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 (224)
Related Products (224)
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Recombinant Proteins (5)
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Antibodies (2)
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Palbociclib
0 ImagesSynonyms: PD 0332991Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
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Abemaciclib
0 ImagesSynonyms: LY2835219
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Ribociclib
0 ImagesSynonyms: LEE011RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
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Palbociclib hydrochloride
0 ImagesSynonyms: PD-0332991 hydrochloridePalbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
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RGB-286638
0 ImagesRGB-286638 is a potent inhibitor of CDK and MAPK9. RGB-286638 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 inhibits GSK-3β and TAK1, with IC50 values of 3 nM and 5 nM, respectively. RGB-286638 induces caspase-dependent Apoptosis in cells. RGB-286638 delays tumor growth in an orthotopic glioblastoma mouse model. RGB-286638 extends survival in multiple myeloma models. RGB-286638 can be used in research related to glioblastoma and multiple myeloma.
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CDK4 degrader 1
0 ImagesCDK4 degrader 1 is a selective CDK4 molecular glue degrader. CDK4 degrader 1 induces intracellular CDK4 degradation, and its activity is dependent on DCAF16. CDK4 degrader 1 targets the cysteine residue on DCAF16 through its vinylsulfonylpiperazine domain, thereby mediating the degradation of CDK4. CDK4 degrader 1 can be used in research related to cervical cancer.
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GSK3326595
0 ImagesSynonyms: EPZ015938GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
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Palbociclib monohydrochloride
0 ImagesSynonyms: PD 0332991 monohydrochloridePalbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
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Abemaciclib methanesulfonate
0 ImagesSynonyms: LY2835219 methanesulfonate
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Palbociclib isethionate
0 ImagesSynonyms: PD 0332991 isethionatePalbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
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GSK 3 Inhibitor IX
0 ImagesSynonyms: 6-Bromoindirubin-3'-oxime; BIO; MLS 2052GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
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Samuraciclib hydrochloride
0 ImagesSynonyms: CT7001 hydrochloride; ICEC0942 hydrochlorideSamuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.
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Toyocamycin
0 ImagesToyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM.
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CVT-313
0 ImagesSynonyms: Cdk2 Inhibitor IIICVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
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Ribociclib succinate
0 ImagesSynonyms: LEE011 succinateRRibociclib (LEE011) succinate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
