|5-(6-(4-(哌嗪-1-基)苯基)吡唑并[1,5-a]嘧啶-3-基)喹啉|CsnPharm

CAS No.: 1432597-26-6

LDN-212854/5-(6-(4-(哌嗪-1-基)苯基)吡唑并[1,5-a]嘧啶-3-基)喹啉 Catalog No. CSN17852

Synonyms: BMP Inhibitor III;5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉

LDN-212854 is an inhibitor of BMP and can inhibit ALK2 with IC50 of 1.3 nM. It is used to prevent heterotopic ossification.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ALK1

IC50:2.4nM ALK3

IC50:85.8nM ALK2

IC50:1.3nM
描述The bone morphogenetic protein (BMP) signaling pathway has essential functions in development, homeostasis, and in the normal and pathophysiologic remodeling of tissues. BMPs initiate their signaling events through an interaction of their type I and type II receptors, both of which are transmembrane serine/threonine kinases. Seven type I receptors (a.k.a. activin receptor-like receptors; ALK1 to ALK7) and four type II receptors have been identified in mice and humans^[3].. LDN-212854 is a selective and potent inhibitor of the BMP type I receptor kinases, with the IC50 values of 1.3 nM, 2.4 nM, 85.8 nM, 2133 nM, 9276 nM for ALK2, ALK1, ALK3, ALK4 and ALK5, respectively. LDN-212854 (IC50=37 nM) displayed low nanomolar potency in blocking the phosphorylation of SMAD1/5/8 induced by BMP7 (20 ng/mL, 30 min) in BMPR2^−/− pulmonary vascular smooth muscle cells. ALK2^Q207D transgenic mice model was used to evaluate the efficacy of LDN-212854 in vivo. After pretreating pericytes with 570nM LDN-212854 for 1 day, the osteoblast differentiation of pericytes from FOR hiPSCs was partly inhibited. Treatment with LDN-212854 on the dose of 6 mg/kg twice daily for 4 weeks can prevent the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice^[4].
作用机制LDN-212854 binds type I BMP receptor at the ATP-binding pocket. The pendant 5-quinoline group of LDN-212854 is predicted to form an alternative water-mediated hydrogen bond to the catalytic lysine (K235) of ALK2^[5].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
mouse C2C12BRA cells	-	Function assay	14 h	Inhibition of BMP4 in mouse C2C12BRA cells after 14 hrs by luciferase reporter gene assay, IC50=0.117 μM	23639540

动物研究
剂量
Mice: 6 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 6 mg/kg^[1] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4601 mL
- 12.3007 mL
- 24.6013 mL
- 5 mM
- 0.4920 mL
- 2.4601 mL
- 4.9203 mL
- 10 mM
- 0.2460 mL
- 1.2301 mL
- 2.4601 mL

技术信息

CAS号

1432597-26-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H22N6

运输

蓝冰

分子量

406.48

别名

BMP Inhibitor III;5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉

溶解度

DMSO	79.0 mg/mL (194.4 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
ALK1		IC50:2.4nM
ALK3		IC50:85.8nM
ALK2		IC50:1.3nM

LDN-212854/5-(6-(4-(哌嗪-1-基)苯基)吡唑并[1,5-a]嘧啶-3-基)喹啉 Catalog No. CSN17852

靶点选择性

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