product name LDN-212854
Description: LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively. LDN-212854 potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. In vitro, LDN-212854 exhibits some selectivity for ALK2 in preference to other BMP type I receptors, ALK1 and ALK3, which may permit the interrogation of ALK2-mediated signaling, transcriptional activity and function.
References: ACS Chem Biol. 2013;8(6):1291-302.
406.48
Formula
C25H22N6
CAS No.
1432597-26-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 81 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BMP Inhibitor III
other peoduct :
| In Vitro |
In vitro activity: In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6- versus BMP4-induced osteogenic differentiation. Kinase Assay: In the kinase assay, LDN-212854 shows inhibitory activities against caALK2 and caALK5 with IC50 values of 16nM and 2μM, respectively. It demonstrates that LDN-212854 is selective against BMP over TGF-β signaling. Besides that, the inhibition of caALK2 caused by LDN-212854 is 6- and 10-fold more potent than that of caALK1 and caALK3, respectively. Cell Assay: In C2C12 cells transfected with BMP receptors, LDN-212854 also exerts preferential inhibition against caALK2. Furthermore, in a transgenic ALK2Q207D model of heterotopic ossification, treatment of LDN-212854 prevents the formation of heterotopic bone and preserves limb range of motion |
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| In Vivo | |
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| Formulation & Dosage | |
| References | ACS Chem Biol. 2013;8(6):1291-302. |
