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Formula | C24H25N5O |
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Molecular Weight | 399.49 | CAS No. | 866405-64-3 | |
Solubility (25°C)* | In vitro | DMSO | 5 mg/mL warmed with 50ºC water bath (12.51 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Dorsomorphin 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. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended. | ||||||||
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Targets |
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In vitro | Dorsomorphin inhibits ACC inactivation by either AICAR, and also attenuates AICAR’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] |
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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] |
Kinase Assay: |
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Animal Study: |
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, , J Cell Physiol, 2017, 232(7):1893-1906
, , Clin Exp Pharmacol Physiol, 2016, 43(1):125-34.
Data from [Data independently produced by , , Oncotarget, 2016, 6(41):43605-19.]
Data from [Data independently produced by , , Exp Cell Res, 2016, 345(1):25-36.]
ALKBH5 governs human endoderm fate by regulating the DKK1/4-mediated Wnt/β-catenin activation [ Nucleic Acids Res, 2024, gkae707] | PubMed: 39166492 |
Autism patient-derived SHANK2BY29X mutation affects the development of ALDH1A1 negative dopamine neuron [ Mol Psychiatry, 2024, 10.1038/s41380-024-02578-6] | PubMed: 38704506 |
Progranulin promotes regulatory T cells plasticity by mitochondrial metabolism through AMPK/PGC-1α pathway in ARDS [ Clin Immunol, 2024, 261:109940] | PubMed: 38365048 |
A splice site variant in MADD affects hormone expression in pancreatic β cells and pituitary gonadotropes [ JCI Insight, 2024, 9(10)e167598] | PubMed: 38775154 |
Metformin enhances endogenous neural stem cells proliferation, neuronal differentiation, and inhibits ferroptosis through activating AMPK pathway after spinal cord injury [ J Transl Med, 2024, 22(1):723] | PubMed: 39103875 |
Artemisinin conferred cytoprotection to human retinal pigment epithelial cells exposed to amiodarone-induced oxidative insult by activating the CaMKK2/AMPK/Nrf2 pathway [ J Transl Med, 2024, 22(1):844] | PubMed: 39285426 |
Methionine deficiency inhibited pyroptosis in primary hepatocytes of grass carp (Ctenopharyngodon idella): possibly via activating the ROS-AMPK-autophagy axis [ J Anim Sci Biotechnol, 2024, 15(1):116] | PubMed: 39218924 |
Multiple factors to assist human-derived induced pluripotent stem cells to efficiently differentiate into midbrain dopaminergic neurons [ Neural Regen Res, 2024, 19(4):908-914] | PubMed: 37843228 |
Calpain-1 Up-Regulation Promotes Bleomycin-Induced Pulmonary Fibrosis by Activating Ferroptosis [ Am J Pathol, 2024, S0002-9440(24)00356-0] | PubMed: 39326733 |
Ultrasound-targeted microbubble technology facilitates SAHH gene delivery to treat diabetic cardiomyopathy by activating AMPK pathway [ iScience, 2024, 27(2):108852] | PubMed: 38303706 |
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