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LDN-193189 HCl

LDN-193189 HCl (LDN193189 Hydrochloride) 是一种选择性 BMP I 型受体激酶抑制剂。

CAS号

1062368-62-0

分子式

C25H22N6·HCl

主要靶点

ALK

仅限科研使用

Cat No : CM06625

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Synonyms

LDN193189 Hydrochloride

验证数据展示

  • CAS No.: 1062368-62-0

    LDN-193189 HCl
    CAS#: 1062368-62-0

产品信息

LDN193189 hydrochloride is a selective BMP type I receptor kinases inhibitor.

CAS号 1062368-62-0
分子式 C25H22N6·HCl
主要靶点 ALK
主要通路 血管生成|蛋白酪氨酸激酶
分子量 442.94
纯度 99.94%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LDN193189 Hydrochloride

靶点活性

ALK6:16.7 nM|ALK1:0.8 nM|ALK3:5.3nM|ALK2:0.8nM

体内活性

In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. [1] LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2] In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3] In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. [4]

体外活性

LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. [1] A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. [4]

溶解度

DMSO:10 mg/mL (22.58 mM),Sonification is recommended.

细胞实验

Concentrations: 3 μM

参考文献

1.Yu PB, et al. Nat Med, 2008, 14(12), 1363-1369.
2.Cannon JE, et al. Br J Pharmacol, 2010, 161(1), 140-149.
3.Lee YC, et al. Cancer Res, 2011, 71(15), 5194-5203.
4.Derwall M, et al. Arterioscler Thromb Vasc Biol, 2012, 32(3), 613-622.

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