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LDN193189

产品编号 T1935 CAS 1062368-24-4

别名: LDN-193189, DM-3189, LDN 193189

LDN193189 (LDN-193189) 是BMPI 型受体的选择性抑制剂，能够抑制 ALK2 (IC50:5 nM)、 ALK3 (IC50:30 nM)。对 ALK4、ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。

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LDN193189, CAS 1062368-24-4

规格	价格/CNY	货期
1 mg	￥ 398	现货
2 mg	￥ 578	现货
5 mg	￥ 788	现货
10 mg	￥ 1,330	现货
25 mg	￥ 2,430	现货
50 mg	￥ 3,930	现货
100 mg	￥ 5,590	现货
200 mg	￥ 7,690	现货

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其他形式的 LDN193189:

选择批次

纯度: 99.86%

纯度: 99.11%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).
靶点活性	ALK3:30 nM (C2C12 cells), ALK2:5 nM (C2C12 cells)
体外活性	LDN-193189 inhibited BMP4-mediated Smad1, Smad5 and Smad8 activation (IC50: 5 nM). LDN-193189 efficiently inhibited the transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50s: 5/30 nM), with substantially weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50 ≥ 500 nM). LDN-193189 inhibited the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation [1]. Treatment of human aortic endothelial cells with LDN-193189 abrogated the production of reactive oxygen species induced by oxidized LDL. Treatment of mice with LDN-193189 lowered LDL serum cholesterol by 35% and markedly decreased hepatosteatosis without inhibiting HMG-CoA reductase activity. Treatment with BMP2 increased, whereas LDN-193189 inhibited apolipoprotein B100 secretion in HepG2 cells [2].
体内活性	Treatment of Ad.Cre-injected, caALK2-expressing mice with LDN-193189 (3 mg/kg i.p. every 12 h) prevented radiographic lesions at P15 in all mice examined. At P30, LDN-193189 prevented ectopic bone in approximately two-thirds of mice and attenuated lesions in the remainder, whereas at P60 LDN-193189 prevented ectopic bone in one-third of mice and attenuated lesions in the remainder. In contrast to vehicle-treated mice, LDN-193189–treated mice appeared to preserve knee and ankle joints at P30 and P60 [1]. Prolonged treatment of LDLR-/- mice with LDN-193189 was well-tolerated and potently inhibited development of atheroma, as well as associated vascular inflammation, osteogenic activity, and calcification [2]. Treatment of SCID mice bearing MDA-PCa-118b tumors with LDN-193189 significantly reduced tumor growth [3].
细胞实验	C2C12 cells were seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. We treated the wells in quadruplicate with BMP ligands and LDN-193189 or vehicle. We collected the cells after 6 d in culture in 50 μl Tris-buffered saline and 1% Triton X-100. We added the lysates to p-nitro-phenylphosphate reagent in 96-well plates for 1 h and then evaluated alkaline phosphatase activity (absorbance at 405 nm). We measured cell viability and quantity by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements [1].
动物实验	In the first experiment, SCID mice were implanted with MDA-PCa-118b tumors. After 7 days when tumors reached measurable sizes, mice were injected with LDN-193189 (3 mg/kg) or with vehicle intraperitoneally twice a day. Tumor sizes and body weights were measured weekly. Mice were injected with calcein at three days and one day prior to sacrifice. Blood was collected and tumors were weighed. A portion of the tumors were fixed in formaldehyde for micro-computed tomography, using EVS CT, or further decalcified for bone histomorphometric analysis, using the OsteoMeasure Analysis System, or flash frozen for RNA preparation. Osteocalcin in the mouse serum was determined by ELISA. In the second experiment, PCa-118b tumors were first digested with Accumax, and the isolated cells were plated overnight, digested by Accutase, resuspended in Matrigel in 1:1 ratio, and injected into SCID mice (1 × 10^6 cells/mouse) subcutaneously. Mice were treated with LDN-193189 five days post-injection [3].

别名	LDN-193189, DM-3189, LDN 193189
分子量	406.48
分子式	C25H22N6
CAS No.	1062368-24-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 1.45mg/ml(3.56mM), when pH is adjusted to 2 with HCl. Sonification is recommended.

0.01M HCL: 1.67mg/ml（4.1mM）

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / 0.01M HCL	1 mM	2.4601 mL	12.3007 mL	24.6015 mL	61.5036 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369. 2. Derwall M, et al. Inhibition of bone morphogenetic protein signaling reduces vascular calcification and atherosclerosis. Arterioscler Thromb Vasc Biol. 2012 Mar;32(3):613-22. 3. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.

文献引用

1. Zhang H, Chen C, Liu Y, et al. NRF-2/HO-1 Pathway-Mediated SHOX2 Activation Is a Key Switch for Heart Rate Acceleration by Yixin-Fumai Granules. Oxidative Medicine and Cellular Longevity. 2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LDN193189 1062368-24-4 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad LDN-193189 Inhibitor Transforming growth factor beta receptors DM-3189 LDN 193189 inhibit DM3189 DM 3189 TGF-β Receptor inhibitor

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LDN193189

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

剂量换算

体内实验配液计算器

技术支持

Keywords