[CAS NO. 1435934-00-1] LDN-193189 2HCl

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PRODUCTS SPECIFICATIONS [1435934-00-1]

Catalog

SLK-S7507

Brand

Selleck

CAS

1435934-00-1

DESCRIPTION [1435934-00-1]

Overview

MDL	MFCD23098917
Molecular Weight	479.4
Molecular Formula	C25H24Cl2N6
SMILES	[H]Cl.[H]Cl.C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16

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.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0859 mL	10.4297 mL	20.8594 mL
5 mM	0.4172 mL	2.0859 mL	4.1719 mL
10 mM	0.2086 mL	1.0430 mL	2.0859 mL
50 mM	0.0417 mL	0.2086 mL	0.4172 mL

Description

LDN-193189 (DM3189) 2HCl 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.

Features

Selective BMP type I receptor inhibitor.

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.
[6] Sanvitale CE, et al. PLoS One. 2013 Apr 30;8(4):e62721.