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LDN-193189 2HCl

Catalog No. T35348 CAS 1435934-00-1

Synonyms: LDN-193189 2HCl, DM-3189 2HCl

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.

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LDN-193189 2HCl, CAS 1435934-00-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 67.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 237.00
100 mg	In stock	$ 353.00
500 mg	In stock	$ 837.00
1 mL * 10 mM (in DMSO)	In stock	$ 80.00

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Purity: 99.78%

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Description	LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.
Targets&IC50	ALK1 (cell-free assay):0.8 nM, ALK2 (cell-free assay):0.8 nM, ALK3 (cell-free assay):5.3 nM, ALK6 (cell-free assay):16.7 nM
In vitro	LDN193189 can effectively inhibit BMP4-mediated activation of Smad1, Smad5, and Smad8, with IC50 of 5 nM. It can also effectively inhibit the transcriptional activity of BMP type I receptors ALK2 and ALK3, with IC50 of 5 nM and 30 nM, respectively. LDN193189 also has an inhibitory effect on transcriptional activation induced by persistently activated ALK2R206H or ALK2Q207D mutant proteins.[1] A recent study showed that LDN-193189 blocks the production of oxidative free radicals induced by oxidized LDL in human arterial endothelial cells.[4]
In vivo	LDN-193189 (3 mg/kg, intraperitoneal injection; birth in conditional caALK2) caused weak calcification of the left tibia and fibula, which was visible on day 13 and blocked on day 15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density, or abnormal behavior.[1] LDN193189 forms curved Zebrafish embryos by inhibiting the signal pathway induced by bone morphogenetic protein (BMP) 6 and has no effect on vascular development.[2] In mice with PCa-118b tumors, LDN-193189 treatment slowed down tumor growth and reduced bone formation in the tumor.[3] In LDLR -/- mice, LDN-193189 inhibited the development of arterial atherosclerosis. In addition, LDN-193189 has inhibitory effects on vascular inflammation, osteogenic activity, and calcification.[4]

Synonyms	LDN-193189 2HCl, DM-3189 2HCl
Molecular Weight	479.4
Formula	C25H24Cl2N6
CAS No.	1435934-00-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 9.0 mg/mL (18.8 mM)

H2O: 45.0 mg/mL (93.9 mM)

References and Literature

1. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification [published correction appears in Nat Med. Nat Med. 2008;14(12):1363-1369. 2. Cannon JE, et al. Intersegmental vessel formation in zebrafish: requirement for VEGF but not BMP signalling revealed by selective and non-selective BMP antagonists. Br J Pharmacol. 2010;161(1):140-149. 3. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res. 2011;71(15):5194-520 4. Derwall M, et al. Inhibition of bone morphogenetic protein signaling reduces vascular calcification and atherosclerosis. Arterioscler Thromb Vasc Biol. 2012;32(3):613-622. 5. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013;8(4):e62721.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library

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Keywords

LDN-193189 2HCl 1435934-00-1 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad DM3189 DM-3189 DM 3189 LDN-193189 LDN 193189 LDN193189 DM-3189 2HCl inhibitor inhibit

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