COMPOUND C
Dorsomorphin
CAS: 866405-64-3
Molecular Formula: C24H25N5O
COMPOUND C - Names and Identifiers
COMPOUND C - Physico-chemical Properties
| Molecular Formula | C24H25N5O |
| Molar Mass | 399.49 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Melting Point | >228°C(dec.) |
| Solubility | DMSO: >2mg/mL (warmed) |
| Appearance | powder |
| Color | white to beige |
| pKa | 8.53±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | In hepatocytes, Dorsomorphin inhibits ACC inactivation by AICAR or metformin and attenuates the effect of AICAR or metformin to increase fatty acid oxidation or inhibit adipogenic genes. Inhibition of AMPK activity by Dorsomorphin almost completely inhibited autophagy proteolysis in HT-29 cells. In addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2,ALK3 and ALK6, thereby blocking BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. |
| In vivo study | Dorsomophin (10 mg/kg) decreased basal levels of hepcidin expression in adult mice and increased serum iron concentrations. Dorsomorphin (0.2 mg/kg, I. v.) significantly reduced VCAM-1 and ICAM-1 expression in LPS-treated rat thoracic aortas. |
COMPOUND C - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
COMPOUND C - Biological activity
Dorsomorphin (Compound C, BML-275) is an effective, reversibly selective AMPK inhibitor. Ki is 109 nM in cell-free test. It is effective for several structurally related kinases, including ZAPK,SYK,PKC & theta;,PKA, and JAK3 have no significant inhibitory effect. It also inhibits the activity of type I BMP receptors ALK2,ALK3 and ALK6. Dorsomorphin are applied to promote the differentiation of specific cells and induce autophagy of cancer cells. For animal experiments, it is recommended to choose the water soluble product S7306 Dorsomorphin (Compound C) 2HCl.
Last Update：2024-04-10 22:29:15
COMPOUND C - Research
In vitro studies
In hepatocytes, Dorsomorphin inhibits ACC inactivation through AICAR or metformin, and attenuates the effects of AICAR or metformin on increasing fatty acid oxidation or inhibiting lipogenic genes. In HT-29 cells, Dorsomorphin inhibition of AMPK activity almost completely inhibited autophagy protein hydrolysis. In addition, Dorsomorphin selectively inhibit BMP type I receptors ALK2,ALK3 and ALK6, thereby blocking BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation.
In vivo studies
Dorsomorphin (10 mg/kg) reduces the basal level of ferritin expression in adult mice and increases the concentration of serum iron. Dorsomorphin (0.2 mg/kg, I. v.) significantly reduced the expression of VCAM-1 and ICAM-1 in LPS-treated thoracic aorta of rats.
Last Update：2024-04-09 20:52:54
COMPOUND C - Reference Information
| biological activity | Dorsomorphin (Compound C, BML-275) is an effective, reversibly selective AMPK inhibitor. Ki is 109 nM in cell-free test and has no significant inhibitory effect on several structurally related kinases, including ZAPK,SYK,PKCθ,PKA, and JAK3. It also inhibits the activity of type I BMP receptors ALK2,ALK3 and ALK6. Dorsomorphin are applied to promote the differentiation of specific cells and induce autophagy of cancer cells. For animal experiments, it is recommended to choose the water soluble product S7306 Dorsomorphin (Compound C) 2HCl. |
| 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 | in hepatocytes, Dorsomorphin inhibit ACC inactivation through AICAR or metformin, and weaken the effect of AICAR or metformin on increasing fatty acid oxidation or inhibiting adipogenesis genes. In HT-29 cells, Dorsomorphin inhibition of AMPK activity almost completely inhibited autophagy protein hydrolysis. In addition, Dorsomorphin selectively inhibit BMP type I receptors ALK2,ALK3 and ALK6, thereby blocking BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. |
| in vivo study | Dorsomorphin (10 mg/kg) reduces the basal level of ferritin expression in adult mice and increases the concentration of serum iron. Dorsomorphin (0.2 mg/kg, I. v.) significantly reduced the expression of VCAM-1 and ICAM-1 in LPS-treated thoracic aorta of rats. |
Last Update：2024-04-09 21:04:16
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