Dorsomorphin 2HCl - Names and Identifiers
Dorsomorphin 2HCl - Physico-chemical Properties
Molecular Formula | C24H27Cl2N5O
|
Molar Mass | 472.41008 |
Appearance | Light yellow powder solid. |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Use | A potent and selective AMPK inhibitor. |
In vitro study | Dorsomorphin inhibits the inactivation of ACC by AICAR or metformin, and also attenuates the effect of AICAR and metformin in hepatocytes to increase fatty acid oxidation or inhibit adipogenic genes. Inhibition of AMPK activity by Dorsomorphin almost completely inhibited proteolysis of autophagy in HT-29 of 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 study | In adult mice, Dorsomorphin (10 mg/kg) decreased basal levels of hepatic bactericidal peptide expression and increased serum iron concentration. Dorsomorphin (0.2 mg/kg, I. V.) significantly reduced VCAM-1 and ICAM-1 expression in LPS-treated rat thoracic aortas. |
Dorsomorphin 2HCl - Introduction
Dorsomorphin 2HCl is an effective and reversible AMPK selective inhibitor with Ki of 109 nM. It has no significant inhibitory effect on some structure-related kinases, including ZAPK, SYK, PKCθ, PKA and JAK3. At the same time, it inhibits the effect of BMP type I receptor.
Last Update:2022-10-16 17:41:20
Dorsomorphin 2HCl - Reference Information
biological activity | Dorsomorphin 2HCl (BML-275, Compound c) is an effective, reversible and selective AMPK inhibitor. Ki is 109 nM in cell-free test. it is effective for some structurally related kinases, including ZAPK, SYK, PKCθ,PKA and JAK3 had no significant inhibitory effect. It also inhibits type I BMP receptors. Dorsomorphin can induce autophagy of cancer cell lines. |
target | TargetValue ALK2 () ALK3 () ALK6 () AMPK (Cell-free say) 109 nM(Ki) |
Target | Value |
ALK2
()
| |
ALK3
()
| |
ALK6
()
| |
AMPK
(Cell-free assay)
| 109 nM(Ki) |
in vitro study | Dorsomorphin inhibit ACC inactivation caused by AICAR or metformin, and also weaken the effects of AICAR and metformin in liver cells on increasing fatty acid oxidation or inhibiting adipogenesis genes. Dorsomorphin inhibition of AMPK activity almost completely inhibited the proteolysis of autophagy in HT-29 cells. In addition, Dorsomorphin selectively inhibits 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 studies | in adult mice, Dorsomorphin (10 mg/kg) reduces the basal level of hepatosmicidal peptide expression and increases the concentration of iron ions in serum. Dorsomorphin (0.2 mg/kg, intravenous injection) significantly reduced the expression of VCAM-1 and ICAM-1 in thoracic aorta of LPS-treated rats. |
use | an effective, selective and ATP competitive AMPK inhibitor, Ki:109nM. |
Last Update:2024-04-09 20:52:54