CDK

Cat. No.

A31948

CAS No.

2197029-81-3

CDK9/HDAC1/HDAC3-IN-1

CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models.

Cat. No.

A31959

CAS No.

2919216-33-2

CDK2-IN-9

CDK2-IN-9 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.63 µM. This compound demonstrates significant antiproliferative activity, inducing apoptosis and causing cell cycle arrest at the S and G2/M phases. CDK2-IN-9 is suitable for research applications focused on melanoma and the exploration of CDK2's role in cell cycle regulation and cancer biology.

Cat. No.

A32054

CAS No.

186692-44-4

(Rac)-Roscovitine

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

(Rac)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), functioning by competitively binding to their active sites in place of ATP. This mechanism effectively inhibits CDK phosphorylation activity, leading to apoptosis in cancer cells. As a valuable research tool, (Rac)-Roscovitine is applicable in studies of cancer and various conditions associated with CDK dysregulation, including neurodegenerative diseases, cardiac disorders, and chronic inflammation.

Cat. No.

A32097

CAS No.

2580938-58-3

CDK/HDAC-IN-2

CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy.

Cat. No.

A32102

CAS No.

1804127-83-0

CDK9-IN-18

CDK9-IN-18 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), effectively obstructing its phosphorylation activity. This compound demonstrates significant anticancer properties, promoting apoptosis in various cancer cell lines while exhibiting low cellular toxicity. Its mechanism of action makes CDK9-IN-18 a valuable tool for research into cancer therapeutics and the regulation of gene expression.

Cat. No.

A32109

CAS No.

2851977-85-8

ZLHQ-5f

ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development.

Cat. No.

A32154

CAS No.

2222285-23-4

CDK2/9-IN-1

CDK2/9-IN-1 is an orally active dual inhibitor targeting cyclin-dependent kinases CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM, respectively. This compound induces apoptosis through G2/M cell cycle arrest, demonstrating notable antitumor activity. CDK2/9-IN-1 is useful for research applications focused on cancer biology and the modulation of cell cycle regulation.

Cat. No.

A32223

CAS No.

3099101-44-4

CDK2-IN-55

CDK2-IN-55 is a selective CDK2 inhibitor with an IC50 value of 4.7 nM, also exhibiting significant inhibitory action on CDK1 (IC50 = 26.3 nM), alongside moderate inhibition of Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM). Its weak inhibitory profile on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM) highlights its specificity. CDK2-IN-55 demonstrates potent anti-proliferative effects against various cancer cell lines, effectively inducing cell cycle arrest and apoptosis, making it a valuable tool for research related to colorectal, lung, and cervical cancers.

Cat. No.

A32235

CAS No.

477726-77-5

BMI-1026

BMI-1026 is a potent cyclin-dependent kinase 1 (Cdk1) inhibitor with an IC50 of 2.3 nM. This compound effectively induces apoptosis by interfering with cell cycle progression, specifically by causing a G2-M phase arrest. Its ability to modulate Cdk1 activity makes BMI-1026 valuable for research applications focused on cell division, cancer biology, and therapeutic strategies targeting cell cycle dysregulation.

Cat. No.

A32273

CAS No.

3077717-99-5

CDK1-IN-8

CDK1-IN-8 is a potent inhibitor of Cyclin-dependent kinase 1 (CDK1), primarily targeting the regulation of cell cycle progression. This compound effectively inhibits cell migration, induces apoptosis, and causes cell cycle arrest at the G2/M phase. Notably, CDK1-IN-8 leads to significant downregulation of CDK1 protein levels in HepG2 cells, making it a valuable tool for investigating mechanisms in hepatocellular carcinoma research.

Cat. No.

A32371

CAS No.

2365230-48-2

SY-5102

SY-5102 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7) with a Kd of 0.03 nM. This compound exhibits significant anti-proliferative activity in HCC70 cells, with an EC50 of 9 nM, and effectively modulates CDK7-mediated functions, including downregulation of CDK2 Thr160 and RNA polymerase II Ser5 phosphorylation. SY-5102 induces G2/M cell cycle arrest and decreases c-Myc oncogene expression, leading to enhanced apoptosis in cancer cells. It is particularly relevant for research focused on triple-negative breast cancer (TNBC).

Cat. No.

A32399

CAS No.

2813347-44-1

ZLWT-37

ZLWT-37 is a potent, orally active inhibitor of cyclin-dependent kinases (CDKs), specifically exhibiting IC50 values of 0.002 μM against CDK9 and 0.054 μM against CDK2. This compound effectively induces apoptosis and arrests the cell cycle at the G2/M phase in HCT116 cells. ZLWT-37 is valuable for researching CDK-related pathways and investigating therapeutic strategies in cancer treatment.

Cat. No.

A32418

CAS No.

2762278-95-3

ZDLD13

ZDLD13 is a selective inhibitor of Cyclin-Dependent Kinase 4 (CDK4) with an IC50 of 0.38 μM. This β-carboline compound demonstrates potent anti-cancer activity against HCT116 cells, effectively inhibiting colony formation, invasion, and migration, while also inducing apoptosis and G1 phase cell cycle arrest. Additionally, ZDLD13 significantly inhibits tumor growth in HCT116 tumor xenograft models, making it a valuable tool for cancer research.

Cat. No.

A32432

CAS No.

481724-82-7

CGP-74514 hydrochloride

Synonyms: CGP-74514A

CGP-74514 hydrochloride is a highly selective inhibitor of cyclin-dependent kinase 1 (CDK1) with an IC50 of 25 nM. By inhibiting the CDK1/cyclin B complex, it effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in tumor cells. This compound shows potential for use in research related to bladder cancer and other malignancies driven by CDK1 deregulation.

Cat. No.

A32515

CAS No.

666837-93-0

(E/Z)-SU9516

(E/Z)-SU9516 is a selective inhibitor of cyclin-dependent kinases (CDKs), primarily targeting CDK2, with an IC50 value of 22 nM. This compound also exhibits inhibitory effects on CDK1 and CDK4, with IC50 values of 40 nM and 200 nM, respectively. Its potent inhibition of CDKs makes (E/Z)-SU9516 a valuable tool for studying cell cycle regulation and therapeutic applications in cancer research.

Cat. No.

A32568

CAS No.

129821-08-5

3-ATA

Synonyms: NSC 680434

3-ATA is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), demonstrating both neuroprotective and antitumor properties. This compound has been shown to reduce kainic acid-induced apoptosis in cerebellar granule neurons, making it a valuable tool for investigating neurodegenerative diseases. Its ability to modulate cell cycle progression and prevent neuronal death highlights its potential applications in both cancer research and neuroprotection studies.

Cat. No.

A32599

CAS No.

2995336-58-6

CDK9-Cyclin T1 PPI-IN-1

CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model.

Cat. No.

A32659

CAS No.

3031561-92-6

CDK-IN-9

CDK-IN-9 is a potent cyclin-dependent kinase (CDK) inhibitor that serves as a molecular glue, promoting the interaction between CDK12 and DDB1. With an IC50 value of 4 nM for CDK2/E, CDK-IN-9 facilitates the polyubiquitination and subsequent degradation of cyclin K. Additionally, it induces apoptosis through the dephosphorylation of retinoblastoma protein and RNA polymerase II, making it a valuable tool for research in cancer biology and cell cycle regulation.

Cat. No.

A32667

CAS No.

3064994-97-1

PROTAC CDK4/6/9 degrader 1

PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype.

Cat. No.

A32699

CAS No.

1010440-84-2

(rac)-ZK-304709

(rac)-ZK-304709 is a drug isomer that serves as a multi-targeted inhibitor of tumor growth, particularly in neuroendocrine tumors (NET). This compound inhibits various kinases, including cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). It demonstrates dose-dependent inhibition of NET cell proliferation and colony formation, inducing G2 cell cycle arrest and apoptosis while downregulating MCL1, survivin, and HIF1α expression. By promoting apoptosis and impeding tumor-induced angiogenesis, (rac)-ZK-304709 shows promise as a potential therapeutic agent for NET treatment.

Cat. No.

A32719

CAS No.

3080812-16-1

CDC20-IN-2

CDC20-IN-2 is a selective inhibitor of Cdc20 with a dissociation constant (KD) of 7.65 μM. It effectively induces G2/M phase arrest and promotes the accumulation of DNA damage. By stabilizing critical substrates, including Cyclin B1 and Bim, CDC20-IN-2 enhances apoptotic signaling and inhibits tumor cell proliferation and migration, making it a valuable compound for cancer research and therapy development.

Cat. No.

A32778

CAS No.

2688098-11-3

CDK4/6-IN-10

CDK4/6-IN-10 is a potent and selective inhibitor of CDK4 and CDK6, exhibiting IC50 values of 22 nM and 10 nM, respectively. This compound demonstrates significant antitumor activity and is particularly relevant for research targeting multiple myeloma (MM). Its oral bioavailability combined with its selectivity makes CDK4/6-IN-10 a valuable tool for investigating the therapeutic potential in cancer biology.

Cat. No.

A32806

CAS No.

3052304-23-8

PARP-1/2-IN-2

PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A32853

CAS No.

1983984-04-8

Avotaciclib sulfate

Synonyms: BEY1107 sulfate

Avotaciclib sulfate is an orally bioavailable inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. This compound is particularly useful for research applications focused on oncology, including the study of pancreatic and lung cancer.

Cat. No.

A32929

CAS No.

2634811-35-9

ZSQ836

ZSQ836 is an orally active dual covalent inhibitor of CDK12 and CDK13, demonstrating an EC50 value of 32 nM for CDK12 inhibition. This compound has been shown to induce apoptosis and exhibits significant anticancer efficacy in vivo. ZSQ836 is a valuable tool for investigating the mechanisms and treatment strategies associated with ovarian cancer.