LDN-193189

ArtNr	S2618-5
Hersteller	Selleckchem
CAS-Nr.	1062368-24-4
Menge	5 mg
Kategorie	Neuroscience Metabolism Glucose Homeostasis Cholesterol & Lipid Metabolism Molecular Targets for Neuroscience Targets for Rodent Neurosciences Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	DM3189
Similar products	LDN193189
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Administration	Administered via i.p.
Animal Models	Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
Chemical Name	4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1, 5-a]pyrimidin-3-yl)quinoline
Description	LDN193189 is a selective inhibitor of ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.
Dosages	<=3 mg/kg
Formulation	LDN193189 is dissolved in DMSO and then diluted in water.
IC50	5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1]
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 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]
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]
Kinase Assay	Alkaline phosphatase activity, 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 uL 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.
Molecular Weight (MW)	406, 48
Picture ChemicalStructure Description	LDN193189 Chemical Structure
Solubility (25C)	DMSO <1 mg/mL, Water 26 mg/mL, Ethanol <1 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Menge: 5 mg

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