上海金畔生物科技有限公司提供Dorsomorphin dihydrochloride,索莱宝,ID2840-5mg CAS : 1219168-18-9,可以访问官网了解更多产品信息。 Dorsomorphin dihydrochloride,索莱宝,ID2840-5mg CAS : 1219168-18-9
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:
上海金畔生物科技有限公司提供Dorsomorphin dihydrochloride,索莱宝,ID2840-10mM *1mL in Water CAS : 1219168-18-9,可以访问官网了解更多产品信息。 Dorsomorphin dihydrochloride,索莱宝,ID2840-10mM *1mL in Water CAS : 1219168-18-9
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: