Dorsomorphin (Compound C) 2HCl
Catalog No.S7306 Synonyms: BML-275 2HCl,Compound C 2HCl
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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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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|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.|
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.  Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells.  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. 
|In vivo||Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice.  Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. |
|In vitro||Water||94 mg/mL (198.97 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
|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|
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Frequently Asked Questions
Is there any information you may provide as to WHICH AMPK SUBUNIT is this drug targeting in the AMPK complex?
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