Dorsomorphin dihydrochloride

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.

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BML-275 dihydrochloride | Compound C dihydrochloride

Membrane Transporter/Ion Channel

AMPK

AMPK

Cancer

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1219168-18-9

472.4

C24H27Cl2N5O

>98% (HPLC)

H2O: ≥ 48 mg/mL; DMSO: 5.2 mg/mL (Need ultrasonic)

Cl.Cl.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)-, hydrochloride (1:2)

(-20℃)

With Ice Pack

≥ 2 years