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 (233)
Related Products (233)
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Recombinant Proteins (4)
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Antibodies (2)
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Ribociclib succinate hydrate
0 ImagesSynonyms: LEE011 succinate hydrateRRibociclib (LEE011) succinate hydrate 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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Samuraciclib hydrochloride hydrate
0 ImagesCat. No.: HY-103712CPurity: 99.80%Synonyms: CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrateSamuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
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HEMTAC CDK4/6 degrader 1
0 ImagesHEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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CDK4-IN-3
0 ImagesCDK4-IN-3 (Compound 389) is a potent irreversible cyclin-dependent kinase 4 (CDK4) inhibitor (IC50=25 nM, >10-fold selective over CDK6). CDK4-IN-3 arrests the cell cycle at G₁ phase, and induces tumor cell apoptosis. CDK4-IN-3 is promising for research of solid tumors such as breast and lung cancers.
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SRX3177
0 ImagesSRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer.
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Isosilybin B
0 ImagesIsosilybin 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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DB1113
0 ImagesDB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
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Voruciclib hydrochloride
0 ImagesVoruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
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RSS0680
0 ImagesRSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC. RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
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Damulin B
0 ImagesCat. No.: HY-16942CAS No.: 1202868-75-4Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum. Damulin B can inhibit cancer cell apoptosis, decrease mitochondrial membrane potential, inhibit ROS production and cause G0/G1 phase arrest. Damulin B can prevent Cisplatin (HY-17394)-induced acute kidney injury and induce hair growth. Damulin B shows anti-inflammation anti-diabetic and anti-obesity effect. Damulin B can be used for the researches of cancer, inflammation, metabolic disease, such as lung cancer, osteoarthritis and diabetes.
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PNU-292137
0 ImagesPNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model.
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CDK9-IN-7
0 ImagesCDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
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CAN508
0 ImagesCAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
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Inixaciclib
0 ImagesSynonyms: NUV-422Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR+ HER2- metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer.
