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 (315)
Related Products (315)
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Recombinant Proteins (12)
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Antibodies (3)
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CDK2-IN-41
0 ImagesCat. No.: HY-172153CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that exerts anticancer activity by binding to CDK2, thereby inhibiting the cell cycle, inducing cytotoxicity, promoting ROS production, and triggering Apoptosis. CDK2-IN-41 exhibits an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. It holds potential for research in AML-related cancer therapy.
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CDK2/4 ligand 1
0 ImagesCat. No.: HY-W1047040CAS No.: 1211585-07-7
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ZnPc-PEG2-VH032
0 ImagesCat. No.: HY-181906ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC).
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CDK2-IN-12
0 ImagesCat. No.: HY-150573CAS No.: 2410402-88-7CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity.
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ZLMT-72
0 ImagesCat. No.: HY-179633ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC).
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P-gp/CDK2-IN-1
0 ImagesCat. No.: HY-161776P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment.
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CDK2 modulator 1
0 ImagesCat. No.: HY-186126CAS No.: 3066623-95-5CDK2 modulator 1 is a CDK2 modulator with an EC50 < 100 nM and an Emax > 100% of positive control in a TR-FRET proximity assay. CDK2 modulator 1 induces ternary complex formation with CDK2/CCNE1 and CRBN. CDK2 modulator 1 can be used for the research of cancer.
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Multi-kinase-IN-4
0 ImagesCat. No.: HY-149407Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
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CDKI-83
0 ImagesCat. No.: HY-123034CAS No.: 1189558-88-0CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research.
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CDK2-IN-53
0 ImagesCat. No.: HY-180546CDK2-IN-53 (compound 9) is a CDK2 inhibitor with anticancer activity. CDK2-IN-53 selectively inhibits the proliferation of HCT-116 and MCF-7cells with IC50 values of 13.89 and 7.65 μM, respectively, while showing lower cytotoxicity toward normal lung fibroblast (WI-38) cells (IC50 = 71.24 μM). CDK2-IN-53 can be used for cancer research, such as colon and breast cancer.
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Aloisine A
0 ImagesCat. No.: HY-112363CAS No.: 496864-16-5Synonyms: RP107Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
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CDK2-IN-54
0 ImagesCat. No.: HY-180630CAS No.: 3106928-15-5CDK2-IN-54 (Formula I) is a CDK2 inhibitor. CDK2-IN-54 can be used in cancer research such as triple-negative breast cancer, ovarian cancer, bladder cancer, and uterine cancer.
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Cyproheptadine-d3
0 ImagesCat. No.: HY-B1622SCAS No.: 2712455-05-3Cyproheptadine-d3 is the d3-labeled Cyproheptadine (HY-B1622). Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine 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 induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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Carbonic anhydrase inhibitor 14
0 ImagesCat. No.: HY-150570CAS No.: 2410402-75-2Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity.
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PI3Kα-IN-26
0 ImagesCat. No.: HY-176281PI3Kα-IN-26 (Compound 11e) is a PI3Kα inhibitor with an IC50 of 75.31 nM. PI3Kα-IN-26 has a broad-spectrum anticancer activity, such as leukemia, colon and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC50s of 2.74, 3.50, 3.34 and 85.29 μM, respectively).
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Multi-target kinase-IN-7
0 ImagesCat. No.: HY-178157CAS No.: 301820-47-3Multi-target kinase-IN-7 (Compound 1e) is an orally active multi-target kinase inhibitor (IC50 values: CDK2=0.314 μM, EGFR=0.183 μM, HER-2=0.197 μM, VEGFR-2=0.235 μM). Multi-target kinase-IN-7 is promising for research of solid tumors (e.g., lung, breast, prostate cancer).
