Dorsomorphin-dihydrochloride-BML-275-dihydrochloride-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDorsomorphin dihydrochlorideCat. No.: HY-13418CAS No.: 1219168-18-9Synonyms: BML-275 dihydrochloride; Compound C dihydrochloride分式: CHClNO分量: 472.41作靶點(diǎn): AMPK; TGF- Receptor; Autophagy作通路: Epigenetics; PI3K/Akt/mTOR; TGF-beta/Sma

2、d; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 50 mg/mL (105.84 mM)DMSO : 5.2 mg/mL (11.01 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1168 mL 10.5840 mL 21.1681 mL5 mM 0.4234 mL 2

3、.1168 mL 4.2336 mL10 mM 0.2117 mL 1.0584 mL 2.1168 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride)種有效，選擇性和 ATP 競爭性的 AMPK 抑制劑，Ki 為109 nM 1。Dorsomorphin dihydrochloride 通過靶向抑制 I 型受體 ALK2，ALK3 和 ALK6

4、 來抑制 BMP 途徑 2。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target AMPK ALK2 ALK3 ALK6109 nM (Ki)Autophagy體外研究 Dorsomorphin (compound C) (0-10 M, 18 h) suppresses 2DG-induced GRP78 promoter activity in humanfibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunic

5、amycin-induced GRP78promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced byglucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation andreduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells 2.West

6、ern Blot Analysis 2Cell Line: Human fibrosarcoma HT1080 cells.Concentration: 0-10 M.Incubation Time: 18 hoursResult: Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner andalso suppressed GRP78 promoter activity induced by glucose withdrawal.體內(nèi)研究Dorsomorphin (compound C: 10 mg/

7、kg, intravenously once) treatment leads to a 60% increase in total serumiron concentrations, reduces basal levels of hepcidin expression and increasing serum iron concentrations inadult mice 3.Dorsomorphin (compound C: 0.2 mg/kg, i.v., 30 min before LPS injection) reduces ICAM-1 and VCAM-1expression

8、 in LPS-injected rat aorta 4.Dorsomorphin (compound C; 25 mg/kg; i.p. injection, in male BALB/c mice) treatment beforelipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPSchallenge only 5.Animal Model: Wild-type (WT) C57BL/6 adult mice that are fe

9、d a standard iron-replete diet express highlevels of hepcidin 3.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 ironconcentrations in adult mice.Animal

10、Model: Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g) 4.Dosage: 0.2 mg/kg.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration: 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

11、weeks of age weighing 20-22 g 5Dosage: 25 mg/kgAdministration: Injection i.p.; 60 min before LPS challengeResult: Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality incontrast to animals treated with LPS challenge only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Mol Cell. 2017 Oct 19;68(2):336-349

12、.e6. Redox Biol. 2018 Oct;19:339-353. Redox Biol. 2018 Jul;17:180-191. Mol Oncol. 2017 Aug;11(8):1035-1049. Cell Death Dis. 2019 Jul 8;10(7):525.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of metformin action.

13、 J Clin Invest. 2001 Oct;108(8):1167-74.2. Saito S, et al. Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent ofAMPK and BMP signaling. PLoS One. 2012;7(9):e45845.3. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis a

14、nd iron metabolism. Nat Chem Biol. 2008 Jan;4(1):33-41.4. Kim YM, et al. Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activatedendothelial cells in vitro and in vivo. Atherosclerosis. 2011 Nov;219(1):57-64.5. Guo Y, et al. AMPK inhibition blocks ROS-NFB signaling and attenuates endotoxemia-induced liver injury. PLoS One. 2014 Jan24