Dorsomorphin

Dorsomorphin (Compound C) 是一種選擇性，ATP 競(jìng)爭(zhēng)性的 AMPK 抑制劑 (在沒(méi)有 AMP 的情況下，Ki 為 109 nM)。Dorsomorphin 選擇性抑制 BMP I 型受體 ALK2，ALK3 和 ALK6。Dorsomorphin 誘導(dǎo)自噬 (autophagy) 作用。

貨號(hào)：HY-13418A
CAS：866405-64-3

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-13418A

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

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Dorsomorphin (Synonyms: Compound C; BML-275)

Dorsomorphin (Compound C) 是一種選擇性，ATP 競(jìng)爭(zhēng)性的 AMPK 抑制劑 (在沒(méi)有 AMP 的情況下，K_i 為 109 nM)。Dorsomorphin 選擇性抑制 BMP I 型受體 ALK2，ALK3 和 ALK6。Dorsomorphin 誘導(dǎo)自噬 (autophagy) 作用。

生物活性：

Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (K_i=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 ALK2 ALK3 ALK6 Autophagy

109 nM (Ki)

體外研究(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].

MCE 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.

體內(nèi)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].

MCE 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.

分子量：399.49

Formula：C₂₄H₂₅N₅O

CAS 號(hào)：866405-64-3

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

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)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： Saline
Solubility: 20 mg/mL (50.06 mM); Clear solution; Need ultrasonic and adjust pH to 5 with HCl
2.

請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution
6.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution
7.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

參考文獻(xiàn)

[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.

Dorsomorphin

Dorsomorphin (Compound C) 是一種選擇性，ATP 競(jìng)爭(zhēng)性的 AMPK 抑制劑 (在沒(méi)有 AMP 的情況下，Ki 為 109 nM)。Dorsomorphin 選擇性抑制 BMP I 型受體 ALK2，ALK3 和 ALK6。Dorsomorphin 誘導(dǎo)自噬 (autophagy) 作用。

貨號(hào)：HY-13418A
CAS：866405-64-3

品牌：MCE

型號(hào)：HY-13418A

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

15906629305

在線客服

客服一

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產(chǎn)品詳情

Dorsomorphin (Synonyms: Compound C; BML-275)

Dorsomorphin (Compound C) 是一種選擇性，ATP 競(jìng)爭(zhēng)性的 AMPK 抑制劑 (在沒(méi)有 AMP 的情況下，K_i 為 109 nM)。Dorsomorphin 選擇性抑制 BMP I 型受體 ALK2，ALK3 和 ALK6。Dorsomorphin 誘導(dǎo)自噬 (autophagy) 作用。

生物活性：

Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (K_i=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 ALK2 ALK3 ALK6 Autophagy

109 nM (Ki)

體外研究(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].

MCE 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.

體內(nèi)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].

MCE 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.

分子量：399.49

Formula：C₂₄H₂₅N₅O

CAS 號(hào)：866405-64-3

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

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)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： Saline
Solubility: 20 mg/mL (50.06 mM); Clear solution; Need ultrasonic and adjust pH to 5 with HCl
2.

請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution
6.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution
7.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution