Dorsomorphin(Synonyms: Compound C; BML-275)

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Dorsomorphin (Synonyms: Compound C; BML-275) 纯度: 99.91%

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。

Dorsomorphin(Synonyms: Compound C; BML-275)

Dorsomorphin Chemical Structure

CAS No. : 866405-64-3

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生物活性

Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy[1][2].

IC50 & Target[1][2]

AMPK

109 nM (Ki)

ALK2

 

ALK3

 

ALK6

 

Autophagy

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

399.49

Formula

C24H25N5O
CAS 号

866405-64-3
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 60°C)

H2O : 3.33 mg/mL (8.34 mM; ultrasonic and adjust pH to 6 with HCl)

Ethanol : 3.33 mg/mL (8.34 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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: 20 mg/mL (50.06 mM); Clear solution; Need ultrasonic and adjust pH to 5 with HCl

  • 2.

    请依序添加每种溶剂： 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% EtOH    90% corn oil

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。

  • 5.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 2.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 6.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 2.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 7.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 2.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of action. J Clin Invest. 2001 Oct;108(8):1167-74.

    [2]. Kim YM, et al. Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activated endothelial cells in vitro and in vivo. Atherosclerosis. 2011 Nov;219(1):57-64.

    [3]. Saito S, et al. Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signaling. PLoS One. 2012;7(9):e45845.

    [4]. Guo Y, et al. AMPK inhibition blocks ROS-NFκB signaling and attenuates endotoxemia-induced liver injury. PLoS One. 2014 Jan 24;9(1):e86881.

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

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