LDN-193189

Catalog No.S2618 Batch:S261804

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Technical Data

Formula

C25H22N6
Molecular Weight 406.48 CAS No. 1062368-24-4
Solubility (25°C)* In vitro 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.
* 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) 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 cell testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
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]

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.
Cell Assay:

[1]
  • Cell lines

    PASMCs 

  • Concentrations

    5 nM

  • Incubation Time

    12 h

  • Method

    Cells were treated with various concnetrations of LDN-193189.
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 [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]

Data from [Data independently produced by , , Oncol Rep, 2017, 37(2):713-720]

Selleck's LDN-193189 has been cited by 261 publications

Small extracellular vesicles derived from human induced pluripotent stem cell-differentiated neural progenitor cells mitigate retinal ganglion cell degeneration in a mouse model of optic nerve injury [ Neural Regen Res, 2025, 20(2):587-597] PubMed: 38819069
Distinct pathways drive anterior hypoblast specification in the implanting human embryo [ Nat Cell Biol, 2024, 26(3):353-365] PubMed: 38443567
Tankyrase inhibition promotes endocrine commitment of hPSC-derived pancreatic progenitors [ Nat Commun, 2024, 15(1):8754] PubMed: 39384787
Mouse neural tube organoids self-organize floorplate through BMP-mediated cluster competition [ Dev Cell, 2024, S1534-5807(24)00297-1] PubMed: 38776925
CGG repeats in the human FMR1 gene regulate mRNA localization and cellular stress in developing neurons [ Cell Rep, 2024, 43(6):114330] PubMed: 38865241
Parent-of-origin-specific DNA replication timing is confined to large imprinted regions [ Cell Rep, 2024, 43(9):114700] PubMed: 39235941
The chromodomain protein CDYL confers forebrain identity to human cortical organoids by inhibiting neuronatin [ Cell Rep, 2024, 43(10):114814] PubMed: 39378153
Incomplete reprogramming of DNA replication timing in induced pluripotent stem cells [ Cell Rep, 2024, 43(1):113664] PubMed: 38194345
A novel gene-trap line reveals the dynamic patterns and essential roles of cysteine and glycine-rich protein 3 in zebrafish heart development and regeneration [ Cell Mol Life Sci, 2024, 81(1):158] PubMed: 38556571
A novel gene-trap line reveals the dynamic patterns and essential roles of cysteine and glycine-rich protein 3 in zebrafish heart development and regeneration [ Cell Mol Life Sci, 2024, 81(1):158.] PubMed: 38556571

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.