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| 品牌 | absin | CAS | 1260907-17-2 |
|---|---|---|---|
| 分子式 | C22H22ClN5O2 | 纯度 | ＞98% |
| 分子量 | 423.9 | 货号 | abs810335 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent small molecule inhibitors | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Molibresib 1260907-17-2
| 产品描述 | |
| 描述 | GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4). |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | GSK 525762A; I-BET 762 |
| 外观 | 类白色至黄色粉末 |
| 可溶性/溶解性 | DMSO : 78 mg/mL (184 mM) Ethanol : 39 mg/mL (92 mM) |
| 生物活性 | |
| 靶点 | BET proteins |
| In vitro(体外研究) | I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes. I-BET-762 treatment during the first 2 d of differentiation alters CD4+ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines. |
| In vivo(体内研究) | I-BET-762 confers protection against lipopolysaccharide-induced endotoxic shock and bacteria induced sepsisa. Single dose of I-BET applied at 1.5 h after LPS injection cures the mice. Twice-daily injections of I-BET for 2 days protects mice against death caused by sepsis. Limited treatment with I-BET-762 exclusively during early priming inhibited the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in a mouse model of experimental autoimmune encephalomyelitis (EAE). |
| 研究领域 | |
| 研究领域 | Epigenetics Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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