LDN193189 Hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LDN193189是骨形态发生蛋白（BMP）I型受体转录活性的选择性抑制剂，抑制活化素受体样激酶2（ALK2）和ALK3，相应IC50值为5 nM和30 nM[1]。
在C2C12细胞中，LDN193189可以抑制BMP诱导的Smad信号（Smad1/5/8）和非Smad信号磷酸化，包括p38和Akt[2]。
在支气管上皮（Beas2B）细胞和C57BL/6小鼠中，LDN193189对BMP的药理抑制作用可以防止BMP2诱导的E-钙粘蛋白下调。在细胞水平上，LDN193189也能抑制BMP诱导的上皮通透性减少[3]。
参考文献：
[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.
- 1. Xin Yu, Shiguang Li, et al. "Androgen Maintains Intestinal Homeostasis by Inhibiting BMP Signaling via Intestinal Stromal Cells." Stem Cell Reports 2020 Aug 20;S2213-6711(20)30332-5 PMID:32916121
- 2. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 552.33 |
| Cas No. | 1062368-62-0 |
| Formula | C25H26Cl4N6 |
| Synonyms | LDN 193189 hydrochloride; LDN-193189 hydrochloride |
| Solubility | ≥27.6 mg/mL in H2O; insoluble in EtOH; ≥16.4 mg/mL in DMSO |
| Chemical Name | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline tetrahydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CN(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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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. |
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| 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 | ||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
