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 (196)
Related Products (196)
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Recombinant Proteins (9)
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Antibodies (3)
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Lerociclib
0 ImagesSynonyms: G1T38Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
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TC11
0 ImagesTC11 is a MCL1 degrader and apoptosis inducer. TC11 induces sustained CDK1 activation to phosphorylate and degrade MCL1, activates caspase-3, -8, and -9, inhibits centrosomal-regulatory NPM function to block centrosomal clustering, and triggers apoptosis independent of the cereblon pathway. TC11 blocks tumor cell proliferation in vitro and acts against tumor xenografts in vivo. TC11 can be used for the research of multiple myeloma.
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YK-2168
0 ImagesYK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia.
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Samuraciclib hydrochloride dihydrate
0 ImagesCat. No.: HY-103712BPurity: 99.90%Synonyms: CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrateSamuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
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TMX-3013
0 ImagesTMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).
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Desmethylglycitein
0 ImagesSynonyms: 4',6,7-TrihydroxyisoflavoneDesmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
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(S)-Roscovitine
0 ImagesSynonyms: (S)-Seliciclib; (S)-CYC202(S)-Roscovitine ((S)-Seliciclib; (S)-CYC202) is a potent and cross the blood-brain barrier CDKs inhibitor. (S)-Roscovitine shows neuroprotective efficacy. (S)-Roscovitine has the potential for the research of stroke.
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2,4,6-Trihydroxybenzoic acid
0 Images2,4,6-Trihydroxybenzoic acid is a CDK inhibitor that dose-dependently inhibits recombinant CDK1, CDK2, and CDK4 with IC50 values of 580, 262, and 403 μM, respectively. 2,4,6-Trihydroxybenzoic acid is also a flavonoid metabolite. Cellular uptake of 2,4,6-Trihydroxybenzoic acid depends on functional SLC5A8. 2,4,6-Trihydroxybenzoic acid can be used in colorectal cancer-related research.
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RGB-286638 free base
0 ImagesRGB-286638 free base is a potent inhibitor of CDK and MAPK9. RGB-286638 free base inhibits the activities of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3 and p35-CDK5, with IC50 values of 1, 2, 3, 4, 5 and 5 nM, respectively. RGB-286638 free base inhibits GSK-3β and TAK1, with IC50 values of 3 nM and 5 nM, respectively. RGB-286638 free base induces caspase-dependent Apoptosis in cells. RGB-286638 free base delays tumor growth in an orthotopic glioblastoma mouse model. RGB-286638 free base extends survival in multiple myeloma models. RGB-286638 free base can be used in research related to glioblastoma and multiple myeloma.
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Butyrolactone I
0 ImagesSynonyms: OlomoucinButyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research.
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CGP-74514
0 ImagesCGP-74514 (Compound 13) is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 is promising for research of bladder cancer.
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Samuraciclib hydrochloride hydrate
0 ImagesCat. No.: HY-103712CPurity: 99.80%Synonyms: CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrateSamuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
