LDN-193189 Dihydrochloride

製品コードS7507 バッチS750707

印刷

化学情報

Synonyms

DM-3189 2HCl

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₂₄Cl₂N₆

分子量

479.4

CAS No.

1435934-00-1

Solubility (25°C)*

体外

Water

24 mg/mL (50.06 mM)

DMSO

6 mg/mL (12.51 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
in vitro	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 ALK2^R206H or ALK2^Q207D 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]
in vivo	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]
特徴	Selective BMP type I receptor inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ	Alkaline phosphatase activity
キナーゼアッセイ	C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 days in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 hours and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability and quantity are measured by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements.
細胞アッセイ	細胞株	Cell-free assays
	濃度	0.8, 0.8, 5.3 and 16.7 nM (IC50) for ALK1, ALK2, ALK3 and ALK6, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
	投薬量	≤3 mg/kg
	投与方法	Administered via i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/19029982/
https://pubmed.ncbi.nlm.nih.gov/20718746/
https://pubmed.ncbi.nlm.nih.gov/21670081/

https://pubmed.ncbi.nlm.nih.gov/22223731/
https://pubmed.ncbi.nlm.nih.gov/23646137/
https://pubmed.ncbi.nlm.nih.gov/23646137/

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カスタマーフィードバック

: Data from [Data independently produced by Int J Cancer, 2014, 10.1002/ijc.29220]

: Data independently produced by , 2014, 378:107-121

: Data from [Data independently produced by , , RSC Adv, 2018, doi:10.1039/C8RA00750K]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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