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
- Molecular Weight:
- 406.48
- MDL Number:
- MFCD28099808
- MOL File:
- 1432597-26-6.mol
- MSDS File:
- SDS
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 |
LDN212854 price More Price(29)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML0965 | LDN-212854 ≥98% (HPLC) | 1432597-26-6 | 5mg | $179 | 2024-03-01 | Buy |
Sigma-Aldrich | SML0965 | LDN-212854 ≥98% (HPLC) | 1432597-26-6 | 25mg | $716 | 2024-03-01 | Buy |
Cayman Chemical | 17698 | LDN-212854 ≥98% | 1432597-26-6 | 1mg | $36 | 2024-03-01 | Buy |
Cayman Chemical | 17698 | LDN-212854 ≥98% | 1432597-26-6 | 5mg | $145 | 2024-03-01 | Buy |
Cayman Chemical | 17698 | LDN-212854 ≥98% | 1432597-26-6 | 10mg | $274 | 2024-03-01 | Buy |
LDN212854 Chemical Properties,Uses,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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29825 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 24330 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |