CDK2
Cyclin-dependent kinase 2 (CDK2) is a serine/threonine kinase that forms active complexes with cyclin E and cyclin A to regulate the G1/S transition and S-phase progression during cell-cycle control[1][2]. CDK2 functions within the cyclin-CDK regulatory network that coordinates DNA replication, cell proliferation, and checkpoint signaling, thereby linking cell-cycle progression to genome stability mechanisms[2][3]. Mechanistically, aberrant CDK2 activation promotes uncontrolled proliferation and contributes to tumor development in multiple cancer types, making CDK2 a relevant therapeutic target in oncology research[1][3]. In disease models, elevated CDK2 activity has been associated with tumor growth, while genetic or pharmacological suppression of CDK2 can impair cancer-cell proliferation and enhance antitumor responses[1][4]. Compared with related cell-cycle kinases such as CDK1, CDK2 preferentially associates with cyclins E and A and exhibits distinct conformational and regulatory properties that support selective inhibitor development[5]. This isoform-specific behavior is important because CDK1 can compensate for several cell-cycle functions, whereas CDK2 remains particularly relevant in cyclin E-driven and replication-associated oncogenic contexts[1][3]. For experimental applications, selective CDK2 inhibitors are widely used to investigate cell-cycle regulation, DNA-replication stress, and cancer-cell dependency on cyclin E/CDK2 signaling, supporting both mechanistic studies and therapeutic discovery programs[1][3].
References:
- [1]. Tadesse S, et al. Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251. [Content Brief]
- [2]. Pellarin I, et al. Cyclin-dependent protein kinases and cell cycle regulation in biology and disease. Signal Transduct Target Ther. 2025 Jan 13;10(1):11. doi: 10.1038/s41392-024-02080-z. PMID: 39800748; PMCID: PMC11734941. [Content Brief]
- [3]. Asghar U, et al. The history and future of targeting cyclin-dependent kinases in cancer therapy. Nat Rev Drug Discov. 2015 Feb;14(2):130-46. [Content Brief]
- [4]. Chen Y, et al. CDK2 inhibition sensitizes anthracycline-induced immunogenic cell death and enhances the efficacy of anti-PD-1 therapy. Front Immunol. 2025 Jun 10;16:1570040. doi: 10.3389/fimmu.2025.1570040. PMID: 40557162; PMCID: PMC12185487. [Content Brief]
- [5]. Foster WJ, et al. Hippocampal mGluR1-dependent long-term potentiation requires NAADP-mediated acidic store Ca2+ signaling. Sci Signal. 2018 Nov 27;11(558):eaat9093. [Content Brief]
All Product Categories
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CDK2 Related Products (316)
Related Products (316)
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Recombinant Proteins (12)
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Antibodies (3)
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TMX-2172
0 ImagesTMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer.
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CDK2 degrader 5
0 ImagesCDK2 degrader 5 is a CRBN-binding CDK2 molecular glue degrader. CDK2 degrader 5 induces ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 5 can be used for the research of cancer.
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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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CDK12-IN-6
0 ImagesCDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
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CDK4/6-IN-15
0 ImagesCDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.
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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.
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Aristolochic acid D
0 ImagesSynonyms: Aristolochic acid-IVaAristolochic acid D (Aristolochic acid-IVa) is an orally active PDE2 (IC50: 4.673 μM) and CDK2 (IC50: 25 μM) inhibitor that can be isolated from Aristolochia indica L. Aristolochic acid D exhibits anti-inflammatory activity and is non-carcinogenic and non-nephrotoxic. Aristolochic acid D can be used in the research of inflammation and tumor-related diseases.
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Isosilybin B
0 ImagesIsosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
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CDK2-IN-31
0 ImagesCDK2-IN-31 is a CCNE1:CDK2 complex inhibitor with an IC50 of 0.13 μM. CDK2-IN-31 binds to a cryptic allosteric pocket at the CCNE1:CDK2 interface, inducing structural rearrangements of the CDK2 A-loop that disrupt the kinase's active conformation and interfere with substrate binding. CDK2-IN-31 inhibits phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells. CDK2-IN-31 impairs coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 can be used for the research of ovarian cancer.
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CDK2 degrader 4
0 ImagesCDK2 degrader 4 (compound 104) is a potent CDK2 degrader. CDK2 degrader 4 has the potential for the research of cancer.
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GSK-3 inhibitor 3
0 ImagesGSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
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Cdk1/2 Inhibitor III
0 ImagesCdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively.
