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 (313)
Related Products (313)
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Recombinant Proteins (12)
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Antibodies (3)
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CDK12-IN-4
0 ImagesCat. No.: HY-139327CAS No.: 2651196-69-7CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 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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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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NU6301
0 ImagesCat. No.: HY-15570NU6301 is a NU6102 (a CDK2 inhibitor) (HY-15569) prodrug. NU6301 can rapidly generate NU6102 in mouse plasma. NU6301 has anticancer activity against endometrial cancer.
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Ulecaciclib
0 ImagesCat. No.: HY-147409CAS No.: 2075750-05-7Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
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CDK12-IN-9
0 ImagesCat. No.: HY-181645CAS No.: 3024723-74-5
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CDK2-IN-28
0 ImagesCat. No.: HY-161463CAS No.: 3025006-64-5CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM).
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NUAK1-IN-2
0 ImagesCat. No.: HY-172128NUAK1-IN-2 (Compound 24) is a NUAK1 (IC50 of 3.162 nM) and CDK2/4/6 inhibitor. NUAK1-IN-2 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.
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CDK2-IN-51
0 ImagesCDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal 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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Bisindolylmaleimide III hydrochloride
0 ImagesCat. No.: HY-112454CAS No.: 683775-59-9Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer.
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Multi-kinase-IN-6
0 ImagesCat. No.: HY-156470CAS No.: 3009081-73-3Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
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EGFR-IN-45
0 ImagesCat. No.: HY-145867CAS No.: 2765560-03-8
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CDK-IN-9
0 ImagesCat. No.: HY-150641CAS No.: 3031561-92-6CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
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PROTAC CDK2/4/6 Degrader-1
0 ImagesCat. No.: HY-171826CAS No.: 2541626-55-3
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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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CDK2 degrader 11
0 ImagesCat. No.: HY-187363CAS No.: 3121124-92-0CDK2 degrader 11 (Example 5) is a CDK2 degrader. CDK2 degrader 11 is applicable for cancer research.
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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.
