| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M408375-1ml |
1ml |
现货  |
|
| 别名 | 莫利布雷西布 (I-BET-762) |
|---|---|
| 英文别名 | GSK525762, GSK525762A | 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Molibresib (I-BET-762) |
| 生化机理 | Molibresib（I-BET-762，GSK525762，GSK525762A）是一种 BET 蛋白抑制剂，在无细胞试验中的 IC50 值约为 35 nM，可抑制巨噬细胞产生促炎蛋白并阻断急性炎症，对其他含溴结构域的蛋白具有高度选择性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 溴结构域和末端外基团（BET）抑制剂 |
| 产品介绍 |
Molibresib (I-BET-762, GSK525762, GSK525762A) 是一种BET蛋白抑制剂，无细胞试验中IC50约为35 nM，抑制巨噬细胞产生促炎性蛋白质，并抑制急性炎症，对其他溴区结合域包含的蛋白具有高度选择性。 Information Molibresib (I-BET-762) Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly se 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 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). cell lines： Concentrations：~500 nM Incubation Time：60–72 h Powder Purity:≥97% |
| ALogP | 3.288 |
|---|---|
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCNC(=O)CC1N=C(C2=CC=C(Cl)C=C2)C3=CC(=CC=C3[N]4C(=NN=C14)C)OC |
| 分子量 | 423.9 |
| Reaxy-Rn | 21441487 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21441487&ln= |
| DMSO(mg / mL) Max Solubility | 84 |
|---|---|
| DMSO(mM) Max Solubility | 198.16 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 21441487 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21441487&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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