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

Epigenetic Reader Domain Degrader

Epigenetic Reader Domain Isoform Comparison

Epigenetic Reader Domain Degraders (142):

Cat. No. Product Name Effect Purity
  • HY-112588
    dBET6
    		Degrader 99.92%
    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
  • 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-161779
    PLX-3618
    		Degrader 99.86%
    PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models.
  • HY-117690
    dBRD9
    		Degrader 99.75%
    dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
  • HY-169093
    MS41
    		Degrader 98.97%
    MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078).
  • HY-141438
    SIM1
    		Degrader 99.47%
    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.
  • 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-156744
    DBr-1
    		Degrader 98.87%
    DBr-1 is a potent BRD9 PROTAC degrader (KD: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352).
  • 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-148739
    dBRD 9-A
    		Degrader 99.50%
    dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma.
  • 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-158764
    PROTAC BET Degrader-12
    		Degrader 98.10%
    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
  • HY-149878
    BD-9136
    		Degrader 98.81%
    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.
  • 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-115881
    SR-1114
    		Degrader 99.04%
    SR-1114 is a PROTAC degrader targeting ENL. SR-1114 degrades ENL in a CRBN-dependent manner and selectively downregulates ENL target genes. SR-1114 can promote the differentiation of acute myeloid leukemia cells. SR-1114 can be used in tumor research. (Pink: ENL ligand (HY-145409); Black: Linker; Blue: E3 Ligand (HY-14658)).
  • HY-112375
    AT6
    		Degrader 99.93%
    AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by an E3 ligand for von Hippel-Lindau and a ligand for BRD4 with highly selectivity to bromodomain (Brd4).
  • HY-172615
    AMPTX-1
    		Degrader 98.00%
    AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies.