.

Cat. No.

A54196

CAS No.

222035-13-4

CDK2-IN-3

CDK2-IN-3 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting a potent inhibitory activity with an IC50 of 60 nM. This compound is essential for studying the role of CDK2 in cell cycle regulation and its implications in cancer biology. CDK2-IN-3 can be utilized in various research applications, including drug discovery and the investigation of cell proliferation and differentiation processes.

Cat. No.

A54198

CAS No.

2924122-01-8

CDK2 degrader 4

CDK2 Degrader 4 is a selective degrader that targets cyclin-dependent kinase 2 (CDK2). This compound promotes the degradation of CDK2, thereby inhibiting its activity in cell cycle regulation. CDK2 Degrader 4 is significant for cancer research, providing insights into CDK2's role in tumor growth and proliferation. Its application can aid in the development of targeted therapies for CDK2-dependent malignancies.

Cat. No.

A54200

CAS No.

443798-55-8

Cdk1/2 Inhibitor III

Cdk1/2 Inhibitor III is a potent and selective inhibitor targeting cyclin-dependent kinases 1 and 2, with IC50 values of 0.6 nM and 0.5 nM, respectively. This compound demonstrates a high degree of selectivity, with IC50 values of 32 nM against VEGF-R2 and 140 nM against GSK-3β. In cellular assays, Cdk1/2 Inhibitor III effectively reduces proliferation, exhibiting IC50 values of 20 nM, 35 nM, and 92 nM in HCT-116, HeLa, and A375 cell lines, respectively. Its application is relevant for studies in cancer biology and cell cycle regulation.

Cat. No.

A54201

CAS No.

1092443-55-4

BS-194

BS-194 is a selective and potent cyclin-dependent kinase (CDK) inhibitor, primarily targeting CDK2, CDK1, CDK5, CDK7, and CDK9 with IC50 values of 3, 30, 30, 250, and 90 nM, respectively. This compound effectively inhibits the proliferation of cancer cells, making it a valuable tool for cancer research. BS-194 is particularly relevant for studies focusing on breast and colon cancer, providing insights into cellular mechanisms and potential therapeutic strategies.

Cat. No.

A54202

CAS No.

2654075-94-0

CDK7/12-IN-1

CDK7/12-IN-1 is a selective inhibitor of cyclin-dependent kinases 7 and 12, exhibiting IC50 values of 3 nM and 277 nM, respectively. By inhibiting CDK7 and CDK12, this compound effectively disrupts key signaling pathways involved in tumor growth and proliferation. CDK7/12-IN-1 is a valuable tool for researchers investigating the role of these kinases in cancer biology and therapeutic development.

Cat. No.

A54203

CAS No.

2298317-00-5

Cdk5i peptide

Cdk5i peptide is an inhibitor targeting cyclin-dependent kinase 5 (CDK5), displaying a strong binding affinity for the CDK5/p25 complex with a dissociation constant (Kd) of 0.17 μM. This peptide effectively disrupts the interaction between CDK5 and p25, subsequently reducing the kinase activity of the CDK5/p25 complex. Cdk5i peptide is particularly relevant for research into neurodegenerative diseases, providing a valuable tool for elucidating the role of CDK5 in neuronal function and pathology.

Cat. No.

A54206

CAS No.

2789697-52-3

Zeltociclib

Zeltociclib is a potent cyclin-dependent kinase inhibitor that demonstrates significant antitumor activity. By selectively inhibiting CDK activity, it effectively disrupts cell cycle progression, making it a valuable candidate for cancer research. Zeltociclib is particularly relevant in studies examining therapeutic strategies against various malignancies.

Cat. No.

A54207

CAS No.

3117192-80-7

PROTAC CDK9 degrader-9

PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways.

Cat. No.

A54208

CAS No.

2326428-19-5

CDK7-IN-2

CDK7-IN-2 is a selective inhibitor of cyclin-dependent kinases 7 (CDK7), which plays a critical role in cell cycle regulation and transcriptional activation. By targeting CDK7, this compound disrupts the phosphorylation of the Rbpl subunit of RNA Polymerase II, thereby modulating gene expression. CDK7-IN-2 is valuable for research applications focused on cancer biology, particularly in studying aggressive and treatment-resistant tumor types.

Cat. No.

A54209

CAS No.

2748368-15-0

CDK9-IN-11

CDK9-IN-11 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), a critical regulator of transcription and cell cycle progression. This compound serves as a ligand for the PROTAC CDK9 Degrader-1, facilitating targeted degradation of CDK9. CDK9-IN-11 exhibits significant biological activity in cancer research, making it a valuable tool for studies focused on cell proliferation and transcriptional regulation.

Cat. No.

A54210

CAS No.

1957202-71-9

YKL-1-116

YKL-1-116 is a selective and covalent inhibitor of cyclin-dependent kinase 7 (Cdk7), exhibiting enhanced potency compared to THZ1 against both Cdk7 wild type (Cdk7WT) and Cdk7 activated site mutant (Cdk7as). Importantly, YKL-1-116 does not inhibit Cdk9, Cdk12, or Cdk13, making it a valuable tool for studying Cdk7's role in transcriptional regulation and cellular processes. This compound can be utilized in research applications exploring the therapeutic potential of targeting Cdk7 in cancer and other diseases.

Cat. No.

A54211

CAS No.

220749-41-7

CDK1-IN-2

CDK1-IN-2 is a selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 value of 5.8 μM. This compound is primarily utilized in research focusing on cell cycle regulation and cancer therapeutics. By inhibiting CDK1 activity, CDK1-IN-2 serves as a valuable tool for studying the effects of cell proliferation and apoptosis in various cancer models.

Cat. No.

A54212

CAS No.

2813260-27-2

CDK2-IN-31

CDK2-IN-31 is a potent inhibitor of the CCNE1:CDK2 complex, exhibiting an IC50 of 0.13 μM. It binds to a unique allosteric pocket at the interface of CCNE1 and CDK2, leading to significant structural changes in the CDK2 A-loop that disrupt its active conformation and hinder substrate binding. This compound effectively inhibits the phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells and disrupts the coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 is valuable for research investigating ovarian cancer mechanisms and potential therapeutic targets.