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HomeProduct name listLDN212854

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
LDN212854 Structural

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)
ghs
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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