Dorsomorphin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dorsomorphin（BML-275，化合物 C）是一种有效的、选择性的、可逆的 AMPK 抑制剂，Ki 为 109 nM。

Dorsomorphin (BML-275, Compound C) is a potent, selective and reversible AMPK inhibitor with Ki of 109 nM, shows no no significant activity on ZAPK, SYK, PKCθ, PKA and JAK3; inhibits AMPK activation induced by AICAR and Metformin, also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6); promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro, induces autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.(In Vitro):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. (In Vivo):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.

Western Blot Analysis Cell Line:Human fibrosarcoma HT1080 cells Concentration:0-10 μM.Incubation Time:18 hours.Result:Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner and also suppressed GRP78 promoter activity induced by glucose withdrawal.

Animal Model:Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.Dosage:10 mg/kg.Administration:Intravenously once.Result:Led to a 60% increase in total serum iron concentrations.Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice. Animal Model:Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g).Dosage:0.2 mg/kg.Administration:I.V., 30 min before LPS injection.Result:Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.Animal Model:Male BALB/c mice at 6-7 weeks of age weighing 20-22 g Dosage:25 mg/kg Administration:Injection i.p.; 60 min before LPS challenge Result:Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only.

BML-275 | Compound C | BML275 | BML 275

Membrane Transporter/Ion Channel

AMPK

AMPK

Cancer

——

866405-64-3

399.5

C24H25N5O

>98% (HPLC)

10 mM in DMSO

C(CN1CCCCC1)OC1=CC=C(C=C1)C1=CN2N=CC(=C2N=C1)C1=CC=NC=C1

Pyrazolo[1,5-a]pyrimidine, 6-[4-[2-(1-piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-

(-20℃)

With Ice Pack

≥ 2 years