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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KDM1/CDK1-IN-1
0 ImagesCat. No.: HY-147901CAS No.: 2938990-92-0KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively.
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Cyproheptadine hydrochloride (Standard)
0 ImagesSynonyms: Cyproheptadine HCl (Standard)Cyproheptadine hydrochloride (Standard) (Cyproheptadine HCl (Standard)) is the analytical standard of Cyproheptadine hydrochloride (HY-B0366A). This product is intended for research and analytical applications. 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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CDK7-IN-20
0 ImagesCat. No.: HY-151878CAS No.: 3034210-97-1
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ZNL-02-096
0 ImagesCat. No.: HY-208742CAS No.: 2414418-56-5ZNL-02-096 is a selective Wee1 PROTAC degrader. ZNL-02-096 binds to CRBN and Wee1 to form a ternary complex, inducing CRBN- and proteasome-dependent ubiquitination and proteasomal degradation of Wee1. ZNL-02-096 inhibits recombinant PLK1 with an IC50 of 102 nM, but does not induce its degradation in cells. ZNL-02-096 induces G2/M phase arrest, Apoptosis, transient integrated stress response, upregulation of ATF4, and phosphorylation of GCN2. ZNL-02-096 reduces Tyr15 phosphorylation of CDK1. ZNL-02-096 can be used in research related to ovarian cancer, acute lymphoblastic leukemia, triple-negative breast cancer, multiple myeloma, and pancreatic ductal adenocarcinoma.
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CDK2-IN-47
0 ImagesCat. No.: HY-178112CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer.
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CDK2-IN-55
0 ImagesCDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC50 value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC50 = 26.3 nM), moderate inhibitory effects on Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.
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8-Acetonyldihydronitidine
0 ImagesCat. No.: HY-N21597CAS No.: 80330-39-88‑Acetonyldihydronitidine is a naturally occurring benzophenanthridine alkaloid with antibacterial, antifungal, and anti-proliferative activities against colorectal cancer cells. 8‑Acetonyldihydronitidine inhibits Staphylococcus aureus and exerts a potent antifungal effect against Cladosporium cladosporioides. 8‑Acetonyldihydronitidine activates the p53 signaling pathway, upregulates the expression of target genes including p21, BAX, and FAS, downregulates cyclin A and cyclin B, and induces cell cycle arrest and apoptosis, thereby suppressing the proliferation of colorectal cancer cells. 8‑Acetonyldihydronitidine is used in research related to colorectal cancer, fungal infections, and bacterial infections.
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BMI-1026
0 ImagesCat. No.: HY-123369CAS No.: 477726-77-5BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC50 of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase.
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CDK1-IN-8
0 ImagesCat. No.: HY-179521CAS No.: 3077717-99-5
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KB-0742 hydrochloride
0 ImagesCat. No.: HY-137478B
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BLINK15
0 ImagesCat. No.: HY-173348BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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PKMYT1-IN-12
0 ImagesCat. No.: HY-180484CAS No.: 2974454-59-4
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3-Methylthienyl-carbonyl-JNJ-7706621
0 ImagesCat. No.: HY-141685CAS No.: 443798-09-23-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
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BMS-357075
0 ImagesCat. No.: HY-182734CAS No.: 350509-99-8BMS-357075 is a pan-CDK inhibitor with CDK1 IC50 18 nM, CDK2 IC50 3 nM, CDK4 IC50 26 nM. BMS-357075 induces cytotoxicity in human ovarian cancer A2780 cells. BMS-357075 exhibits anticancer activity in mice against P388 murine leukemia. BMS-357075 can be used for the research of leukemia.
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Dimethyl bisphenolate
0 ImagesCat. No.: HY-180820Dimethyl bisphenolate (Compound DMB) is a natural neolignan derivative with orally active anti-tumor activity. Dimethyl bisphenolate can inhibit cancer cells proliferation, invasion and migration. Dimethyl bisphenolate can activate the p53 signaling pathway, upregulate the expression of p21 protein, inhibit the activity of the CDK1-cyclin B1 complex, and cause cells to stall at the G2/M phase. Dimethyl bisphenolate can induce ROS production, upregulate pro-apoptotic proteins Noxa and Bim, downregulate anti-apoptotic protein Bcl-2, activate caspase-9 and caspase-3, and ultimately induce cell apoptosis. Dimethyl bisphenolate can be used for research of glioblastoma.
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PI3Kα-IN-33
0 ImagesCat. No.: HY-183787PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer.
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CDK1/2/4-IN-1
0 ImagesCat. No.: HY-146253CAS No.: 2414633-49-9CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research.
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CIRc-014
0 ImagesCat. No.: HY-181838CAS No.: 3064485-73-7CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer.
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Antitumor agent-174
0 ImagesCat. No.: HY-161826Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity.
