Dorsomorphin (Compound C) 2HCl

Catalog No.S7306 Synonyms: BML-275 2HCl,Compound C 2HCl

Dorsomorphin (Compound C) 2HCl Chemical Structure

Molecular Weight(MW): 472.41

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.

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4 Customer Reviews

  • AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. *P < 0.05, ***P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group.

    Mol Brain, 2015 ,8:20.. Dorsomorphin (Compound C) 2HCl purchased from Selleck.

    MEFs were cultured under hypoxia, and the activity of endogenous AMPK was inhibited with Dorsomorphin 2HCl (1 μM). Cells were fixed in 4% paraformaldehyde and stained with anti-TIM23(mouse) and anti-ULK1 (rabbit) primary antibodies then Alexa Fluor 488-labeled donkey anti-rabbit IgG and Alexa Fluor 555-labeled donkey anti-mouse IgG secondary antibodies before analysis by immunofluorescence microscopy. Arrows indicate ULK1 puncta that colocalize with mitochondria. Bar, 10 μm.

    FEBS Lett, 2015, 589(15):1847-54.. Dorsomorphin (Compound C) 2HCl purchased from Selleck.

  • MEFs were cultured under hypoxia for 6 h and treated with Dorsomorphin 2HCl (1 μM) to inhibit AMPK, si-AMPK to knock down endogenous AMPK, or Metformin (2 mM) to activate AMPK. The cells were fixed in 4% paraformaldehyde and stained with anti-TIM23 (mouse) and anti-LC3 (rabbit) primary antibodies then Alexa Fluor 488-labeled donkey anti-mouse IgG and Alexa Fluor 555-labeled donkey anti-rabbit IgG secondary antibodies before analysis by immunofluorescence microscopy. Bar, 10 μm.

    FEBS Letters, 2015, 1847-1854.. Dorsomorphin (Compound C) 2HCl purchased from Selleck.

    The expression levels of pSmad1/5 were analyzed after 12 h of RA treatment, 2 h of dorsomorphin (Dorso, inhibitor of BMP signaling pathway) treatment, or both. Similar results were obtained in two separate experiments.

    BMC Biotechnol, 2017, 17(1):17. Dorsomorphin (Compound C) 2HCl purchased from Selleck.

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Biological Activity

Description Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.
Targets
AMPK [1]
(Cell-free assay)
109 nM(Ki)
In vitro

Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse C2C12 cells M2XONGZ2dmO2aX;uJIF{e2G7 M{XDblQh|ryP NV7RR2RjUW6qaXLpeIlwdiCxZjDCUXBTOS2vZXTpZZRm\CCxc4Tlc4Jt[XO2IHTp[oZmemWwdHnheIlwdiCrbjDCUXA1NXO2aX31cIF1\WRibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[WytYXzpcoUheGixc4DoZZRie2VibHX2[Ywh[XRiNDD1UUBjgSC|cHXjeJJweGixdH;t[ZRzgQ>? NXjaT|lCOThyMk[wPVQ>

... Click to View More Cell Line Experimental Data

In vivo Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Iron-replete mice
  • Formulation: DMSO
  • Dosages: ~10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro Water 94 mg/mL (198.97 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
PBS
15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.41
Formula

C24H25N5O.2HCl

CAS No. 1219168-18-9
Storage powder
Synonyms BML-275 2HCl,Compound C 2HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01251562 Suspended Solid Tumors Berg, LLC January 2011 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Is there any information you may provide as to WHICH AMPK SUBUNIT is this drug targeting in the AMPK complex?

  • Answer:

    According to the reference (see link below), Dorsomorphin(Compound C) should target the AMPK alpha subunit through ALCAR or metformin. http://www.ncbi.nlm.nih.gov/pubmed/20844250

Related Antibodies

AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID