| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I408610-1ml |
1ml |
现货  |
|
| 英文别名 | 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | I-BET151 (GSK1210151A) |
| 生化机理 | I-BET151（GSK1210151A）是一种新型选择性 BET 抑制剂，在无细胞实验中对 BRD2、BRD3 和 BRD4 的 IC50 分别为 0.5 μM、0.25 μM 和 0.79 μM。 |
| 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 | 含 2 个溴odomain 的抑制剂；含 3 个溴odomain 的抑制剂；含 4 个溴odomain 的抑制剂 |
| 产品介绍 |
I-BET151 (GSK1210151A) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂，抑制 BRD4，BRD2 和 BRD3 的 pIC50 分别为 6.1，6.3 和 6.6。 产品应用： GSK1210151A 或 I-BET151 已用于研究其在治疗 MLL（混合谱系白血病）-融合性白血病中对 BET（溴结构域和额外末端）募集染色质的抑制作用。 Information I-BET151 (GSK1210151A) I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2 , BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively. I-BET151 exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with KD of 0.02-0.1 μM, and significantly inhibits lipopolysaccharide-stimulated IL-6 cytokine production in human peripheral blood mononuclear cells (PBMC) and whole blood (WB) as well as rat WB with IC50 of 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151 (0.5 or 5 μM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins in HL60 nuclear extract to acetylated histone peptides. I-BET151 has potent efficacy against cell lines harboring different MLL-fusions such as MV4;11, RS4;11, MOLM13, and NOMO1 cells with IC50 of 15-192 nM. Consistently, I-BET151 completely ablates the colony-forming potential of MLL-fusion-driven leukaemias (MOLM13) but not leukaemias driven by tyrosine kinase activation (K562). I-BET151 also displays potent efficacy in both liquid culture and clonogenic assays using primary murine progenitors transformed with either MLL-ENL or MLL-AF9. I-BET151 treatment significantly induces apoptosis and prominent G0/G1 arrest in MLL-fusion cell lines driven by distinct MLL fusions (MOLM13 and MV4;11 containing MLL-AF9 and MLL-AF4, respectively) but not the K562 cells, probably due to the inhibition of transcription of BCL2, C-MYC and CDK6 by blocking the recruitment of BRD3/4, PAFc and SEC components into transcriptional start site (TSS). In vivo Administration of I-BET151 at 30 mg/kg/day significantly inhibits tumor growth of murine MLL-AF9 and human MLL-AF4 leukaemia in mice, and provides marked survival benefit. cell lines：Syk-dependent BaF3 cell Concentrations：Dissolved in DMSO, final concentrations ~100 μM Incubation Time：24, or 72 hours Powder Purity:≥99% |
| ALogP | 2.601 |
|---|---|
| hba_count | 6 |
| HBD Count | 1 |
| Rotatable Bond | 4 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=C(C=C2N=CC3=C(N(C(C)C4=CC=CC=N4)C(=O)N3)C2=C1)C5=C(C)ON=C5C |
| 分子量 | 415.44 |
| Reaxy-Rn | 21460437 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21460437&ln= |
| DMSO(mg / mL) Max Solubility | 83 |
|---|---|
| DMSO(mM) Max Solubility | 199.79 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 21460437 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21460437&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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