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JQ1

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40

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13030
    (+)-JQ-1
    Maximum Cited Publications
    230 Publications Verification

    JQ1

    Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) [1]. (+)-JQ-1 also activates autophagy .
    (+)-JQ-1
  • HY-78695
    JQ-1 (carboxylic acid)
    5+ Cited Publications

    Epigenetic Reader Domain PD-1/PD-L1 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-148864

    Epigenetic Reader Domain Cancer
    JQ1-TCO is the double bond E configuration of JQ1-TCO (HY-148864A). JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo [1] .
    JQ1-TCO
  • HY-112789
    (+)-JQ1 PA
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (+)-JQ1 PA
  • HY-145667
    Biotinylated-JQ1
    1 Publications Verification

    Biotin-JQ1

    Epigenetic Reader Domain Cancer
    Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM [1].
    Biotinylated-JQ1
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer
    5+ Cited Publications

    Epigenetic Reader Domain Cancer
    (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
    (R)-(-)-JQ1 Enantiomer
  • HY-169082

    E3 Ligase Ligand-Linker Conjugates Cancer
    JQ-1 (carboxylic acid)-NH-C2-NH-COOH is a conjugate of E3 ligase ligand and linker (E3 Ligase Ligand-Linker Conjugates), which is composed of JQ-1 carboxylic acid (HY-78695) and the corresponding linker: (2-Aminoethyl)carbamic acid (HY-W398806). JQ-1 (carboxylic acid)-NH-C2-NH-COOH can be used as a Cereblon ligand to recruit CRBN protein and as a key intermediate for the synthesis of complete PROTACs molecules [1].
    JQ-1 (carboxylic acid)-NH-C2-NH-COOH
  • HY-169150

    E3 Ligase Ligand-Linker Conjugates Cancer
    JQ-1 carboxylic acid-PEG3-C2-NH2 is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACT [1].
    JQ-1 carboxylic acid-PEG3-C2-NH2
  • HY-137075

    Epigenetic Reader Domain Cancer
    (±)-JQ1 is the racemate of (+)-JQ-1 (HY-13030) [1].
    (±)-JQ1
  • HY-161125

    Others Others
    (+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy [1].
    (+)-JQ1-OH
  • HY-148864A

    Epigenetic Reader Domain Cancer
    JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo [1] .
    (Z)-JQ1-TCO
  • HY-129917
    KB02-JQ1
    4 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 [1].
    KB02-JQ1
  • HY-131633A

    Epigenetic Reader Domain Cancer
    (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains [1].
    (+)-JQ-1-aldehyde
  • HY-147046

    Epigenetic Reader Domain Cancer
    ET-JQ1-OH is an allele-specific BET inhibitor [1].
    ET-JQ1-OH
  • HY-156214

    AP1867-PEG2-JQ1; AP-PEG2-JQ1

    Others Others
    NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins [1].
    NICE-01
  • HY-130256

    PROTACs Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity [1].
    β-NF-JQ1
  • HY-153574

    pArg-JQ1

    PROTACs Epigenetic Reader Domain Infection
    BI01826025 (pArg-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. BI01826025 can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease [1].
    BI01826025
  • HY-153573

    dCym-JQ1

    PROTACs Epigenetic Reader Domain Infection
    SRG-II-19F (dCym-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. SRG-II-19F can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease [1].
    SRG-II-19F
  • HY-160528

    Molecular Glues Epigenetic Reader Domain Cancer
    IBG3 is a dual-JQ1-containing BET molecular glue degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively [1].
    IBG3
  • HY-111823

    VHL ligand 6

    Ligands for E3 Ligase Cancer
    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC [1].
    VH032 thiol
  • HY-100696

    Epigenetic Reader Domain Cancer
    PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1) [1].
    PNZ5
  • HY-161769

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770)) [1]
    HL435
  • HY-101838
    dBET1
    10+ Cited Publications

    PROTACs Epigenetic Reader Domain Cancer
    dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker [1].
    dBET1
  • HY-169081

    PROTACs Others
    QS-57 is a PROTAC targeting BRD4. QS-57 can be used as a 14-3-3 molecular glue. (Red: EN171 (HY-W1005067), black: (2-Aminoethyl) carbamic acid (HY-W398806), Blue: JQ-1 (carboxylic acid) (HY-78695)) [1].
    QS-57
  • HY-131385

    Ligands for E3 Ligase Cancer
    KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610) [1].
    KB02-COOH
  • HY-162835

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) [1].
    PROTAC SMARCA2/4-degrader-28
  • HY-111875

    SNIPERs Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively [1].
    SNIPER(BRD)-1
  • HY-159973

    Ligands for E3 Ligase Cancer
    Me-SJ46411 is an E3 ubiquitin ligase ligand, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411 combined with PROTAC linker Boc-Piperazine-OH (HY-20797) and target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635).
    Me-SJ46411
  • HY-W007545

    PROTAC Linker 35

    PROTAC Linkers Cancer
    NH2-PEG3 (PROTAC Linker 35) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. NH2-PEG3 (PROTAC Linker 35) can be used in the synthesis of the PROTAC (β-NF-JQ1) [1].
    NH2-PEG3
  • HY-130842

    β-NF-CH2-Br

    E3 Ligase Ligand-Linker Conjugates Cancer
    β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256) [1].
    β-Naphthoflavone-CH2-Br
  • HY-159974

    E3 Ligase Ligand-Linker Conjugates Cancer
    Me-SJ46411-PEG1-Piperazine-Boc is a conjugate of E3 ubiquitin ligase and PROTAC linker, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411-PEG1-Piperazine-Boc combined with target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635).
    Me-SJ46411-PEG1-Piperazine-Boc
  • 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. (Pink: ligand for target protein (+)-JQ-1 (HY-13030); Black: linker (HY-159077); Blue: ligand for E3 ligase (HY-159076)) [1]
    PROTAC BET Degrader-12
  • 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 [1]. 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 [1].
    TD-428
  • HY-19541A

    Epigenetic Reader Domain Cancer
    I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin [1].
    I-CBP112 hydrochloride
  • HY-168646

    Ligands for E3 Ligase Cancer
    SJ46411-Br is one of CRL2 KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs [1].
    SJ46411-Br
  • HY-168634

    PROTACs Epigenetic Reader Domain Cancer
    SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC50 of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)) [1].
    SJ46421
  • HY-130269

    β-NF-CH2-OH

    E3 Ligase Ligand-Linker Conjugates Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins [1].
    β-Naphthoflavone-CH2-OH
  • HY-111976

    Epigenetic Reader Domain Cancer
    MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1) [1].
    MT1
  • HY-157591

    Molecular Glues Epigenetic Reader Domain Cancer
    MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader [1].
    MMH1-NR
  • HY-157592

    Molecular Glues Epigenetic Reader Domain Cancer
    MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader [1].
    MMH2-NR

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