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 (178)
Related Products (178)
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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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PROTAC CDK4/6 degrader-2
0 ImagesCat. No.: HY-189460CAS No.: 3135520-67-8PROTAC CDK4/6 degrader-2 is an orally active and selective PROTAC degrader that targets CDK4/6 degradation by recruiting cereblon. PROTAC CDK4/6 degrader-2 exhibits DC50 values of 10.9 nM and 9.6 nM for CDK4 and CDK6, respectively. PROTAC CDK4/6 degrader-2 inhibits RB phosphorylation and cell cycle progression. PROTAC CDK4/6 degrader-2 is applicable for research on breast cancer and CDK4/6 inhibitor resistance.
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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
