CDK4
CDK4 is a cyclin-dependent serine/threonine kinase that partners with D-type cyclins to drive G1-phase progression before DNA synthesis[1]. Mechanistically, cyclin D-CDK4/6 phosphorylates RB, weakens RB-dependent transcriptional repression, and enables late-G1 signaling toward E2F-linked S-phase entry[2]. In cancer models, disruption of the CDK-RB1-E2F pathway supports malignant proliferation, and HR^+/HER2^- breast cancer provides a clinically established setting for CDK4/6 inhibition[3]. Compared with related isoforms, CDK4 and CDK6 share cell-cycle functions, but CDK4 is described as a prominent oncogenic driver in breast cancer, whereas CDK6 has a crucial role in hematopoietic stem-cell differentiation[3][4]. For experimental and translational applications, palbociclib, ribociclib, and abemaciclib inhibit CDK4/6, reduce RB phosphorylation, induce G1 arrest, and support endocrine-therapy combinations in HR^+/HER2^- advanced breast cancer studies[3][5][6][7].
References:
- [1]. Baker SJ, et al. CDK4: a master regulator of the cell cycle and its role in cancer. Genes Cancer. 2022 Aug 25;13:21-45. [Content Brief]
- [2]. Harbour JW, et al. Cdk phosphorylation triggers sequential intramolecular interactions that progressively block Rb functions as cells move through G1. Cell. 1999 Sep 17;98(6):859-69. [Content Brief]
- [3]. Braal CL, et al. Inhibiting CDK4/6 in Breast Cancer with Palbociclib, Ribociclib, and Abemaciclib: Similarities and Differences. Drugs. 2021 Feb;81(3):317-331. [Content Brief]
- [4]. Fassl A, et al. CDK4 and CDK6 kinases: From basic science to cancer therapy. Science. 2022 Jan 14;375(6577):eabc1495. [Content Brief]
- [5]. Finn RS, et al. Palbociclib and Letrozole in Advanced Breast Cancer. N Engl J Med. 2016 Nov 17;375(20):1925-1936. [Content Brief]
- [6]. Hortobagyi GN, et al. Ribociclib as First-Line Therapy for HR-Positive, Advanced Breast Cancer. N Engl J Med. 2016 Nov 3;375(18):1738-1748. [Content Brief]
- [7]. Goetz MP, et al. MONARCH 3: Abemaciclib As Initial Therapy for Advanced Breast Cancer. J Clin Oncol. 2017 Nov 10;35(32):3638-3646. [Content Brief]
All Product Categories
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CDK4 Related Products (229)
Related Products (229)
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Recombinant Proteins (4)
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Antibodies (2)
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Pemrametostat succinate
0 ImagesCat. No.: HY-101563ACAS No.: 1848944-46-6Synonyms: GSK3326595 succinate; EPZ015938 succinateGSK3326595 succinate (EPZ015938 succinate) is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 succinate decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 succinate can be used for research of relapsed/refractory mantle cell lymphoma.
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CGC-11144 hydrochloride
0 ImagesCat. No.: HY-187643CAS No.: 304911-07-7CGC-11144 hydrochloride is a polyamine analog. CGC-11144 hydrochloride reduces the kinase activities of CDK4, CDK2 and CDK6, induces activation of the p53 pathway and p53-dependent p21 expression, and mediates cell cycle regulation, growth inhibition and apoptosis. CGC-11144 hydrochloride induces G1 phase cell cycle arrest, downregulates cyclin D1 and cyclin B1, upregulates cyclin E, induces dephosphorylation of pRb, and inhibits ERα-mediated transcriptional activity by disrupting the DNA binding of Sp1/Sp3 to the ERα promoter, while also stimulating activation of the JNK/AP-1 pathway. CGC-11144 hydrochloride can be used in research related to breast cancer, choroidal neovascularization and cancer.
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Tabersonine hydrochloride
0 ImagesTabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
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MG-002
0 ImagesCat. No.: HY-173172CAS No.: 3076503-34-6MG-002 is an orally active eIF4A1 and eIF4A2 inhibitor with a human eIF4A1 IC50 of 43 nM. MG-002 prevents competent ribosome recruitment to mRNA, inhibits cap-dependent mRNA translation, and engages eIF4A2 via the same RNA clamping mechanism to inhibit mRNA translation. MG-002 induces G2/M cell cycle delay, induces apoptosis, suppresses synthesis of c-MYC and cyclin D1, and shows minimal overt toxicity in mice. MG-002 inhibits primary triple-negative breast cancer tumor growth, attenuates metastatic spread, and enhances anti-neoplastic activity of Doxorubicin (HY-15142A) in pre-clinical models.
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Momilactone B
0 ImagesMomilactone B is an inhibitor of α-amylase and α-glucosidase, with an IC50 of 146.85 μg/mL against Aspergillus oryzae α-amylase and an IC50 of 612.03 μg/mL against Saccharomyces cerevisiae α-glucosidase. Momilactone B upregulates the expression of p21Waf1/Cip1, reduces the kinase activity of Cdk4 and Cdk6, induces cell cycle arrest and apoptosis in cancer cells, and triggers irreversible cell death via cell membrane damage. Momilactone B inhibits the growth of neighboring plant species and serves as a major contributing factor to the allelopathy of rice. Momilactone B can be used in studies related to rice allelopathy, type 2 diabetes, colon cancer and leukemia.
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Antitrypanosomal agent 31
0 ImagesCat. No.: HY-183529CAS No.: 551919-54-1Antitrypanosomal agent 31 is an antitrypanosoma agent with a pEC50 of 6.4. Antitrypanosomal agent 31 inhibits GSK-3β, CDK-2, and CDK-4 with pIC50s of 5.8, 6.9, and 7.1, respectively. Antitrypanosomal agent 31 can be used for the research of human african trypanosomiasis.
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P18IN011
0 ImagesCat. No.: HY-102088CAS No.: 77408-67-4P18IN011 is an inhibitor that specifically targets the interaction between p18(INK4C) and CDK6, with an IC50 of 3.61 μM against mouse p18INK4C. P18IN011 relieves p18-mediated CDK6 inhibition, thereby effectively regulating the G1 phase cell cycle checkpoint. P18IN011 significantly enhances the proliferation, self-renewal and bone marrow reconstitution abilities of hematopoietic stem cells, and increases the frequency of primitive hematopoietic cells to promote cobblestone area formation. Acting specifically on p18-expressing hematopoietic cells via CDK4/6, P18IN011 not only supports the ex vivo expansion of human umbilical cord blood hematopoietic stem cells, but also maintains their long-term reconstitution capacity during in vitro culture to enable multi-lineage transplantation.
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RO0505124
0 ImagesCat. No.: HY-118447CAS No.: 443913-79-9RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitosis, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer.
