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
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
N-Bromosuccinimide Price
- Product number
- SML0965
- Product name
- LDN-212854
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $179
- Updated
- 2024/03/01
- Product number
- SML0965
- Product name
- LDN-212854
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $716
- Updated
- 2024/03/01
- Product number
- 17698
- Product name
- LDN-212854
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
- Product number
- 17698
- Product name
- LDN-212854
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $145
- Updated
- 2024/03/01
- Product number
- 17698
- Product name
- LDN-212854
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $274
- Updated
- 2024/03/01
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
LDN212854 Suppliers
- Tel
- --
- Fax
- --
- info@axonmedchem.com
- Country
- The Netherlands
- ProdList
- 477
- Advantage
- 30
View Lastest Price from LDN212854 manufacturers
- Product
- LDN212854 1432597-26-6
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100KG
- Release date
- 2019-12-20