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| Product Name: | LDN212854 | | Synonyms: | LDN212854;Quinoline, 5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-;BMP Inhibitor III;5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyriMidin-3-yl]quinoline;CS-1202;BMP INHIBITOR III;LDN212854;LDN 212854;5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline LDN 212854;LDN 212854 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline | | CAS: | 1432597-26-6 | | MF: | C25H22N6 | | MW: | 406.48 | | EINECS: | 808-898-3 | | Product Categories: | Inhibitors | | Mol File: | 1432597-26-6.mol |  |
| | LDN212854 Chemical Properties |
| density | 1.33±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble1mg/mL, clear (warmed) | | pka | 8.79±0.10(Predicted) | | form | powder | | color | white to beige | | InChIKey | BBDGBGOVJPEFBT-UHFFFAOYSA-N | | CAS DataBase Reference | 1432597-26-6 |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 |
| | LDN212854 Usage And Synthesis |
| 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. | | In vitro | In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6-versus BMP4-induced osteogenic differentiation. | | In vivo | LDN-212854 (6 mg/kg, i.p.) effectively neutralize ALK2 signaling in vivo, and potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. | | Uses | 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline, contains the pyrazolo[1,5-a]pyrimidine scaffold, acting as a novel and selective bone morphogenetic protein receptor (BMP) inhibitors. It is a COVID19-related research product. | | Biological Activity | ldn-212854 is a selective inhibitor of bone morphogenetic protein (bmp) signaling with ic50 value of 1.2nm [1].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. 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 [1]. | | Biochem/physiol Actions | LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2). | | references | [1] mohedas a h, xing x, armstrong k a, et al. development of an alk2-biased bmp type i receptor kinase inhibitor. acs chemical biology, 2013, 8(6): 1291-1302. |
| | LDN212854 Preparation Products And Raw materials |
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