product name Dorsomorphin
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. Dorsomorphin is also an inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.
References: Nat Chem Biol. 2008 Jan;4(1):33-41; J Biol Chem. 2006 Nov 17;281(46):34870-9.
399.49
Formula
C24H25N5O
CAS No.
866405-64-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (7.5 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (5.0 mM)
Solubility (In vivo)
Synonyms
BML-275,Compound C
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393266
| In Vitro |
In vitro 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Iron-replete mice |
| Formulation & Dosage | Dissolved in DMSO; 10 mg/kg; i.v. administration |
| References | Nat Chem Biol. 2008 Jan;4(1):33-41; Atherosclerosis. 2011 Nov;219(1):57-64. (3):302-15. |
Related Posts
product name Dorsomorphin
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. Dorsomorphin is also an inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.
References: Nat Chem Biol. 2008 Jan;4(1):33-41; J Biol Chem. 2006 Nov 17;281(46):34870-9.
399.49
Formula
C24H25N5O
CAS No.
866405-64-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (7.5 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (5.0 mM)
Solubility (In vivo)
Synonyms
BML-275,Compound C
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393266
| In Vitro |
In vitro 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Iron-replete mice |
| Formulation & Dosage | Dissolved in DMSO; 10 mg/kg; i.v. administration |
| References | Nat Chem Biol. 2008 Jan;4(1):33-41; Atherosclerosis. 2011 Nov;219(1):57-64. (3):302-15. |