Dorsomorphin (Compound C) 是一种选择性，ATP 竞争性的AMPK抑制剂 (在没有 AMP 的情况下，Ki为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体ALK2，ALK3和ALK6。Dorsomorphin 诱导自噬 (autophagy) 作用。
| 生物活性 | Dorsomorphin (Compound C) is a selective and ATP-competitiveAMPKinhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptorsALK2,ALK3, andALK6. Dorsomorphin inducesautophagy[1][2]. |
| IC50& Target[1][2] | AMPK 109 nM (Ki) | ACVR1 | BMPR1A | ALK6 | Autophagy |
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体外研究
(In Vitro) | Dorsomorphin (compound C) (0-10 μM, 18 h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells[2].
Western Blot Analysis[2] | Cell Line: | Human fibrosarcoma HT1080 cells | | Concentration: | 0-10 μM. | | Incubation Time: | 18 hours. | | Result: | Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner and also suppressed GRP78 promoter activity induced by glucose withdrawal. |
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体内研究
(In Vivo) | Dorsomorphin (compound C: 10 mg/kg, intravenously once) treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increasing serum iron concentrations in adult mice[3].
Dorsomorphin (compound C: 0.2 mg/kg, I.V., 30 min before LPS injection) reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta[4].
Dorsomorphin (compound C; 25 mg/kg; i.p. injection; in male BALB/c mice) treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only[5].
| Animal Model: | Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels 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 iron concentrations in adult mice. |
| Animal 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[5] | | Dosage: | 25 mg/kg | | Administration: | Injection i.p.; 60 min before LPS challenge | | Result: | Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: 1M HCl : 50 mg/mL(125.16 mM;ultrasonic and adjust pH to 1 with HCl) DMSO : 5 mg/mL(12.52 mM;ultrasonic and warming and heat to 80℃) Ethanol : 3.33 mg/mL(8.34 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.5032 mL | 12.5160 mL | 25.0319 mL | | 5 mM | 0.5006 mL | 2.5032 mL | 5.0064 mL | | 10 mM | 0.2503 mL | 1.2516 mL | 2.5032 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： Saline Solubility: 12.5 mg/mL (31.29 mM); Clear solution; Need ultrasonic and adjust pH to 5 with 0.1 M HCL
*以上所有助溶剂都可在本网站选购。 |
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