1. Search Result
Search Result
Results for "

BET degrader

" in MedChemExpress (MCE) Product Catalog:

68

Inhibitors & Agonists

1

Screening Libraries

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-78695
    JQ-1 carboxylic acid
    Maximum Cited Publications
    9 Publications Verification

    Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC Androgen Receptor Cancer
    JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    JQ-1 carboxylic acid
  • HY-112078

    VHL ligand 2; E3 ligase Ligand 1A

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me
  • HY-42424

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me hydrochloride
  • HY-141438
    SIM1
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity .
    SIM1
  • HY-129937A
    GNE-987
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer .
    GNE-987
  • HY-114407

    PROTACs Epigenetic Reader Domain Cancer
    TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
    TD-428
  • HY-112718

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-10 (dBET37) is a potent BET protein BRD4 degrader, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM .
    PROTAC BET Degrader-10
  • HY-103633
    PROTAC BET Degrader-1
    2 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1
  • HY-103634
    dFKBP-1
    1 Publications Verification

    PROTACs FKBP Cancer
    dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker .
    dFKBP-1
  • HY-117690

    PROTACs Epigenetic Reader Domain Cancer
    dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
    dBRD9
  • HY-123941
    FKBP12 PROTAC dTAG-7
    3 Publications Verification

    dTAG-7

    PROTACs FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional PROTAC degrader. FKBP12 PROTAC dTAG-7 targets FKBP12 F36V and BET BRD4. FKBP12 PROTAC dTAG-7 enables rapid and selective degradation of target proteins, and is suitable for cellular and in vivo studies to analyze protein functions and validate targets .
    FKBP12 PROTAC dTAG-7
  • HY-112429
    HJB97
    2 Publications Verification

    Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
    HJB97
  • HY-114229
    PROTAC BET degrader-3
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET.
    PROTAC BET degrader-3
  • HY-158764

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM
    PROTAC BET Degrader-12
  • HY-129938

    PROTAC-Linker Conjugates for PAC Cancer
    GNE-987 GSH linker-1, a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 (HY-129937A) and disulfide-containing linker. GNE-987 GSH linker-1 remains inactive as a degrader until intracellular release of GNE-987 via disulfide reduction and linker self-immolation. GNE-987 GSH linker-1 can be used for the research of acute myeloid leukemia .
    GNE-987 GSH linker-1
  • HY-145125

    PROTACs Epigenetic Reader Domain Others
    SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
    SJ995973
  • HY-145264

    Epigenetic Reader Domain PROTACs Cancer
    OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
    OARV-771
  • HY-135250B

    E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis Cancer
    Thalidomide-4-O-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12 F36V and BET .
    Thalidomide-4-O-C6-NH2 hydrochloride
  • HY-147046

    Epigenetic Reader Domain Ligands for Target Protein for PROTAC Cancer
    ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).
    ET-JQ1-OH
  • HY-131318

    Ligands for E3 Ligase Cancer
    Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609) .
    Lenalidomide-I
  • HY-123911

    PROTACs Epigenetic Reader Domain Cancer
    dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein .
    dBET23
  • HY-42424A

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me dihydrochloride
  • HY-44103

    PROTAC BRD4-binding moiety 4

    Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Desmethyl-QCA276
  • HY-168546

    PROTACs Epigenetic Reader Domain Cancer
    CFT-1297 is a BET PROTAC degrader that can degrade BRD4 .
    CFT-1297
  • HY-114228
    PROTAC BET degrader-2
    2 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
    PROTAC BET degrader-2
  • HY-161346

    PROTACs Epigenetic Reader Domain Cancer
    EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
    EBET-1055
  • HY-161346A

    PROTACs Epigenetic Reader Domain Cancer
    (Rac)-EBET-1055 is the racemate of EBET-1055 (HY-161346). EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
    (Rac)-EBET-1055
  • HY-130612

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect .
    PROTAC BRD2/BRD4 degrader-1
  • HY-175354

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader targeting BET. PROTAC BET Degrader-13 significantly degrades PML-eGFP-BRD4 fusion protein with a near-complete loss of EGFP+ nuclear puncta with an EC50 of 1.4 μM . Pink: BET ligand (HY-13030); Blue: E3 ligase ligand (HY-W1125585); Black: linker
    PROTAC BET Degrader-13
  • HY-130813

    Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612) .
    BET-IN-6
  • HY-170900

    PROTACs Epigenetic Reader Domain c-Myc MDM-2/p53 Neurological Disease Cancer
    SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma .
    SJ44236
  • HY-157426

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-19 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC50 of 21.1 nM (4h) .
    PROTAC BET Degrader-19
  • HY-157491

    PROTACs Androgen Receptor Epigenetic Reader Domain Cancer
    K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .
    K2-B4-5e
  • HY-111978

    Epigenetic Reader Domain Cancer
    ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .
    ZEN-3862
  • HY-78695A

    Drug Isomer Epigenetic Reader Domain PD-1/PD-L1 Cancer
    (R)-JQ-1 carboxylic acid, is an isomer of JQ-1 carboxylic acid (HY-78695). JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    (R)-JQ-1 carboxylic acid
  • HY-111977

    Epigenetic Reader Domain Cancer
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4 .
    ZEN-3219
  • HY-111979

    Epigenetic Reader Domain Cancer
    ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4 .
    ZEN-3411
  • HY-122703

    Epigenetic Reader Domain Ligands for Target Protein for PROTAC Cancer
    BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
    BETi-211
  • HY-160262

    Androgen Receptor PROTACs Epigenetic Reader Domain Cancer
    PROTAC AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .
    PROTAC AR/BET protein degrader-1
  • HY-156814

    Hedgehog Cancer
    HPP-9 is a Proteolysis-Targeting Chimeras (PROTACs) based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC50 of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity [1[.
    HPP-9
  • HY-W1120221

    E3 Ligase Ligand-Linker Conjugates Others
    Lenalidomide-C3-NH2 is an E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based CRBN ligand (HY-43722) and linker. Lenalidomide-C3-NH2 can be used for synthesis of PROTAC BET degrader-2 (HY-114228) .
    Lenalidomide-C3-NH2
  • HY-130814

    E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis Cancer
    Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .
    Thalidomide-NH-C4-NH2 TFA
  • HY-135250A

    E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis Cancer
    Thalidomide-4-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13 (HY-114421), a degrader of FKBP12 F36V and BET .
    Thalidomide-4-O-C6-NH2 TFA
  • HY-170390

    PROTACs Epigenetic Reader Domain Cancer
    AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM .
    AB3067
  • HY-172562

    PROTACs Epigenetic Reader Domain Cancer
    BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236) .
    BTR2004
  • HY-129937

    PROTACs Epigenetic Reader Domain Cancer
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
    (S)-GNE-987
  • HY-145177

    E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader . (From patent WO2017180417A1 compound s7).
    Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc
  • HY-179588

    PROTACs Epigenetic Reader Domain c-Myc Cancer
    PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .
    PROTAC BET Degrader-14
  • HY-181867

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia .
    PROTAC BET Degrader-16
  • HY-184335

    PROTACs Epigenetic Reader Domain c-Myc Apoptosis Cancer
    PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer .
    PROTAC BET Degrader-18

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

 

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

 

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: