LDN-193189

製品コードS2618 バッチS261805

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	DMSO	Insoluble
		Water	Insoluble
		Ethanol	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, 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]

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, 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]

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

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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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Distinct pathways drive anterior hypoblast specification in the implanting human embryo [ Nat Cell Biol, 2024, 26(3):353-365]	PubMed: 38443567
Shear Stress and Sub-Femtomolar Levels of Ligand Synergize to Activate ALK1 Signaling in Endothelial Cells [ Cells, 2024, 13(3)285]	PubMed: 38334677
Host-to-graft propagation of inoculated α-synuclein into transplanted human induced pluripotent stem cell-derived midbrain dopaminergic neurons [ Regen Ther, 2024, 25:229-237]	PubMed: 38283940
Generation of a control iPS cell line (JUCGRMi005-A) with no abnormalities in Parkinson's disease-related genes [ Stem Cell Res, 2024, 74:103271]	PubMed: 38100917
Generation of three clones (JUCGRMi002-A, B, C) of induced pluripotent stem cells from a Parkinson's disease patient with SNCA duplication [ Stem Cell Res, 2024, 74:103296]	PubMed: 38154385
Elevated levels of FMRP-target MAP1B impair human and mouse neuronal development and mouse social behaviors via autophagy pathway [ Nat Commun, 2023, 14(1):3801]	PubMed: 37365192
Time space and single-cell resolved tissue lineage trajectories and laterality of body plan at gastrulation [ Nat Commun, 2023, 14(1):5675]	PubMed: 37709743
Time space and single-cell resolved tissue lineage trajectories and laterality of body plan at gastrulation [ Nat Commun, 2023, 14(1):5675]	PubMed: 37709743
Generation of human otic neuronal organoids using pluripotent stem cells [ Cell Prolif, 2023, 56(5):e13434]	PubMed: 36825797
Photo-click hydrogels for 3D in situ differentiation of pancreatic progenitors from induced pluripotent stem cells [ Stem Cell Res Ther, 2023, 14(1):223]	PubMed: 37649117

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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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