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JQ1

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59

Inhibitors & Agonists

2

Click Chemistry

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

    JQ1

    Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1), a chemical probe, 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-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-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-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-169150A

    E3 Ligase Ligand-Linker Conjugates Cancer
    JQ-1 carboxylic acid-PEG3-C2-NH2 (hydrochloride) is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACT [1].
    JQ-1 carboxylic acid-PEG3-C2-NH2 hydrochloride
  • HY-172126

    Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain Cancer
    JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a ligand for BRD4, and a PROTACs linker that can be used in the synthesis of PROTAC BRD4 Degrader-29 (HY-172124) [1].
    JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222
  • HY-174995

    Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain Cancer
    JQ-1-Azidopropylamine is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-151862), which recruits E3 ligases. JQ-1-Azidopropylamine can be used for synthesis of PROTAC JY-21 (HY-174975) [1].
    JQ-1-Azidopropylamine
  • HY-137075

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

    Drug Metabolite 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-13030A
    (R)-(-)-JQ1 Enantiomer
    10+ 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-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-176391

    Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain Cancer
    Ad-JQ1 (Compound 16) is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-176390), which recruits E3 ligases. Ad-JQ1 can be used for synthesis of PROTAC β-NF-JQ1 (HY-130256) [1].
    Ad-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-176724

    Epigenetic Reader Domain Reactive Oxygen Species (ROS) HIF/HIF Prolyl-Hydroxylase Cancer
    ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 consists of three parts: BRD4 ligand (HY-78695); Linker (HY-W040165); Photosensitizer (HY-176725) [1].
    ZnPc-O3-JQ1
  • 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

    Epigenetic Reader Domain 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-176725

    Photosensitizer Reactive Oxygen Species (ROS) Cancer
    ZnPcPs is a photosensitizer that generates ROS. ZnPcPs can be used to synthesize the photo-activated BRD4 degrader pZnPc-O3-JQ1 (HY-176724) [1].
    ZnPcPs
  • 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-156774

    PROTACs Epigenetic Reader Domain Others
    CCW 28-3 is a PROTAC-based BRD4 degrader in a proteasome- and RNF4-dependent manner (Pink: JQ-1 (carboxylic acid) (HY-78695); Black: linker (HY-170384); Blue: RNF4 ligand CCW16 (HY-143346)) [1].
    CCW 28-3
  • 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
    15+ 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-170453

    Epigenetic Reader Domain Cancer
    iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models [1].
    iHAC
  • HY-169081

    PROTACs Molecular Glues 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-176390

    PROTAC Linkers Others
    Adamantan-C-amide-PEG2-C2-amine (Compound 8) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC β-NF-JQ1 (HY-130256) [1].
    Adamantan-C-amide-PEG2-C2-amine
  • 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-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). [1].
    Me-SJ46411
  • HY-169358

    PROTACs Epigenetic Reader Domain Cancer
    L134 is a potent PROTAC BRD4 degrader with a DC50 value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)) [1].
    L134
  • 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-170808

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)) [1].
    PROTAC BRD4 Degrader-28
  • HY-111875

    SNIPERs PROTACs Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC50 values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research [1]. (Blue: LCL161 (HY-15518); Black: linker (HY-W008005); Pink: (+)-JQ-1 (HY-13030))
    SNIPER(BRD)-1
  • HY-176726

    Reactive Oxygen Species (ROS) Cancer
    ZnPc-amide-PEG3-C2-NH2 is a photosensitizer-linker conjugate which consists of ZnPcPs (HY-176725) and a linker (HY-W040165). ZnPc-amide-PEG3-C2-NH2 can be used to synthesize the photo-activated BRD4 degrader pZnPc-O3-JQ1 (HY-176724) [1].
    ZnPc-amide-PEG3-C2-NH2
  • HY-175179

    Epigenetic Reader Domain E1/E2/E3 Enzyme Cancer
    LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells [1].
    LO-3-61
  • 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). [1].
    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-132991
    ML 2-14
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487) [1].
    ML 2-14
  • 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) [1] .
    BTR2004
  • 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 Molecular Glues 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

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