Dorsomorphin,1219168-18-9

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Dorsomorphin dihydrochloride

CAS No. : 1219168-18-9

MCE 国际站：Dorsomorphin dihydrochloride

产品活性：Dorsomorphin (Compound C) dihydrochloride 是一种有效，选择性和 ATP 竞争性的 AMPK 抑制剂，K_i 为 109 nM。Dorsomorphin dihydrochloride 通过靶向抑制 I 型受体 ALK2，ALK3 和 ALK6 来抑制 BMP 途径。Dorsomorphin dihydrochloride 还能够逆转 Urolithin A (HY-100599) 导致的自噬 (autophagy) 激活和抗炎作用。

研究领域：Epigenetics  |  PI3K/Akt/mTOR  |  TGF-beta/Smad  |  Autophagy

作用靶点：AMPK  |  TGF-β Receptor  |  Autophagy

In Vitro: Dorsomorphin (compound C; 0-10 μM; 18 h) dihydrochloride suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on Tunicamycin (HY-A0098)-induced GRP78 promoter activity. Dorsomorphin dihydrochloride also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin dihydrochloride has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells.

In Vivo: Dorsomorphin (compound C; 10 mg/kg, intravenously once) dihydrochloride treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice.
Dorsomorphin (0.2 mg/kg, i.v., 30 min before LPS injection) dihydrochloride reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.
Dorsomorphin (25 mg/kg; i.p. injection, in male BALB/c mice) dihydrochloride treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only.

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