LDN-193189 2HCl

Catalog No.S7507 Batch:S750705

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Technical Data

Formula

C25H24Cl2N6
Molecular Weight 479.4 CAS No. 1435934-00-1
Solubility (25°C)* In vitro DMSO 24 mg/mL (50.06 mM)
Water 24 mg/mL (50.06 mM)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
ALK1 [5]
(Cell-free assay)		 ALK2 [5]
(Cell-free assay)		 ALK3 [5]
(Cell-free assay)		 ALK6 [5]
(Cell-free assay)
0.8 nM 0.8 nM 5.3 nM 16.7 nM
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]
Features Selective BMP type I receptor inhibitor.

Protocol (from reference)

Kinase Assay:

[1]
  • 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 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.
Animal Study:

[1]
  • Animal Models

    Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.

  • Dosages

    ≤3 mg/kg

  • Administration

    Administered via i.p.

Customer Product Validation

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]

Selleck's LDN-193189 2HCl has been cited by 99 publications

A noncoding variant confers pancreatic differentiation defect and contributes to diabetes susceptibility by recruiting RXRA [ Nat Commun, 2024, 15(1):9771] PubMed: 39532884
Dissecting peri-implantation development using cultured human embryos and embryo-like assembloids [ Cell Res, 2023, 10.1038/s41422-023-00846-8] PubMed: 37460804
Electrical stimulation affects the differentiation of transplanted regionally specific human spinal neural progenitor cells (sNPCs) after chronic spinal cord injury [ Stem Cell Res Ther, 2023, 14(1):378] PubMed: 38124191
Proteomics and disease network associations evaluation of environmentally relevant Bisphenol A concentrations in a human 3D neural stem cell model [ Front Cell Dev Biol, 2023, 11:1236243] PubMed: 37664457
Proteomics and disease network associations evaluation of environmentally relevant Bisphenol A concentrations in a human 3D neural stem cell model [ Front Cell Dev Biol, 2023, 11:1236243] PubMed: 37664457
Accelerated differentiation of human induced pluripotent stem cells into regionally specific dorsal and ventral spinal neural progenitor cells for application in spinal cord therapeutics [ Front Neurosci, 2023, 17:1251906] PubMed: 37781243
Accelerated differentiation of human induced pluripotent stem cells into regionally specific dorsal and ventral spinal neural progenitor cells for application in spinal cord therapeutics [ Front Neurosci, 2023, 17:1251906] PubMed: 37781243
Generating Neural Retina from Human Pluripotent Stem Cells [ J Vis Exp, 2023, (202).] PubMed: 38189566
Primate gastrulation and early organogenesis at single-cell resolution [ Nature, 2022, 612(7941):732-738] PubMed: 36517595
Stretchable Mesh Nanoelectronics for Three-Dimensional Single-Cell Chronic Electrophysiology from Developing Brain Organoids [ Adv Mater, 2022, e2106829] PubMed: 35014735

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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