BRD4 Inhibitor
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BRD4-BD1-IN-2
0 ImagesCat. No.: HY-143300CAS No.: 2761321-26-8
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BRD4 ligand 8
0 ImagesCat. No.: HY-174812BRD4 ligand 8 (Compound J558) is a BRD4 inhibitor. BRD4 ligand 8 can be used for synthesis of PROTAC BRD4 Degrader-33 (HY-174811).
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BRD4-IN-3
0 ImagesCat. No.: HY-104072CAS No.: 1380087-86-4BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM.
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BRD4 ligand 2
0 ImagesCat. No.: HY-150941CAS No.: 2133902-07-3BRD4 ligand 2 is a BRD4 BD1 inhibitor with an IC50 of 46.4 nM. BRD4 ligand 2 inhibits the proliferation of lymphoma cells. BRD4 ligand 2 also serves as a target protein ligand for PROTACs, and is used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131). BRD4 ligand 2 is applicable to research related to lymphoma.
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BRD4 D1-IN-3
0 ImagesCat. No.: HY-180831BRD4 D1-IN-3 (compound 39) is a potent, selective, and cell-active BRD4-D1 inhibitor (IC50 = 39 nM, Ki = 2.4 nM) with >1700-fold selectivity over BRD2-D1. BRD4 D1-IN-3 reduces the expression of pro-inflammatory chemokines CXCL1 and CCL2 in an LPS (HY-D1056)-mediated cellular model of liver inflammation. BRD4 D1-IN-3 can be used for liver inflammation research.
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Bromodomain inhibitor-10
0 ImagesCat. No.: HY-147375CAS No.: 1870849-58-3Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
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CZL-077
0 ImagesCat. No.: HY-180804CAS No.: 3032444-06-4CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.
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BRD4-IN-12
0 ImagesCat. No.: HY-181505CAS No.: 3112325-99-9BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).
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CDK8/BRD4-IN-1
0 ImagesCat. No.: HY-184727CDK8/BRD4-IN-1 is a dual CDK8/BRD4 inhibitor, with an IC50 of 5.44 μM against CDK8 and an IC50 of 4.03 μM against BRD4. CDK8/BRD4-IN-1 exhibits anticancer activity against colorectal cancer. CDK8/BRD4-IN-1 can be used for the research of colorectal cancer.
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XY-06-005
0 ImagesCat. No.: HY-184949CAS No.: 1642783-78-5XY-06-005 is a modified selective inhibitor of BET bromodomain that binds to BRD4 BD1 L94V, BRD4 BD2 L387V and BRD2 BD2 L383V. XY-06-005 serves as a Ligand for Target Protein for PROTAC for studies related to PROTAC synthesis, such as acting as the target protein ligand structure of XY-06-007 (HY-145226).
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Bromodomain inhibitor-9
0 ImagesCat. No.: HY-147374CAS No.: 1870849-34-5Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases.
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CBP/p300-IN-22
0 ImagesCat. No.: HY-176251CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
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BRD4 Inhibitor-25
0 ImagesCat. No.: HY-151972CAS No.: 2976403-41-3BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
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(S)-BI 2536
0 ImagesCat. No.: HY-50698ACAS No.: 1241725-90-5(S)-BI 2536 is the enantiomer of BI 2536 (HY-50698). (S)-BI 2536 acts as an inhibitor of the BRD4 bromodomain and PLK1 kinase, with a Ki value of 54 nM against BRD4 and a Ki value of 0.42 nM against PLK1 kinase. (S)-BI 2536 exhibits anticancer activity against acute myeloid leukemia. (S)-BI 2536 can be used for the research of acute myeloid leukemia.
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WWL0245
0 ImagesCat. No.: HY-153519CAS No.: 2869057-11-2WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4.
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BRD4/AKT-IN-1
0 ImagesCat. No.: HY-183273CAS No.: 3087270-50-3BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
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GSK778 hydrochloride
0 ImagesCat. No.: HY-136570ACAS No.: 2863657-79-6Synonyms: iBET-BD1 hydrochloride
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TW9
0 ImagesCat. No.: HY-155222CAS No.: 2614417-90-0TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026).
