2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BRD4 Isoform
  6. BRD4 Degrader

BRD4 Degrader

BRD4 Degraders (55):

Cat. No. Product Name Effect Purity
  • HY-100972
    ARV-771
    		Degrader 99.87%
    ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
  • HY-181553A
    PROTAC BRD4 Degrader-45
    		Degrader
    PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells.
  • HY-181553
    PROTAC BRD4 Degrader-44
    		Degrader
    PROTAC BRD4 Degrader-44 (compound 2a) is a PROTAC degrader targeting BRD4 with passive membrane permeability. PROTAC BRD4 Degrader-44 maintains stability within 6 hours in medium supplemented with 10% FBS. PROTAC BRD4 Degrader-44 shows a trend of increasing intracellular accumulation within 6 hours, indicating reduced efflux.
  • HY-153385
    TMX1
    		Degrader 99.57%
    TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.
  • HY-153459
    IBG1
    		Degrader 99.88%
    IBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)).
  • HY-156828
    MMH2
    		Degrader 98.95%
    MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2).
  • HY-163638
    BRD4 degrader-1
    		Degrader 99.85%
    BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research.
  • HY-174995
    JQ-1-Azidopropylamine
    		Degrader 99.5700%
    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).
  • HY-136857
    BRD4 degrader-3
    		Degrader 99.43%
    BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-156827
    MMH1
    		Degrader 99.83%
    MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2).
  • HY-132991
    ML 2-14
    		Degrader 99.43%
    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).
  • HY-138632
    PROTAC BRD4 Degrader linker conjugate
    		Degrader 98.98%
    PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)).\n
  • HY-132941
    CFT-2718
    		Degrader 99.87%
    CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer.
  • HY-178510
    JQ1-S(GlcNAc)Cq
    		Degrader
    JQ1-S(GlcNAc)Cq is a sugar-coated BRD4 PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-178514); Black: linker (HY-W105727); BRD4 ligand-Linker: (HY-178519))
  • HY-175224
    PROTAC BRD4 Degrader-36
    		Degrader
    PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-36 has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI50: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)).
  • HY-175610
    PROTAC FLT3/JAK2/BRD4 Degrader-1
    		Degrader
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)).
  • HY-161650
    PROTAC BRD4 Degrader-26
    		Degrader
    PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% BRD4 at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))
  • HY-143328
    PROTAC BRD4 Degrader-17
    		Degrader
    PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
  • HY-179589
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen
    		Degrader
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker, which recruits E3 ligases. JQ-1 (carboxylic acid)-amine-PEG8-cyanogen can be used for the synthesis of PROTAC BET Degrader-14 (HY-179588 ).
  • HY-173327
    BRD4 degrader-6
    		Degrader
    BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.