LDN-193189
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是一种选择性的转录活性形态发生蛋白(BMP)I型受体抑制剂,抑制活化素受体样激酶-2(ALK2)和ALK3,IC50值分别为5 nM和30 nM[1]。
在C2C12细胞中,LDN193189抑制BMP诱导的Smad信号(Smad1/5/8)和非Smad信号(包括p38和Akt)的磷酸化[2]。
在支气管上皮(Beas2B)细胞和C57BL/6小鼠中,LDN193189对BMP的药理学抑制可阻止BMP2诱导的E-钙粘蛋白下调。LDN193189也抑制细胞水平BMP诱导的上皮通透性的减少[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. Michael Raymond, Warren Vieira, et al. "Development of a model system to study the regulation of patterning competency in regenerating axolotl limbs." Research Square. 07 Dec, 2023.
- 2. Wai Kit Chan, Danilo Negro, et al. "Loss of PAX6 alters the excitatory/inhibitory neuronal ratio in human cerebral organoids." bioRvix. August 01, 2023.
- 3. Xiaoya An, Guoliang Wang, et al. "Novel cell culture paradigm prolongs mouse corneal epithelial cell proliferative activity in vitro and in vivo." Front Cell Dev Biol. 2021 Jun 30;9:675998. PMID: 34277619
- 4. Xin Yu, Shiguang Li, et al. "Androgen Maintains Intestinal Homeostasis by Inhibiting BMP Signaling via Intestinal Stromal Cells." Stem Cell Reports. 2020 Oct 13;15(4):912-925. PMID: 32916121
- 5. Xiaohong Zhang, Xueshuang Xing, et al. "Ionizing radiation induces ferroptosis in granulocyte-macrophage hematopoietic progenitor cells of murine bone marrow." Int J Radiat Biol , 1-35 2020 Jan 6. PMID: 31906761
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 406.48 |
Cas No. | 1062368-24-4 |
Formula | C25H22N6 |
Synonyms | LDN 193189;LDN193189 |
Solubility | insoluble in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline |
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 |
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肌成纤维细胞,支气管上皮(Beas2B)细胞 |
溶解方法 |
该化合物在DMSO中的溶解度有限。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 |
0.005-5 μM,30-60 min |
应用 |
在C2C12细胞中,LDN-193189抑制BMP诱导的Smad1/5/8磷酸化和BMP介导的p38 MAPK、Erk1/2和Akt通路。LDN-193189以剂量依赖性方式抑制Smad1/5/8、p38和Akt的活化。LDN-193189显著增加磷酸化p38 MAPK水平,轻微增加p-Akt的含量。LDN(10 μM,60分钟)诱导p38和Akt磷酸化。LDN(0.5 μM,30 min)抑制BMP介导的Smad1/5/8、p38、ATF2和CREB磷酸化。 |
动物实验 [2]: | |
动物模型 |
C57BL/6小鼠 |
给药剂量 |
腹腔注射,每12小时3 mg/kg |
应用 |
在Ad.Cre注射的表达CaALK2的小鼠中,LDN-193189处理可防止P15的放射损伤。LDN-193189处理的小鼠在P30和P60处保留膝盖和踝关节。LDN-193189处理的小鼠在P15处没有显示异位骨,但在周围的软组织中软骨形成增强。在P30没有放射学可见的疾病的情况下,LDN-193189处理的小鼠表现出轻微的运动受损。 |
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]. 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]. 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. |
Description | LDN193189是一种选择性的BMP信号抑制剂,作用于BMP I型受体ALK2和ALK3,IC50值分别为5 nM和30 nM。 | |||||
靶点 | ALK2 | ALK3 | ||||
IC50 | 5 nM | 30 nM |
质量控制和MSDS
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