ML-180 (SR1848) 是一种有效的孤儿核受体肝受体同源物 1 (LRH-1; NR5A2) 反向激动剂,IC50 为 3.7 μM。 ML-180 对 steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM) 无活性。 ML-180 具有治疗 LRH-1 依赖性癌症的潜力。
Cas No. | 863588-32-3 |
别名 | SR1848 |
Canonical SMILES | ClC1=CC(N2CCN(C3=CC(N(C4CCCCC4)C(N3)=O)=O)CC2)=CC=C1 |
分子式 | C20H25ClN4O2 |
分子量 | 388.9 |
溶解度 | DMSO: 10 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 µM) with maximum efficacy of 64% repression. It is inactive at the related steroidogenic factor-1 transcriptional activator. Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.05 µM). |