Description In vitro In vivo
ChemicalBook > CAS DataBase List > LDN212854

LDN212854

Description In vitro In vivo
Product Name
LDN212854
CAS No.
1432597-26-6
Chemical Name
LDN212854
Synonyms
CS-1202;LDN212854;BMP Inhibitor III;LDN-212854, >=98%;LDN212854 USP/EP/BP;BMP INHIBITOR III;LDN212854;LDN 212854;LDN-212854 (This product is only available in Japan.);5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyriMidin-3-yl]quinoline;5-[6-[4-(Piperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline;Quinoline, 5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-
CBNumber
CB12684548
Molecular Formula
C25H22N6
Formula Weight
406.48
MOL File
1432597-26-6.mol
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LDN212854 Property

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
InChIKey
BBDGBGOVJPEFBT-UHFFFAOYSA-N
CAS DataBase Reference
1432597-26-6
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0965
Product name
LDN-212854
Purity
≥98% (HPLC)
Packaging
5mg
Price
$179
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0965
Product name
LDN-212854
Purity
≥98% (HPLC)
Packaging
25mg
Price
$716
Updated
2024/03/01
Cayman Chemical
Product number
17698
Product name
LDN-212854
Purity
≥98%
Packaging
1mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
17698
Product name
LDN-212854
Purity
≥98%
Packaging
5mg
Price
$145
Updated
2024/03/01
Cayman Chemical
Product number
17698
Product name
LDN-212854
Purity
≥98%
Packaging
10mg
Price
$274
Updated
2024/03/01
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LDN212854 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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LDN212854 Suppliers

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View Lastest Price from LDN212854 manufacturers

Career Henan Chemical Co
Product
LDN212854 1432597-26-6
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2019-12-20

1432597-26-6, LDN212854Related Search:

LDN-212320 LDN-193189 HCl LDN-214117 5-[6-(4-Methoxyphenyl)pyrazolo[1,5-a] ALK5 inhibitor II SB525334 LDN-193189 K 02288 AT9283

  • 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
  • LDN-212854, >=98%
  • LDN-212854 (This product is only available in Japan.)
  • 5-[6-[4-(Piperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
  • LDN212854 USP/EP/BP
  • 1432597-26-6
  • 1432587-26-6
  • Inhibitors