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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CDK4/6-IN-8
0 ImagesCat. No.: HY-143258CAS No.: 2649120-22-7
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PROTAC CDK2/4/6 Degrader-1
0 ImagesCat. No.: HY-171826CAS No.: 2541626-55-3
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PROTAC CDK4/6/9 degrader 1
0 ImagesCat. No.: HY-178452CAS No.: 3064994-97-1PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)).
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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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CDK4/6-IN-19
0 ImagesCat. No.: HY-162529CAS No.: 3033950-86-3CDK4/6-IN-19 (Compound II-7) is a CDK4/CDK6 inhibitor with IC50 values of 0.2, 5.0 nM, respectively. CDK4/6-IN-19 also inhibits cell proliferation and can be used in 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.
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CDK4-IN-4
0 ImagesCat. No.: HY-171740CAS No.: 3027994-03-9
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LS-Q2
0 ImagesCat. No.: HY-182986LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
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Rafutrombopag diolamine
0 ImagesCat. No.: HY-125101ACAS No.: 1257792-42-9Rafutrombopag (Hetrombopag) diolamine is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag diolamine can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag diolamine specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag diolamine effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag diolamine protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag diolamine can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease.
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CDK4/6-IN-10
0 ImagesCat. No.: HY-115993CAS No.: 2688098-11-3CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
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MRTX849-amide-C4-(o)-carborane
0 ImagesCat. No.: HY-182044MRTX849-amide-C4-(o)-carborane is a KRASG12C inhibitor with mutation selectivity for cells expressing KRASG12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRASG12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRASG12C-positive cancers.
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AG-012986 dihydrochloride
0 ImagesCat. No.: HY-182470CAS No.: 486414-32-8AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity.
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UNC10112785
0 ImagesCat. No.: HY-128491CAS No.: 748142-06-5UNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC50 of 0.031 μM, human CDK-2 IC50 of 0.016 μM, and human CDK-4 IC50 of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.
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FLT3/CDK4-IN-1
0 ImagesCat. No.: HY-115904CAS No.: 2762296-44-4
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Isosilybin B (Standard)
0 ImagesCat. No.: HY-N7045RCAS No.: 142796-22-3Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin 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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Alisol B 23-acetate (Standard)
0 ImagesSynonyms: 23-Acetylalismol B (Standard); 23-O-Acetylalisol B (Standard); Alisol B monoacetate (Standard)Alisol B 23-acetate (Standard) is the analytical standard of Alisol B 23-acetate (HY-N0805). This product is intended for research and analytical applications. Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma.
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PHA-793887 hydrochloride
0 ImagesCat. No.: HY-11001ACAS No.: 718630-60-5PHA-793887 hydrochloride is a CDK inhibitor (with IC50 values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 hydrochloride inhibits purified GSK3β (IC50 79 nM). PHA-793887 hydrochloride reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 hydrochloride exhibits anticancer activity against leukemia. PHA-793887 hydrochloride can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors.
