CDK1
CDK1 (cyclin-dependent kinase 1) is a highly conserved serine/threonine kinase that functions as a central regulator of eukaryotic cell-cycle progression through cyclin-dependent substrate phosphorylation, particularly during G2/M transition and mitosis[1][2]. Mechanistically, CDK1 forms active complexes with cyclins and coordinates centrosome dynamics, chromosome segregation, spindle organization, and mitotic progression through phosphorylation-dependent signaling networks[2][3]. CDK1 also regulates translational control during mitosis by directly phosphorylating key components of the protein synthesis machinery, including 4E-BP1, thereby linking cell-cycle progression with cellular growth programs[4][5]. In disease models, aberrant CDK1 activity contributes to tumor-cell proliferation, and elevated dependence on CDK1-mediated mitotic signaling has supported its investigation as a therapeutic target across multiple malignancies[6][7]. Compared with related cyclin-dependent kinase isoforms, CDK1 is distinguished by its indispensable role in driving mitotic entry and execution, making it a critical node for cell-cycle control and experimental interrogation of mitotic mechanisms[1][2]. For experimental applications, the ATP-competitive inhibitor RO-3306 is widely used to achieve reversible CDK1 suppression, inducing G2/M arrest and enabling mechanistic studies of mitotic regulation, DNA-damage responses, apoptosis, and cancer-cell vulnerability[6][8]. Furthermore, pharmacological inhibition of CDK1 blocks phosphorylation-dependent oncogenic functions of downstream substrates, including SET isoform 1, which regulates mitotic fidelity, cell migration, invasion, and tumor growth in cellular and xenograft models[3][6].
References:
- [1]. Wikipedia.
- [2]. Łukasik P, et al. Cyclin-Dependent Kinases (CDK) and Their Role in Diseases Development-Review. Int J Mol Sci. 2021 Mar 13;22(6):2935. [Content Brief]
- [3]. Yin L, et al. Cyclin-dependent kinase 1-mediated phosphorylation of SET at serine 7 is essential for its oncogenic activity. Cell Death Dis. 2019 May 16;10(6):385. [Content Brief]
- [4]. Jin Z, et al. Compartmentation of Metabolism of the C12-, C9-, and C5-n-dicarboxylates in Rat Liver, Investigated by Mass Isotopomer Analysis: ANAPLEROSIS FROM DODECANEDIOATE. J Biol Chem. 2015 Jul 24;290(30):18671-7. [Content Brief]
- [5]. Velásquez C, et al. Mitotic protein kinase CDK1 phosphorylation of mRNA translation regulator 4E-BP1 Ser83 may contribute to cell transformation. Proc Natl Acad Sci U S A. 2016 Jul 26;113(30):8466-71. [Content Brief]
- [6]. Kojima K, et al. Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009 Jun;100(6):1128-36. [Content Brief]
- [7]. Shi Z, et al. From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. J Med Chem. 2022 May 12;65(9):6390-6418. [Content Brief]
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CDK1 Related Products (195)
Related Products (195)
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Recombinant Proteins (9)
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Antibodies (3)
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PKMYT1-IN-15
0 ImagesCat. No.: HY-187562PKMYT1-IN-15 is an orally active PKMYT1 inhibitor with an IC50 of 6.02 nM. PKMYT1-IN-15 inhibits the phosphorylation of CDK1 at Thr14. As an antiproliferative agent, DNA damage inducer and antitumor agent, PKMYT1-IN-15 triggers replication-associated DNA damage and cell death in CCNE1-amplified cancer cells, and suppresses tumor growth in the OVCAR3 xenograft model. PKMYT1-IN-15 can be used for the research of CCNE1-amplified cancers (e.g., ovarian cancer, breast cancer).
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CGP-74514 hydrochloride
0 ImagesCat. No.: HY-118976CAS No.: 481724-82-7Synonyms: CGP-74514ACGP-74514 hydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50: 25 nM). CGP-74514 hydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 hydrochloride is promising for research of bladder cancer.
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Anticancer agent 29
0 ImagesCat. No.: HY-115942CAS No.: 2907774-89-2Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent, with IC50 values of 0.054 μM, 0.127 μM, 0.129 μM, 0.396 μM for CDK2, CDK1, CDK4 and CDK6, respectively.
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GIT1-IN-1
0 ImagesCat. No.: HY-181978CAS No.: 844464-54-6GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.
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Tubulin-IN-65
0 ImagesCat. No.: HY-181763Tubulin-IN-65 (Compound Imp-18) is a Tubulin inhibitor. Tubulin-IN-65 exhibits tubulin-disrupting activity. Tubulin-IN-65 disrupts microtubule integrity. Tubulin-IN-65 induces Apoptosis and increases the expression of CDK1 and Cyclin B1. Tubulin-IN-65 possesses anticancer activity against breast cancer and colorectal cancer. Tubulin-IN-65 can be used in research related to triple-negative breast cancer and colorectal adenocarcinoma.
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Anticancer agent 264
0 ImagesCat. No.: HY-170965Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM. Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins. Anticancer agent 264 can be used for research in the field of cancer-related diseases.
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WEE1/PKMYT1-IN-4
0 ImagesCat. No.: HY-183547CAS No.: 3055032-68-0WEE1/PKMYT1-IN-4 is a selective WEE1/PKMYT1 inhibitor, with IC50 values of 0.185 μM and 2.2 nM for human WEE1 and PKMYT1, respectively. WEE1/PKMYT1-IN-4 inhibits phosphorylation of CDK1 at T14 and Y15, disrupting the G2/M cell cycle checkpoint. WEE1/PKMYT1-IN-4 can be used for the research of colorectal cancer and amplified breast cancer.
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Cyproheptadine hydrochloride-d3
0 ImagesCat. No.: HY-W745430Synonyms: Cyproheptadine HCl-d3Cyproheptadine hydrochloride-d3 (Cyproheptadine HCl-d3) is the d3-labeled Cyproheptadine (hydrochloride) (HY-B0366A). Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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CCNE1 degrader-2
0 ImagesCat. No.: HY-189497CAS No.: 3133169-21-5CCNE1 degrader-2 is an orally active CCNE1 degrader with a paDC50 of 7.7 nM. CCNE1 degrader-2 promotes the targeted degradation of Cyclin E1 protein. CCNE1 degrader-2 inhibits tumor cell proliferation and exerts antitumor activity in CDX in vivo models. CCNE1 degrader-2 is used in research on cancers such as ovarian cancer and breast cancer.
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UNPD139734
0 ImagesCat. No.: HY-181140CAS No.: 116764-24-0UNPD139734 is a CDK-1 inhibitor and PARP-1 inhibitor that forms stable complexes with each target protein. UNPD139734 serves as a lead compound for structural optimization to develop dual-target anticancer agents targeting CDK-1 and PARP-1. UNPD139734 can be used for the research of breast cancer.
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CGP-74514 dihydrochloride
0 ImagesCat. No.: HY-110359CGP-74514 dihydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 dihydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 dihydrochloride is promising for research of bladder cancer.
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PKMYT1-IN-13
0 ImagesCat. No.: HY-181004PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer.
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Aloisine RP106
0 ImagesAloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively.
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PARP1-IN-50
0 ImagesCat. No.: HY-179614CAS No.: 2255341-36-5PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer.
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Indirubin-5-sulfonate
0 ImagesCat. No.: HY-111932CAS No.: 244021-67-8Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
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CDK1-IN-9
0 ImagesCat. No.: HY-182752CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer.
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Cyclin K degrader 2
0 ImagesCat. No.: HY-177780Cyclin K degrader 2 is a molecular glue degrader of Cyclin K. By bridging CDK12 and DDB1, the receptor of the CRL4 E3 ligase, Cyclin K degrader 2 specifically induces the targeted degradation of Cyclin K within the CDK12-Cyclin K complex. Cyclin K degrader 2 can be used in studies related to acute myeloid leukemia.
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HS-36
0 ImagesCat. No.: HY-180912HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC50 values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia.
