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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
16 Results for "
BRD4-BD1/2-IN-1
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "BRD4-BD1/2-IN-1" in MCE Product Catalog:
Cat. No.: HY-142674
CAS No.: 1781219-19-9
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BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) .
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GSK778 (iBET-BD1), a chemical probe, 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 .
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2 Cited Publications
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MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .
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2 Cited Publications
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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).
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1 Cited Publications
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GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC50 = 0.059 μM), with a binding constant pKd = 8.1 and a pKi = 8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1. GSK8814 can be researched for cancer associated with ATAD2 bromodomain .
Cat. No.: HY-19760
CAS No.: 1422554-34-4
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I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
MMH1 is a novel BRD4 molecular glue degrader. MMH1 functions by recruiting the CUL4 DCAF16 ligase to the second bromodomain of BRD4 (BRD4 BD2). MMH1 binds to the JQ1-binding site of BRD4 BD2, acts as a template to covalently modify Cys58 of DCAF16, stabilizes the BRD4-DCAF16 ternary complex, and thereby promotes BRD4 degradation via the CRL4DCAF16 ubiquitin ligase pathway. Using BRD4 BD2 as a structural template, MMH1 covalently modifies Cys87 of GAK and induces the GAK-BRD4 BD2 interaction. Through its covalent mechanism, MMH1 exhibits sustained BRD4 degradation activity, and shows selective degradation activity for BRD4 BD2 over BRD4 BD1 .
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ZEN-2759 is a potent BET (Bromodomain and Extra-Terminal Domain) inhibitor, with IC50 values of 0.23, 0.08 and 0.28 μM for BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2), respectively .
Cat. No.: HY-136570A
CAS No.: 2863657-79-6
Synonyms: iBET-BD1 hydrochloride
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GSK778 (iBET-BD1) hydrochloride 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 .
Cat. No.: HY-178510
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JQ1-S (GlcNAc) Cq is a sugar-modified BRD4 PROTAC degrader with a DC50 of 2.1 μM. JQ1-S (GlcNAc) Cq inhibits the formation of the ternary complex between CRBN and BRD4 (BD1/BD2). JQ1-S (GlcNAc) Cq serves as a substrate for O-GlcNAcase, which cleaves its O-GlcNAc domain to restore binding ability with CRBN, thereby forming a BRD4-containing ternary complex and triggering ubiquitination and proteasomal degradation of BRD4. JQ1-S (GlcNAc) Cq is applicable for cancer research .
Cat. No.: HY-176535
CAS No.: 2648377-08-4
Synonyms: BBC0115
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KB-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.
Cat. No.: HY-173062
CAS No.: 2994635-04-8
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BRD4 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 .
Cat. No.: HY-149098
CAS No.: 2924546-70-1
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SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively .
Cat. No.: HY-19760B
CAS No.: 2885162-99-0
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I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
Cat. No.: HY-168628
CAS No.: 3054869-29-0
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BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .
Cat. No.: HY-186267
CAS No.: 3037514-35-2
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BD-7148 is a potent, highly selective BRD4 PROTAC degrader with a DC50 of 0.9 nM. BD-7148 binds to recombinant human BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1 and BRD4-BD2 domain proteins, with Kd values ranging from 26 nM to 240 nM, and shows no binding preference for BRD4 domains over BRD2 or BRD3 domains. BD-7148 inhibits the growth of leukemia and breast cancer cells. BD-7148 can be used in the research of leukemia and breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
