BML-275 dihydrochloride; Compound C dihydrochloride; BML275 dihydrochloride; BML 275 dihydrochloride。

Dorsomorphin dihydrochloride：Dorsomorphin(Compound C; BML-275)双盐酸盐是AMPK选择性抑制剂，Ki为109 nM，还能抑制ALK2，ALK3和ALK6。

Dorsomorphin dihydrochloride：DMSO: ≤ 5.2 mg/mL (Need ultrasonic)

Dorsomorphin 2Hcl (Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK 6).

IC50 value: 109 nM (Ki for AMPK)
Target: AMPK
in vitro: Compound C treatment of MCF7 cells led to Bax redistribution from the cytoplasm to mitochondria and cell death.ceramide synthase 5 (LASS/CerS 5) is involved in Compound C-induced ceramide upregulation. Downregulation of LASS/CerS 5 was found to attenuate Compound C-mediated ceramide production, Bax redistribution, and cell death [1]. compound C prevented UPR marker glucose-regulated protein 78 (GRP78) accumulation and exerted enhanced cytotoxicity during glucose deprivation. compound C had a unique mode of action to suppress the transcriptional activation of UPR-targeted genes, as compared with the classic UPR inhibitors versipelostatin and biguanides. Surprisingly, the UPR-inhibiting activity of compound C was not associated with either AMPK or BMP signaling inhibition [2]. Compound C-mediated inhibition of AMPK and raptor in U251 cells was associated with paradoxical decrease in phosphorylation of AMPK/raptor-repressed mTOR, a major negative regulator of autophagy, and its downstream target p70S6K [3].
in vivo: