产品描述
| 敏感性 | 对光及空气敏感 |
| 溶解性 | Soluble in DMSO (4 mg/ml warm), 100 mM HCl, and MeOH. |
| 存贮条件 | 储存温度2-8℃ |
| 应用 | A potent inhibitor of AMPK and fatty acid biosynthesis. |
| 产品介绍 | BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and Fatty Acid Synthase inhibitor. Phosphorylation of AMPK occurs in vivo when energy sources are low and in-turn suppresses expression of SREBP-1. SREBP-1 is a key lipogenic transcription factor, and its suppression allows glucose production by hepatocytes. In mouse studies it has been reported that BML-275 rapidly reduces the level of the phosphorylated AMPK α subunit in the hypothalamus, in an ATP-competitive manner, therefore altering energy perception and affecting the physiological energy sensor of the body. Over-activation of AMPK has also been found to be deleterious in ischemic stroke conditions and inhibition of AMPK by BML-275 may provide a small level of neuroprotection. Additional research on zebrafish has shown that BML-275 also inhibits bone morphogenetic protein signals required for iron metabolism and embryogenesis. BML-275 is an inhibitor of ACTR-I, BMPR-IA and BMPR-IB. |
| 生化机理 | Dorsomorphin is a selective inhibitor of Bone morphogenetic protein (BMP) signaling. It has been found to inhibit BMP signals required for embryogenesis and promoted significant neural differentiation from human pluripotent stem cell (hPSC) lines. Dorsomorphin also acts as a potent, selective, reversible, and ATP-competitive inhibitor of AMPK (AMP-activated protein kinase); Ki = 109 nM in the presence of 5 μM ATP and the absence of AMP). |
| 别名 | 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-a]嘧啶;AMPK 抑制剂;BML-275;6-[4-(2-Piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine; AMPK Inhibitor;Compound C;BML-275 |
