LDN-193189

製品コードS2618 バッチS261804

化学情報

	Synonyms	DM3189	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₅H₂₂N₆
	分子量	406.48	CAS No.	1062368-24-4
Solubility (25°C)*	体外	0.01M HCl	2.5 mg/mL (6.15 mM)
		DMSO	Insoluble
		Water	Insoluble
* <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) 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. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
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, this compound 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 this chemical 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] This compound 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, this chemical treatment attenuates tumor growth and reduces bone formation in the tumors. ^[3] In LDL receptor-deficient (LDLR-/-) mice, this agent potently inhibits development of atheroma. Moreover, it also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. ^[4]

製品説明

LDN-193189 (DM3189) 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. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

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, this compound 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 this chemical 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]

This compound 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, this chemical treatment attenuates tumor growth and reduces bone formation in the tumors. ^[3]

In LDL receptor-deficient (LDLR-/-) mice, this agent potently inhibits development of atheroma. Moreover, it also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. ^[4]

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	PASMCs
	濃度	5 nM
	反応時間	12 h
	実験の流れ	Cells were treated with various concnetrations of LDN-193189.
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/

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カスタマーフィードバック

: Data from [Int J Cancer, 2014, 136(5):E455-69]

: Data from [Dev Biol, 2014, 378:107-121]

: Data from [Data independently produced by , , J Cell Sci, 2013, 126: 234-43]

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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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