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LDN193189 Hydrochloride

现货
Catalog No.
A3545
ALK选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,500.00
现货
5mg
¥ 850.00
现货
10mg
¥ 1,600.00
现货
50mg
¥ 6,000.00
现货

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Background

LDN193189 is a selective transcriptional activity morphogenetic protein (BMP) type I receptors inhibitor. It inhibits activin receptor-like kinase-2 (ALK2) and ALK3 with IC50 values of 5 nM and 30 nM, respectively [1].

LDN193189 has been showed to inhibit BMP induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling including p38 and Akt in C2C12 cells [2].

Pharmacological inhibition of BMP by LDN193189 has shown to prevent down-regulation of E-cadherin in response to BMP2 both in bronchial epithelial (Beas2B) cells and in C57BL/6 mice. LDN193189 also inhibits the BMP-induced reduction of epithelial permeability at cellular level [3].

References:
[1] Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9.
[2] Boergermann JH1, Kopf J, Yu PB, Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol. 2010 Nov;42(11):1802-7.
[3] Helbing T1, Herold EM, Hornstein A, Wintrich S, Heinke J, Grundmann S, Patterson C, Bode C, Moser M. Inhibition of BMP activity protects epithelial barrier function in lung injury. J Pathol. 2013 Sep;231(1):105-16. doi: 10.1002/path.4215. Epub 2013 Jul 10.

文献引用

1. Bae JS, Jeon Y, et al. "Depletion of MOB1A/B causes intestinal epithelial degeneration by suppressing Wnt activity and activating BMP/TGF-β signaling." Cell Death Dis. 2018 Oct 22;9(11):1083. PMID:30349003

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt552.33
Cas No.1062368-62-0
FormulaC25H26Cl4N6
SynonymsLDN 193189 hydrochloride; LDN-193189 hydrochloride
Solubility≥16.4 mg/mL in DMSO, ≥27.6 mg/mL in H2O, <2.59 mg/mL in EtOH
Chemical Name4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline tetrahydrochloride
SDFDownload SDF
Canonical SMILESC1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3.Cl.Cl.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

C2C12细胞

溶解方法

该化合物在DMSO中的溶解度大于2.1 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

100 nM,0-72h

应用

在BMP刺激后12小时,LDN-193189抑制BMP4 诱导的C2C12细胞中碱性磷酸酶活性。

动物实验 [2, 3]:

动物模型

条件性CaALK2转基因小鼠,PCa-118b荷瘤小鼠

给药剂量

腹腔注射,3 mg/kg

应用

在出生后第7天(P7)的Ad.Cre条件性CaALK2转基因小鼠中,腹腔注射LDN-193189(3 mg/kg)导致左胫骨周围的轻度钙化,引起P13上产生可见的腓骨,并且防止P15处的放射损伤,不引起体重减轻或发育迟缓、自发性骨折、骨密度降低或行为异常等现象。在PCa-118b肿瘤小鼠中,LDN-193189减轻肿瘤生长并减少肿瘤中的骨形成。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Boergermann JH1, Kopf J, Yu PB, Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol. 2010 Nov;42(11):1802-7.

[2]. Paul B Y, Deng D Y, Lai C S, et al. BMP type I receptor inhibition reduces heterotopic ossification[J]. Nature medicine, 2008, 14(12): 1363-1369.

[3]. Lee Y C, Cheng C J, Bilen M A, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis[J]. Cancer research, 2011, 71(15): 5194-5203.

生物活性

Description LDN193189 HCl,LDN193189的盐酸盐,是BMP信号的选择性抑制剂,对BMP I型受体ALK2和ALK3转录活性的IC50值分别为5 nM和30 nM。
靶点   ALK3        
IC50 5 nM 30 nM        

质量控制

化学结构

LDN193189 Hydrochloride

相关生物数据

LDN193189 Hydrochloride