Dorsomorphin

SKU: orb1223809

Description

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.\n(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.

Key Properties

• CAS Number: 866405-64-3
• MW: 399.5
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₅N₅O
• SMILES: C(CN1CCCCC1)OC1=CC=C(C=C1)C1=CN2N=CC(=C2N=C1)C1=CC=NC=C1
• Target: AMPK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BML-275 | Compound C | BML275 | BML 275

Quick Database Links

Gene Symbol

AMPK