· 别名 : 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。
· CAS : 1219168-18-9
· 分子式 : C24H27Cl2N5O
· 分子量 : 472.41
· 单位 : 支
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:
浓度 | |
规格 | 5mg |
保存 |
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