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> Dorsomorphin [866405-64-3]

Dorsomorphin [866405-64-3]

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Référence HY-13418A-10mg

Conditionnement : 10mg

Marque : MedChemExpress

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Description

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 can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599)[1][2].

IC50 & Target[1][2]

AMPK

109 nM (Ki)

ACVR1

 

BMPR1A

 

ALK6

 

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
A2780 EC50
0.9 μM
Compound: 1; Cpd C
Antimitotic activity against human A2780 cells by ATP lite luminescence assay
Antimitotic activity against human A2780 cells by ATP lite luminescence assay
[PMID: 31831383]
MCF7 EC50
4.9 μM
Compound: 1; Cpd C
Antimitotic activity against human MCF7 cells by ATP lite luminescence assay
Antimitotic activity against human MCF7 cells by ATP lite luminescence assay
[PMID: 31831383]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dorsomorphin Related Antibodies

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.
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].

MedChemExpress (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.
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.
Masse moléculaire

399.49

Formule

C24H25N5O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Solvant et solubilité
In Vitro: 

1M HCl : 50 mg/mL (125.16 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 25 mg/mL (62.58 mM; ultrasonic and adjust pH to 3 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (25.03 mM); Suspended solution; Need ultrasonic and warming and heat to 35°C

  • Protocol 2

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 10 mg/mL (25.03 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
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