Dorsomorphin 2HCl

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Chemical Structure| 1219168-18-9 同义名 : Compound C dihydrochloride; BML-275 dihydrochloride; CpdC; Compound C; BML-275; Dorsomorphin (hydrochloride); Dorsomorphin dihydrochloride
CAS号 : 1219168-18-9
货号 : A213616
分子式 : C24H27Cl2N5O
纯度 : 99%+
分子量 : 472.41
MDL号 : MFCD11112197
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(8.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(211.68 mM)，配合低频超声助溶
生物活性
描述 Dorsomorphin dihydrochloride is the dihydrochloride form of dorsomorphin. Dorsomorphin, known as compound C, is a reversible selective ATP-competitive inhibitor of AMPK with Ki of 109 nM. Dorsomorphin can also inhibit the bone morphogenic protein (BMP) signaling and do not effect the expression of several structurally related kinases including ZAPK, SYK, PKCq, PKA, and JAK3[1]. In addition, dorsomorphin could stimulate the oxidation of long chain fatty acids independently in adipocytes by increasing carnitine palmitoyltransferase-1 (CPT1) activity[2] and remarkly reduce the adipogenic Differentiation of 3T3-L1 cells at 10 μM[3]. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway[4]. In vivo, dorsomorphin induces dorsalization in zebrafish embryos and the differentiation of osteoblast[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
mouse C2C12 cells 4 μM Function assay Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry 18026094
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL
参考文献

[1]Zhou G, Myers R, Li Y, et al. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest. 2001;108(8):1167-1174.

[2] Gaidhu MP, Fediuc S, Ceddia RB. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside-induced AMP-activated protein kinase phosphorylation inhibits basal and insulin-stimulated glucose uptake, lipid synthesis, and fatty acid oxidation in isolated rat adipocytes. J Biol Chem. 2006;281(36):25956-25964.

[3] Gao Y, Zhou Y, Xu A, Wu D. Effects of an AMP-activated protein kinase inhibitor, compound C, on adipogenic differentiation of 3T3-L1 cells. Biol Pharm Bull. 2008;31(9):1716-1722.

[4] Vucicevic L, Misirkic M, Janjetovic K, et al. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy. 2011;7(1):40-50.

[5] Yu PB, Hong CC, Sachidanandan C, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008;4(1):33-41.