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LDN-212854
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
LDN-212854图片
CAS NO:1432597-26-6
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)406.48
FormulaC25H22N6
CAS No.1432597-26-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 81 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

InChi Key: BBDGBGOVJPEFBT-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2

SMILES Code: C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2

SynonymsBMP Inhibitor III; LDN212854; LDN 212854; LDN-212854.
实验参考方法
In Vitro

In vitro activity: In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6- versus BMP4-induced osteogenic differentiation.

Kinase Assay: 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.

Cell Assay: 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

In Vivo
Animal model
Formulation & Dosage
References

ACS Chem Biol. 2013;8(6):1291-302.