Information GSK1324726A (I-BET726) GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. Targets BRD4 (Cell-free assay); BRD3 (Cell-free assay); BRD2 (Cell-free assay) 22 nM; 31 nM; 41 nM In vitro In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN. In vivo In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals. Cell Research(from reference) Cell lines：LA-N-1, Kelly, LA1-55n, BE(2)-M17, BE(2)-C, KanTS, IMR32, LA-N-2, SK-N-SH, SK-N-BE(2), CHP-134, SK-N-AS, SH-SY5Y, SK-N-FI, CHP-212, LA1-5s, SK-N-DZ cells Concentrations：~10 μM Incubation Time：6 days
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GSK1324726A (I-BET726)
Dangerous GoodsCAS number：1300031-52-0 molecular formula：C25H23ClN2O3
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 4-((2S,4R)-1-acetyl-4-(4-chlorophenylamino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid | ||
| CAS number | 1300031-52-0 | molecular formula | C25H23ClN2O3 |
| molecular weight | 434.91 g/mol | Exact mass | 10mM in DMSO |
| PSA | 69.600 Ų | logp | 4.648 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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MSDS
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