[CAS NO. 1062368-24-4] LDN-193189

Name: LDN-193189
Brand: Arctom Scientific
SKU: SLK-S2618

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PRODUCTS SPECIFICATIONS [1062368-24-4]

Store

Catalog

SLK-S2618

Brand

Selleck

CAS

1062368-24-4

DESCRIPTION [1062368-24-4]

Overview

MDL	MFCD17392570
Molecular Weight	406.48
Molecular Formula	C25H22N6
SMILES	C1(=C2N(N=C1)C=C(C=N2)C3=CC=C(C=C3)N4CCNCC4)C=5C6=C(N=CC5)C=CC=C6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the , , and 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 animal testing, the water-soluble 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 ALK2 or ALK2 mutant proteins. 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.

References

[1] Yu PB, et al. Nat Med, 2008, 14(12), 1363-1369.
[2] Cannon JE, et al. Br J Pharmacol, 2010, 161(1), 140-149.
[3] Lee YC, et al. Cancer Res, 2011, 71(15), 5194-5203.
[4] Derwall M, et al. Arterioscler Thromb Vasc Biol, 2012, 32(3), 613-622.
[5] Caroline E Sanvitale, et al. PLoS One. 2013 Apr 30;8(4):e62721.

Synonyms

Quinoline, 4-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-

4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline

LDN 193189

DM 3189