LDN-193189 --- BMP inhibitor

LDN-193189 is a cell-permeable, highly potent and selective BMP pathway inhibitor by inhibiting BMP type I receptors ALK2 (IC50=5 nM) and ALK3 (IC50=30 nM), but not ALK4, ALK5, and ALK7 (> 0.5 µM). It prevents Smad1, Smad5, and Smad8 phosphorylation. It is a useful tool compound to modulate stem cell differentiation (for example, neural differentiation of human ESC/iPSC in combination with SB431542). It was also used in animal models to treat FOP and ectopic ossification, as well as NSCLC lung cancer.

Product information

CAS Number: 1062368-24-4

Molecular Weight: 406.48

Formula: C25H22N6

Related CAS Number:

1435934-00-1 (dihydrochloride)

1062368-62-0 (hydrochloride)

Chemical Name: 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

Smiles: C1CNCCN1C1C=CC(=CC=1)C1=CN2N=CC(=C2N=C1)C1=CC=NC2=CC=CC=C21

InChiKey: CDOVNWNANFFLFJ-UHFFFAOYSA-N

InChi: InChI=1S/C25H22N6/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

LDN-193189 is typically used at 0.1 µM final concentration in stem cell differentiation conditions.

In Vivo:

Intraperitoneal (IP) administration of 3 mg/kg LDN-193189 was used once or twice daily.

References:

1. Cuny GD, et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. (2008), Bioorg Med Chem Lett. 18(15):4388-92.
2. Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. (2008), Nature Med. 14: 1363-1369.
3. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. (2008), Nature Chem Biol. 4: 33-41.
4. Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. (2009), Nature Biotechnology 27, 275-280.
5. Boergermann JH, et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. (2010), Int J Biochem Cell Biol. 42(11):1802-7.
6. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. (2011), Cancer Res 71:5194-5203.
7. Najm FJ, et al. Rapid and robust generation of functional oligodendrocyte progenitor cells from epiblast stem cells. (2011) Nature Methods 8, 957–962

Products are for research use only. Not for human use.

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