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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Cited by 17 Publications

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 NXnNT5V4TnWwY4Tpc44h[XO|YYm= NYDWUWprPCEQvF2= NX;LTmhnUW6qaXLpeIlwdiCxZjDCUXBTOS2vZXTpZZRm\CCxc4Tlc4Jt[XO2IHTp[oZmemWwdHnheIlwdiCrbjDCUXA1NXO2aX31cIF1\WRibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[WytYXzpcoUheGixc4DoZZRie2VibHX2[Ywh[XRiNDD1UUBjgSC|cHXjeJJweGixdH;t[ZRzgQ>? MYOxPFAzPjB7NB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-SMAD / SMAD; 

PubMed: 30808965     


SMAD phosphorylation was assessed by Western blot after cells were treated with dorsomorphin (0 µM to 10 µM) from day 1 to day 3 or from day 3 to day 4.

Id1 / Id2 / Id3 ; 

PubMed: 25010525     


Dorsomorphin dramatically inhibited the expression of Ids. KMM cells were treated with 5 µM Dorsomorphin for 24 hours before harvesting. Expressions of Ids were detected by immunoblotting.

pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α ; 

PubMed: 29531259     


PC-3 and LNCaP cells were treated with vehicle, 25 µM compound 8c, 25 µM compound 8c + 5 μM Dorsomorphin (8c + D) or 5 μM Dorsomorphin (D), for 1 hour or 24 hours and levels of the phosphorylated AMPK (pAMPK), phosphorylated ACC (pACC), phosphorylated Raptor (pRaptor) forms and HIF1α were determined by Western blot. Upper panel, representative Western blot of three different experiments. β-tubulin (β-Tub) serves as a loading control. Lower panel, densitometric analyses of bands represented as the mean of the ratio pAMPK/AMPK or pACC/ACC.

p-ERK / ERK / Bcl2 / BAX / Cleaved caspase-3; 

PubMed: 30155931     


Western blot analysis of the protein expression of ERK, p‐ERK, Bcl2, BAXand cleaved caspase‐3 in T98 cells stimulated by Compound C (0, 1, 5, 10 μmol/L) for 24 h.

LC3B I/ LC3B II; 

PubMed: 30155931     


The representative western blot analysis showed that stimulation by Compound C for 24 h decreased the ratio of LC3BI/IIin T98 cells in a dose-dependent manner. 

30808965 25010525 29531259 30155931
Immunofluorescence
MyHC; 

PubMed: 20689554     


Satellite cell-derived myoblasts were plated at high cell density (80–90% confluency) and cultured in proliferation medium for 2 days with or without Dorsomorphin. Immunostaining for MyHC showed that Dorsomorphin promoted myogenic differentiation and fusion in a dose-dependent manner. 

Id1 / MyoD ; 

PubMed: 20689554     


(a) Exposure to 3 μM Dorsomorphin for 6 h to inhibit BMP signalling resulted in a downregulation of Id1 expression in satellite cells associated with a myofibre. (b) Similarly, immunostaining of plated satellite cells after exposure to 3 μM Dorsomorphin for 18 h in proliferation medium also resulted in downregulation of Id1 protein. Scale bar equals 20 μm.

20689554
Growth inhibition assay
Cell viability (MM cells); 

PubMed: 25010525     


Dorsomorphin showed preferential toxicity to KMM (KSHV-transformed MM cells) cells. KMM cells or MM cells were seeded 4000 cells/well. 24 hours after seeding, medium was replaced with Dorsomorphin medium as indicated. Cell viability was measured by MTT assay 48 hours post Dorsomorphin treatment. Data were shown as mean ± s.e.m., n = 3. 

Cell viability (glioma cell lines); 

PubMed: 24419061     


Histogram showing the dose-dependent effect of Compound C (1, 2.5, 5 and 10μM) on the viability of three glioma cell lines. Numbers inside bars represent % dead cells.

25010525 24419061
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 to the product individually and in order(Data is from Selleck tests instead of citations):
PBS
For best results, use promptly after mixing.
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
in solvent
Synonyms BML-275 2HCl,Compound C 2HCl

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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.

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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

AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID