BRD2 Inhibitor
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GSK785
0 ImagesCat. No.: HY-181003CAS No.: 3125088-67-4
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BET-IN-30
0 ImagesCat. No.: HY-181735BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
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PROTAC BRD2/BRD4 degrader-1
0 ImagesCat. No.: HY-130612CAS No.: 2570470-42-5PROTAC 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. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
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KB-0118
0 ImagesCat. No.: HY-176535CAS No.: 2648377-08-4Synonyms: BBC0115KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
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SJ46421
0 ImagesCat. No.: HY-168634SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research.
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BET-IN-13
0 ImagesCat. No.: HY-152213CAS No.: 2506823-08-9BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.
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BRD4 Inhibitor-40
0 ImagesCat. No.: HY-173062CAS No.: 2994635-04-8BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models.
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BET BD2-IN-1
0 ImagesCat. No.: HY-155680CAS No.: 2677039-24-4
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WNY0824
0 ImagesCat. No.: HY-143471CAS No.: 2412707-81-2Synonyms: PLK1/BRD4-IN-1WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
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PARP1/BRD4-IN-3
0 ImagesCat. No.: HY-169170PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy.
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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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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 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.
