Dorsomorphin (Compound C) 是一种选择性，ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下，Ki 为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体 ALK2，ALK3 和 ALK6。Dorsomorphin 诱导自噬 (autophagy) 作用。
| CAS No. | 866405-64-3 |
| 生物活性 | Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy. |
| 分子式 | C24H25N5O |
| 分子量 | 399.49 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | 4°C, protect from light |
| 溶解性数据 | 1M HCl 中的溶解度 : 50 mg/mL (125.16 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈1)) DMSO 中的溶解度 :25 mg/mL (62.58 mM; ultrasonic and adjust pH to 3 with 1 M HCL; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO) H2O 中的溶解度 : < 0.1 mg/mL (insoluble) |
| 体内研究 | Dorsomorphin (compound C: 10 mg/kg, intravenously once) treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increasing serum iron concentrations in adult mice. Dorsomorphin (compound C: 0.2 mg/kg, I.V., 30 min before LPS injection) reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta. Dorsomorphin (compound C; 25 mg/kg; i.p. injection; in male BALB/c mice) treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only. |
| 体外研究 | Dorsomorphin (compound C) (0-10 μM, 18 h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells. |
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