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Pathways Recommended: PROTAC
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PROTAC BRD3 degrader

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-145264
    OARV-771

    		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-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-158764
    PROTAC BET Degrader-12

    		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))
    PROTAC BET Degrader-12
  • HY-149948
    PROTAC BRD3/BRD4-L degrader-2

    		Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
    PROTAC BRD3/BRD4-L degrader-2
  • HY-168635
    SJ46420

    		PROTACs Epigenetic Reader Domain Cancer
    SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)) .
    SJ46420
  • HY-168634
    SJ46421

    		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)) .
    SJ46421
  • HY-153414
    GXF-111

    		Epigenetic Reader Domain PROTACs Cancer
    GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer .
    GXF-111
  • HY-159973
    Me-SJ46411

    		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-159974
    Me-SJ46411-PEG1-Piperazine-Boc

    		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-130612
    PROTAC BRD2/BRD4 degrader-1

    		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. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
    PROTAC BRD2/BRD4 degrader-1
  • HY-162875
    PROTAC BRD4 Degrader-27

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875) [1] .
    PROTAC BRD4 Degrader-27
  • 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 .
    KB02-JQ1
  • HY-149878
    BD-9136

    		PROTACs Epigenetic Reader Domain Cancer
    BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity .(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))
    BD-9136
  • HY-170900
    SJ44236

    		PROTACs Epigenetic Reader Domain Cancer
    SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))
    SJ44236
  • HY-170390
    AB3067

    		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 . (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
    AB3067

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