LDN212854
Synonym(s):5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
- CAS NO.:1432597-26-6
- Empirical Formula: C25H22N6
- Molecular Weight: 406.48
- MDL number: MFCD28099808
- EINECS: 808-898-3
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-31 13:32:20
What is LDN212854?
The Uses of LDN212854
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.
Properties of LDN212854
Density | 1.33±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: soluble1mg/mL, clear (warmed) |
form | powder |
pka | 8.79±0.10(Predicted) |
color | white to beige |
CAS DataBase Reference | 1432597-26-6 |
Safety information for LDN212854
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral |
Precautionary Statement Codes |
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
Computed Descriptors for LDN212854
InChIKey | BBDGBGOVJPEFBT-UHFFFAOYSA-N |
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