CDK6
CDK6 (cyclin-dependent kinase 6) is a serine/threonine kinase that forms active complexes with D-type cyclins and regulates G1-phase progression and the G1/S cell-cycle transition through phosphorylation of the retinoblastoma protein (RB), thereby controlling E2F-dependent transcriptional programs[1][2]. Mechanistically, CDK6 integrates mitogenic and hormone-derived signals through cyclin D activation, linking extracellular growth cues to cell-cycle entry and cellular proliferation[1][3]. Beyond canonical cell-cycle regulation, accumulating evidence indicates that CDK6 contributes to tumor development and progression in hematologic malignancies and solid tumors, where dysregulated cyclin D-CDK6 signaling promotes uncontrolled proliferation and therapeutic resistance[1][4]. In disease models of hormone receptor-positive breast cancer, aberrant CDK4/6 activity drives RB phosphorylation and cell-cycle progression, making this pathway a central therapeutic target[3][5]. Compared with the closely related isoform CDK4, CDK6 displays distinct regulatory and biological functions, including kinase-dependent and kinase-independent activities that influence transcriptional regulation and tumor adaptation[4][6]. For experimental applications, selective CDK4/6 inhibitors including palbociclib, ribociclib, and abemaciclib block the G1/S transition by suppressing CDK4/6 activity, although these compounds exhibit different affinities toward CDK4 and CDK6 and produce distinct biological and clinical effects[3][5]. CDK6 overexpression, CDK6-containing resistant complexes, and alterations in RB-associated pathways have also been implicated in resistance mechanisms, supporting continued investigation of CDK6-selective targeting strategies in cancer research[5][1].
References:
- [1]. Fassl A, et al. CDK4 and CDK6 kinases: From basic science to cancer therapy. Science. 2022 Jan 14;375(6577):eabc1495. [Content Brief]
- [2]. CDK6 gene information from NCBI.
- [3]. Johnston S, et al. Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors: existing and emerging differences. JNCI Cancer Spectr. 2023 Jul 3;7(4):pkad045. [Content Brief]
- [4]. Nebenfuehr S, et al. The role of CDK6 in cancer. Int J Cancer. 2020 Dec 1;147(11):2988-2995. [Content Brief]
- [5]. Shanabag A, et al. Targeting CDK4/6 in breast cancer. Exp Mol Med. 2025 Feb;57(2):312-322. [Content Brief]
- [6]. Nataraj S E, et al. The Kinase-Dependent and Independent Functions of Cdk4 and Cdk6 Regulate Continuous Proliferation and the Exit From Quiescence Differently[J]. bioRxiv, 2020: 2020.04. 23.058347.
All Product Categories
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CDK6 Related Products (176)
Related Products (176)
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Recombinant Proteins (6)
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Antibodies (1)
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Palbociclib-C4-Boc
0 ImagesCat. No.: HY-176365CAS No.: 2139329-48-7Palbociclib-C4-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK4/6 Palbociclib (HY-50767) and a PROTAC linker (HY-W007803), which recruits E3 ligases. Palbociclib-C4-Boc can be used for synthesis of PROTAC BSJ-03-204 (HY-136250).
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G721-0282
0 ImagesG721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
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CDK2/4/6-IN-1
0 ImagesCat. No.: HY-148213CAS No.: 2803837-13-8CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-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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CDK4/6-IN-29
0 ImagesCat. No.: HY-184707CDK4/6-IN-29 is an orally active and highly selective CDK4/6 inhibitor, with an IC50 of 3.17 nM against CDK4 and an IC50 of 4.91 nM against CDK6. CDK4/6-IN-29 induces apoptosis in non-small cell lung cancer cells, inhibits cancer cell migration, induces G1-phase cell cycle arrest, and exhibits anti-tumor efficacy in vivo. CDK4/6-IN-29 can be used for research related to non-small cell lung cancer.
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CDK2/4/6-IN-3
0 ImagesCat. No.: HY-181501CDK2/4/6-IN-3 (compound 32a) is a CDK2/4/6 inhibitor. CDK2/4/6-IN-3 can be used as a target protein ligand for the synthesis of PROTAC WWZ-11-098 (HY-181490).
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CST651
0 ImagesCat. No.: HY-134303CAS No.: 2489241-16-7Synonyms: PROTAC CDK4/6 degrader 34CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin-dependent kinase CDK4/6 PROTAC degrader with DC50 values of 20 nM and 5.1 nM, respectively. CST651 recruits the VHL E3 ubiquitin ligase to mediate the ubiquitination and proteasomal degradation of CDK4/6. CST651 inhibits cancer cell proliferation and migration. CST651 can be used in research related to breast cancer, multiple myeloma, acute myeloid leukemia, and acute lymphoblastic leukemia.
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CDK9-IN-33
0 ImagesCat. No.: HY-162619CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.
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CDK4/6/BRD4-IN-1
0 ImagesCat. No.: HY-173237CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.
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PROTAC CDK6 Degrader 2
0 ImagesCat. No.: HY-180262PROTAC CDK6 Degrader 2 (compound 48b), the active form of PROTAC CDK6 Degrader 1 (HY-180277), is a potent and selective PROTAC CDK6 degrader that binds strongly to KLHDC2 (KD = 0.005 μM). PROTAC CDK6 Degrader 2 functions through a KLHDC2-dependent and ubiquitin-proteasome-mediated mechanism. PROTAC CDK6 Degrader 2 can be used for cancer research.
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KWZL-7f15
0 ImagesCat. No.: HY-182036KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer.
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Dalpiciclib isethionate
0 ImagesCat. No.: HY-114338BCAS No.: 1980822-14-7Synonyms: SHR-6390 isethionateDalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer.
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CDK4/6/HDAC-IN-1
0 ImagesCat. No.: HY-170651CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC50: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma.
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CDK/HDAC-IN-2
0 ImagesCat. No.: HY-146276CAS No.: 2580938-58-3CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.
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FLT3/CDKs ligand-1
0 ImagesCat. No.: HY-161709CAS No.: 2452019-67-7FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).
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ARUK2010489
0 ImagesCat. No.: HY-178171ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7. ARUK2010489 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 7%, 39% and 26% at 1 μM. ARUK2010489 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).
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CDK7-IN-20
0 ImagesCat. No.: HY-151878CAS No.: 3034210-97-1
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Carbonic anhydrase inhibitor 33
0 ImagesCat. No.: HY-172899Carbonic anhydrase inhibitor 33 (11D) is a dual inhibitor of CA (Carbonic anhydrase) IX/XII and CDK6, with Ki values of 19.7 nM and 26.1 nM for hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 33 (11D) induces G1 arrest and apoptosis. Carbonic anhydrase inhibitor 33 (11D) can be used in the research for NSCLC.
