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CDK4/6 inhibitors

" in MedChemExpress (MCE) Product Catalog:

86

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2

Natural
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6

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16297A
    Abemaciclib
    Maximum Cited Publications
    117 Publications Verification

    LY2835219

    CDK Neurological Disease Cancer
    Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib
  • HY-15777
    Ribociclib
    75+ Cited Publications

    LEE011

    CDK Neurological Disease Cancer
    RRibociclib (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 .
    Ribociclib
  • HY-16297
    Abemaciclib methanesulfonate
    Maximum Cited Publications
    117 Publications Verification

    LY2835219 methanesulfonate

    CDK Cancer
    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively .
    Abemaciclib methanesulfonate
  • HY-15777A
    Ribociclib hydrochloride
    75+ Cited Publications

    LEE011 hydrochloride

    CDK Neurological Disease Cancer
    RRibociclib (LEE011) hydrochloride 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 .
    Ribociclib hydrochloride
  • HY-101467
    Trilaciclib
    1 Publications Verification

    G1T28

    CDK Cancer
    Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
    Trilaciclib
  • HY-15777B
    Ribociclib succinate
    75+ Cited Publications

    LEE011 succinate

    CDK Neurological Disease Cancer
    RRibociclib (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 .
    Ribociclib succinate
  • HY-158106
    AZD8421
    1 Publications Verification

    CDK Cancer
    AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer .
    AZD8421
  • HY-138946
    XY028-140
    1 Publications Verification

    CDK PROTACs Cancer
    XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .
    XY028-140
  • HY-112272
    Lerociclib
    2 Publications Verification

    G1T38

    CDK Cancer
    Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
    Lerociclib
  • HY-162318
    MYC degrader 1
    1 Publications Verification

    Molecular Glues c-Myc Cancer
    MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
    MYC degrader 1
  • HY-16297AR

    LY2835219 (Standard)

    Reference Standards CDK Cancer
    Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib (Standard)
  • HY-112280

    CDK4/6/1 Inhibitor

    CDK Cancer
    Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
    Crozbaciclib
  • HY-163786

    PROTACs CDK Apoptosis Cancer
    PROTAC CDK4/6 degrader 1 is a CDK4/CDK6 PROTAC degrader, with DC50 values of 10.5 nM and 2.5 nM, respectively. PROTAC CDK4/6 degrader 1 inhibits the proliferation of Jurkat cells (IC50 = 0.18 μM), arrests the cell cycle at the G1 phase, and induces apoptosis. PROTAC CDK4/6 degrader 1 can be used for cancer research.
    PROTAC CDK4/6 degrader 1
  • HY-142076

    CDK Cancer
    CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
    CDK4/6-IN-15
  • HY-16297AS

    LY2835219-d8

    CDK Cancer
    Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib-d8
  • HY-N0805
    Alisol B 23-acetate
    3 Publications Verification

    23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate

    Apoptosis Reactive Oxygen Species (ROS) CDK MMP PARP FXR Syk Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    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 .
    Alisol B 23-acetate
  • HY-101467A
    Trilaciclib hydrochloride
    1 Publications Verification

    G1T28 hydrochloride

    CDK Cancer
    Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
    Trilaciclib hydrochloride
  • HY-126534A
    Abemaciclib metabolite M18 hydrochloride
    2 Publications Verification

    LSN3106729 hydrochloride

    Ligands for Target Protein for PROTAC CDK Cancer
    Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
    Abemaciclib metabolite M18 hydrochloride
  • HY-15777S

    LEE011-d6

    CDK Cancer
    Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
    Ribociclib-d6
  • HY-126534
    Abemaciclib metabolite M18
    2 Publications Verification

    LSN3106729

    Ligands for Target Protein for PROTAC CDK Cancer
    Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
    Abemaciclib metabolite M18
  • HY-136726

    CINK4

    CDK Cancer
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
    CGP-82996
  • HY-15777C
    Ribociclib succinate hydrate
    75+ Cited Publications

    LEE011 succinate hydrate

    CDK Cancer
    RRibociclib (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 .
    Ribociclib succinate hydrate
  • HY-15777R

    LEE011 (Standard)

    Reference Standards CDK Cancer
    Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
    Ribociclib (Standard)
  • HY-129336
    Abemaciclib metabolite M20
    5 Publications Verification

    LSN3106726

    CDK Cancer
    Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer .
    Abemaciclib metabolite M20
  • HY-137449

    G1T48

    Estrogen Receptor/ERR CDK Cancer
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor .
    Rintodestrant
  • HY-114339

    CDK Cancer
    CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively .
    CDK4/6-IN-2
  • HY-15777AS

    LEE011-d6 hydrochloride

    Isotope-Labeled Compounds CDK Cancer
    Ribociclib-d6 (LEE011-d6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
    Ribociclib-d6 hydrochloride
  • HY-146213

    CDK Cancer
    CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .
    CDK4/6-IN-12
  • HY-153894

    CDK Epigenetic Reader Domain PI3K NF-κB SARS-CoV Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    SRX3177 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 .
    SRX3177
  • HY-169947

    CDK Cancer
    DDO-6079 is a potent CDC37 inhibitor. DDO-6079 inhibits HSP90-CDC37 and CDC37-CDK4/6 chaperone complex by binding to an allosteric site on CDC37. DDO-6079 decreases the thermostability of CDK6 .
    DDO-6079
  • HY-171459

    N-Desmethyl Ribociclib

    Drug Metabolite Cytochrome P450 Cancer
    LEQ803 (N-Desmethyl Ribociclib) is a drug metabolite of the CDK4/6 inhibitor Ribociclib (HY-15777), which is produced through metabolism by CYP3A4. LEQ803 has potential application value in the field of oncology .
    LEQ803
  • HY-162318A
    MYC degrader 1 TFA
    1 Publications Verification

    Molecular Glues c-Myc Cancer
    MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
    MYC degrader 1 TFA
  • HY-115992

    CDK Cancer
    CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .
    CDK4/6-IN-9
  • HY-142076A

    CDK Cancer
    CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
    CDK4/6-IN-15 hydrochloride
  • HY-153336

    CDK Cancer
    PRT3645 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC50 values less than 20 nM .
    PRT3645
  • HY-153088

    CDK Cancer
    CDK4/6-IN-16 (example 195) is a potent CDK4 and CDK6 inhibitor, with an IC50 of 0.013 μM for CDK4. CDK4/6-IN-16 can be used for the research of CDK4-mediated disorders, such as cancer .
    CDK4/6-IN-16
  • HY-129336S

    LSN3106726-d8

    CDK Cancer
    Abemaciclib metabolite M20-d8 is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor .
    Abemaciclib metabolite M20-d8
  • HY-15777S1

    LEE011-d8

    CDK Cancer
    Ribociclib-d8 is the deuterium labeled Ribociclib . Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
    Ribociclib-d8
  • HY-151898

    CDK Cancer
    CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases .
    CDK4/6-IN-14
  • HY-15777AR

    LEE011 hydrochloride (Standard)

    Reference Standards CDK Cancer
    Ribociclib (Standard) (LEE011(Standard)) hydrochloride is the analytical standard of Ribociclib hydrochloride (HY-15777A). This product is intended for research and analytical applications. Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    Ribociclib hydrochloride (Standard)
  • HY-146214

    CDK Cancer
    As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
    CDK4/6-IN-13
  • HY-168996

    CDK Apoptosis Cancer
    LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
    LA-CB1
  • HY-134303

    PROTAC CDK4/6 degrader 34

    PROTACs CDK Cancer
    CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin dependent kinase CDK4/6 PROTAC degrader. CST651 can degrade CDK4 and CDK6 in MM.1S cells with DC50 values of 20 and 5.1 nM. CST651 can inhibit cancer cells proliferation and migration. CST651 can be used for the research of cancer, such as acute lymphoblastic leukemia . (Structure Note: Pink: CDK4/6 ligand (HY-50767); Blue: VHL ligand (HY-125905); Black: linker (HY-W017440))
    CST651
  • HY-155736

    p38 MAPK EGFR Raf CDK c-Met/HGFR Cancer
    MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WT IC50=281 nM, c-MET IC50=205 nM, B-RAF WT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790M IC50=69 nM and B-RAF V600E IC50=83 nM) .
    MAPK-IN-2
  • HY-16297R

    LY2835219 methanesulfonate (Standard)

    Reference Standards CDK Cancer
    Abemaciclib (methanesulfonate) (Standard) is the analytical standard of Abemaciclib (methanesulfonate). This product is intended for research and analytical applications. Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively .
    Abemaciclib methanesulfonate (Standard)
  • HY-178516

    CDK PROTACs Cancer
    PROTAC CDK4/6/9 degrader 2 (Compound P4) is a CDK4/6/9 PROTAC prodrug with oral activity and low toxicity. PROTAC CDK4/6/9 degrader 2 can significantly inhibit tumor growth and suppress tumor lung metastasis. PROTAC CDK4/6/9 degrader 2 can be used in the research of cancer such as breast cancer. (Pink: CDK4/6/9 Ligand (HY-168440); Blue: CRBN Ligand (HY-178517); Black: Linker (HY-178512))
    PROTAC CDK4/6/9 degrader 2
  • HY-178452

    PROTACs CDK Apoptosis Cancer
    PROTAC 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)) .
    PROTAC CDK4/6/9 degrader 1
  • HY-112418

    CDK Cancer
    CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells .
    CDK4/6-IN-18
  • HY-108420
    INK4C-IN-2
    1 Publications Verification

    CDK Cancer
    INK4C-IN-2 is a p18 INK4C inhibitor. NK4C-IN-2 promotes hematopoietic stem cells (HSCs) division by inhibiting INK4C and activating CDK4/6, with an ED50 of 5.21 nM. INK4C-IN-2 shows no cytotoxic to normal 32D cells, HSCs, leukemia cell lines and myeloma cell lines .
    INK4C-IN-2
  • HY-174088

    CDK Discoidin Domain Receptor Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis Cancer
    CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .
    CDK4/6/BRD4-IN-2

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