Biological Activity
Potent inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM). Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKCθ, PKA and JAK3. Inhibits AMPK activation induced by AICAR (Cat. No. 2840) and metformin (Cat. No. 2864). Also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6). Promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro. Shown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.
Compound Libraries
Dorsomorphin dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 472.41 |
| Formula | C24H25N5O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1219168-18-9 |
| PubChem ID | 49761481 |
| InChI Key | RJDVIJJQKMGPMV-UHFFFAOYSA-N |
| Smiles | C(C=N2)(C4=CC=C(OCCN5CCCCC5)C=C4)=CN1C2=C(C3=CC=NC=C3)C=N1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.45 | 20mM with gentle warming | |
| water | 47.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 472.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.58 mL | 21.17 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Zhou et al (2001) Role of AMP-activated protein kinase in mechanism of metformin action. J.Clin.Invest. 108 1167 PMID: 11602624
Yu et al (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat.Chem.Biol. 4 33 PMID: 18026094
Vucicevic et al (2011) Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7 40 PMID: 20980833
Hao et al (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3 2904 PMID: 18682835
Diekmann et al (2015) A reliable and efficient protocol for human pluripotent stem cell differentiation into the definitive endoderm based on dispersed single cells. Stem Cells Dev. 24 190 PMID: 25137387
Keywords: Dorsomorphin dihydrochloride, supplier, Potent, AMPK, inhibitors, inhibits, BMP, type, I, receptor, ALK2, ALK3, ALK6, AMP-Activated, Protein, Kinases, Receptors, Activin, Receptor-like, Receptor, Serine/Threonine, RSTKs, stem, cells, BML275, 866405-64-3, Compound, C, BML-275, BMP, and, Other, Activin, Receptors, AMPK, Autophagy, Cardiomyocyte, Stem, Cells, ESCs, and, iPSC, AMPK, Tocris Bioscience
