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

BRD4

 

BRD4 Related Products (130):

Cat. No. Product Name Effect Purity
  • HY-100972
    ARV-771
    		Inhibitor 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-101838
    dBET1
    		Inhibitor 99.24%
    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.
  • HY-112090
    ABBV-744
    		Inhibitor 99.97%
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-12863
    Pelabresib
    		Inhibitor 99.95%
    Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
  • HY-136570
    GSK778
    		Inhibitor 98.93%
    GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
  • HY-172130
    PI3Kδ/BET-IN-1
    		Inhibitor
    PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC50 = 112 nM) and BRD4-BD1 (IC50 = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells.
  • HY-168634
    SJ46421
    		Inhibitor
    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)).
  • HY-170380
    XY221
    		Inhibitor
    XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
  • HY-122826
    ZXH-3-26
    		Inhibitor 98.90%
    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
  • HY-136571
    GSK046
    		Inhibitor 99.65%
    GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
  • HY-14443
    XMD8-92
    		Inhibitor 99.67%
    XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.
  • HY-123941
    FKBP12 PROTAC dTAG-7
    		Inhibitor 99.07%
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-100482
    CPI-637
    		Inhibitor 99.94%
    CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
  • HY-114305
    A1874
    		Inhibitor 99.70%
    A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
  • HY-107443
    I-BET762 carboxylic acid
    		Inhibitor 99.55%
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
  • HY-19999A
    PF-CBP1 hydrochloride
    		Inhibitor 99.99%
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with?IC50?of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β,?IL-6?and?IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates?RGS4?expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
  • HY-129937A
    GNE-987
    		Inhibitor 99.91%
    GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
  • HY-120028
    GNE-207
    		Inhibitor
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-123844
    dBET57
    		Inhibitor 99.94%
    dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1.
  • HY-101519
    BETd-260
    		Inhibitor 99.59%
    BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.