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CDK4/6

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101

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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-136250

    PROTACs CDK Cancer
    BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity .
    BSJ-03-204
  • 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-129180

    PROTACs CDK Cancer
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .
    XY028-133
  • 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-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-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-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-152263

    Hsp-targeting Chimeras CDK Apoptosis Cancer
    HEMTAC 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.
    HEMTAC CDK4/6 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-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 [4] .
    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-122620

    Hetrombopag (tautomerism); SHR-8735 (tautomerism)

    Thrombopoietin Receptor STAT PI3K ERK Apoptosis CDK Cardiovascular Disease Inflammation/Immunology
    Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
    Rafutrombopag (tautomerism)
  • HY-144995

    CDK4/6-IN-11

    PROTACs CDK Cancer
    CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader . CDK4/6-IN-11 consists of a thalidomide-based E3 ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717), a target protein ligand (red part) Palbociclib (HY-50767), and a PROTAC linker (black part) Boc-NH-C4-Br (HY-W007803). E3 ligase ligand and linker can form Thalidomide-NH-amido-C4-Br (HY-170307).
    BSJ-02-162
  • 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-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-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-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-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-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-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-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-145589

    Hetrombopag; SHR-8735

    Thrombopoietin Receptor STAT PI3K ERK Apoptosis CDK Cardiovascular Disease Inflammation/Immunology Cancer
    Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
    Rafutrombopag
  • 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-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-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-136250A

    PROTACs CDK Cancer
    BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity .
    BSJ-03-204 triTFA
  • 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-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-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-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-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

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