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Dorsomorphin (Compound C) 2HCl
Catalog No.S7306 Synonyms: BML-275 2HCl,Compound C 2HCl
For research use only.
Dorsomorphin 2HCl (BML-275, Compound C) 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 induces autophagy in cancer cell line.
CAS No. 1219168-18-9
Selleck's Dorsomorphin (Compound C) 2HCl has been cited by 432 publications
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Biological Activity
| Description | Dorsomorphin 2HCl (BML-275, Compound C) 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 induces autophagy in cancer cell line. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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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] |
Protocol (from reference)
| Animal Research:[3] |
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Solubility (25°C)
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In vitro |
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In vivo |
Add solvents to the product individually and in order |
15mg/mL |
Chemical Information
| Molecular Weight | 472.41 | ||
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| Formula | C24H25N5O.2HCl |
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| CAS No. | 1219168-18-9 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3.Cl.Cl | ||
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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
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