Dorsomorphin-BML-275-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDorsomorphinCat. No.: HY-13418ACAS No.: 866405-64-3Synonyms: BML-275; Compound C分式: CHNO分量: 399.49作靶点: AMPK; TGF- Receptor; Autophagy作通路: Epigenetics; PI3K/Akt/mTOR; TGF-beta/Smad; Autophagy储存式: 4C, protect from light* In solven

2、t : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 Ethanol : 3.33 mg/mL (8.34 mM; Need ultrasonic)DMSO : 2 mg/mL (5.01 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5032 mL 12.5160 mL 25.0319 mL5 mM 0.5006 mL 2.5032 mL 5.0064 mL10 mM - - -请根据产品在不同溶剂中的溶解度，选择合适的溶

3、剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.2 mg/mL (0.50 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline

4、)Solubility: 0.2 mg/mL (0.50 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/4 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 0.2 mg/mL (0.50 mM); Clear solution4. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 0.33 mg/mL (0.83 mM); Clear solution5. 请依序添加每种溶剂： 10%

5、 EtOH 90% (20% SBE-CD in saline)Solubility: 0.33 mg/mL (0.83 mM); Clear solution6. 请依序添加每种溶剂： 10% EtOH 90% corn oilSolubility: 0.33 mg/mL (0.83 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Dorsomorphin (BML-275; Compound C)种有效的 ATP 竞争性的选择性 AMPK 抑制剂，Ki 为 109 nM1。Dorsomorphin 通过靶向抑制 I 型受体 ALK2，ALK3 和 ALK

6、6 来抑制 BMP 途径 2。IC50 & Target AMPK ALK2 ALK3 ALK6109 nM (Ki)Autophagy体外研究 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 tunicamycin-induced GRP78promoter activity. Dorsomorp

7、hin (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.Western Blot Analysis 2Cell Line: Human fibrosarcoma

8、 HT1080 cellsConcentration: 0-10 M.Incubation Time: 18 hours.Result: Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner andalso suppressed GRP78 promoter activity induced by glucose withdrawal.体内研究Dorsomorphin (compound C: 10 mg/kg, intravenously once) treatment leads to a 60%

9、 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 in LPS-injected rat aorta 4.Dorsomorphin (compo

10、und 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 5.2/4 Master of Small Molecules 您边的抑制剂师www.MedChemEAnimal Model: Wild-type (WT) C57BL/6 adult mice that are f

11、ed 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

12、 Model: Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g) 4.Dosage: 0.2 mg/kg.Administration: 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 weeks of age weighing 20-22 g 5Dosage: 25 mg/kgA

13、dministration: 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.户使本产品发表的科研献 Mol Cell. 2017 Oct 19;68(2):336-349.e6. Redox Biol. 2018 Oct;19:339-353. Redox Biol

14、. 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. J Clin Invest. 2001 Oct;108(8):1167-74.2. Saito

15、 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 and iron metabolism. Nat Chem Biol. 2008 Jan;4(1)

16、:33-41.3/4 Master of Small Molecules 您边的抑制剂师www.MedChemE4. 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 live