Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LDN-193189 2HCl (DM-3189 2HCl) 是一种选择性 BMP 信号抑制剂,对ALK1,ALK2,ALK3和ALK6有抑制作用,在激酶实验中显示的 IC50 分别为 0.8 nM、0.8 nM、5.3 nM 和 16.7 nM。LDN-193189 2HCl 在C2C12细胞中对BMP I 型受体ALK2和ALK3的转录活性有抑制作用,IC50分别为5 nM 和30 nM,作用于BMP 比作用于TGF-β选择性高200倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 329 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,720 | 现货 | ||
50 mg | ¥ 4,990 | 现货 | ||
100 mg | ¥ 6,880 | 现货 | ||
500 mg | ¥ 13,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 939 | 现货 |
产品描述 | LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β. |
靶点活性 | ALK1 (cell-free assay):0.8 nM, ALK2 (cell-free assay):0.8 nM, ALK3 (cell-free assay):5.3 nM, ALK6 (cell-free assay):16.7 nM |
体外活性 |
LDN193189 can effectively inhibit BMP4-mediated activation of Smad1, Smad5, and Smad8, with IC50 of 5 nM. It can also effectively inhibit the transcriptional activity of BMP type I receptors ALK2 and ALK3, with IC50 of 5 nM and 30 nM, respectively. LDN193189 also has an inhibitory effect on transcriptional activation induced by persistently activated ALK2R206H or ALK2Q207D mutant proteins.[1] A recent study showed that LDN-193189 blocks the production of oxidative free radicals induced by oxidized LDL in human arterial endothelial cells.[4] |
体内活性 |
LDN-193189 (3 mg/kg, intraperitoneal injection; birth in conditional caALK2) caused weak calcification of the left tibia and fibula, which was visible on day 13 and blocked on day 15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density, or abnormal behavior.[1] LDN193189 forms curved Zebrafish embryos by inhibiting the signal pathway induced by bone morphogenetic protein (BMP) 6 and has no effect on vascular development.[2] In mice with PCa-118b tumors, LDN-193189 treatment slowed down tumor growth and reduced bone formation in the tumor.[3] In LDLR -/- mice, LDN-193189 inhibited the development of arterial atherosclerosis. In addition, LDN-193189 has inhibitory effects on vascular inflammation, osteogenic activity, and calcification.[4] |
别名 | LDN-193189 2HCl, DM-3189 2HCl |
分子量 | 479.4 |
分子式 | C25H24Cl2N6 |
CAS No. | 1435934-00-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9.0 mg/mL (18.8 mM)
H2O: 45.0 mg/mL (93.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.0859 mL | 10.4297 mL | 20.8594 mL | 52.1485 mL |
5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL | 10.4297 mL | |
10 mM | 0.2086 mL | 1.043 mL | 2.0859 mL | 5.2149 mL | |
H2O | 20 mM | 0.1043 mL | 0.5215 mL | 1.043 mL | 2.6074 mL |
50 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.043 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
LDN-193189 2HCl 1435934-00-1 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad DM3189 DM-3189 DM 3189 LDN-193189 LDN 193189 LDN193189 DM-3189 2HCl Inhibitor inhibitor inhibit