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CAS No.: 1062368-24-4

LDN193189 Catalog No. CSN13848

Synonyms: DM-3189

LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ALK2

IC50:5nM ALK3

IC50:30nM
描述BMPs (Bone morphogenetic proteins) represent the largest subgroup in the TGFβ family of extracellular ligands. Their signaling transduction requires the interaction with the type I and type II transmembrane receptor kinase. Type I receptors, such as ALK1/ACVRL1, ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B all participate in BMP signalling and phosphorylate SMAD1/5/ 8 phosphorylate SMAD family transcription factors. Dysregulation of this pathway links to many disease conditions, for example, fibrodysplasia ossificans progressive^[1]. LDN-193189 is a selective inhibitor of BMP type I receptors with IC50 values of 5 nM and 30 nM for ALK2 and ALK3 (measured by p-Smad1/5/8 in PASMCs), respectively, with substantially weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM). PASMCs treated with LDN-193189 on concentration at 2 - 250 nM showed dose-dependent inhibition on p-Smad1/5/8 induced by BMP4 (10 ng/ml), while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50≥1000 nM). Even LDN-193189 can block the transcriptional activity induced by either constitutively active ALK2^R206H or ALK2^Q207D mutant proteins. Intraperitoneal injection with LDN-193189 on dose of 3 mg/kg, every 12 h, resulted in a reduction in ectopic ossification and functional impairment in ALK2^Q207D mutant mice^[2]. Use of LDN-193189 combined with different small molecular led to the effective generation from ESCs of paraxial mesodermal progeny, and to their further differentiation in vitro through sclerotome specification into growth plate-like chondrocytes^[3]. Inhibition of BMP signaling by LDN-193189 can inhibit endothelial cell differentiation in the ventral blood island^[4].
作用机制LDN-193189 targets to the ATP-binding pocket located within the intracellular kinase domain of the receptors^[1].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A549	0.5-16 μM	Growth Inhibition Assay	-	inhibits cell growth in a dose-dependent manner	24778011
BEAS-2B	0.5-16 μM	Growth Inhibition Assay	-	inhibits cell growth in a dose-dependent manner	24778011
Bx-PC3	5-500 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	23969729

动物研究

剂量

Mice: 2.5 mg/kg^[5] (i.p.), 10 mg/kg^[6] (i.p.), max = 35 mg/kg^[7] (p.o.)

给药途径

i.p., p.o.

动物药代数据

Animal	Mice^[8]
Dose	3 mg/kg
Administration	i.p.
C_max	1.54 μM
T_1/2	1.6 h
AUC_∞	994 ng·h/ml
T_max	< 5 min

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4601 mL
- 12.3007 mL
- 24.6013 mL
- 5 mM
- 0.4920 mL
- 2.4601 mL
- 4.9203 mL
- 10 mM
- 0.2460 mL
- 1.2301 mL
- 2.4601 mL

技术信息

CAS号

1062368-24-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H22N6

运输

蓝冰

分子量

406.48

别名

DM-3189

溶解度

DMSO	insoluble
Water	insoluble
Ethanol	insoluble
DMF	insoluble

动物实验配方

0.5% CMC-Na

38 mg/mL

suspension

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A549	0.5-16 μM	Growth Inhibition Assay	-	inhibits cell growth in a dose-dependent manner	24778011
BEAS-2B	0.5-16 μM	Growth Inhibition Assay	-	inhibits cell growth in a dose-dependent manner	24778011
Bx-PC3	5-500 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	23969729
C2C12	-	Kinase Assay	-	inhibits the kinase activity of ALK4 and ActRIIA with IC50 values of 101 and 210 nm, respectively	25368322
EOC	10-1000 nM	Function Assay	72 h	reduces the phosphorylated BMP R-Smad1/5/8	22249415
EOC216	0.1-10 μM	Growth Inhibition Assay	2-10 d	induce cell death in a dose-dependent manner	25227893
EOC219	2/5 μM	Growth Inhibition Assay	48 h	decreases the percentage of cells in S phas	25227893
HaCaT	0.001-10 μM	Function Assay	2 h	inhibits BMP2-induced phosphorylation of Smad1/5/8 with an IC50 of ~0.005 μM	21740966
HaCaT	0.001-10 μM	Function Assay	2 h	inhibits the ability of ALK2 to phosphorylate GST-Smad1 with an IC50 of 45 nM	21740966
HaCaT	0.001-10 μM	Function Assay	2 h	inhibits the ability of ALK3 to phosphorylate Smad1 with an IC50 of 100 nM	21740966
HaCaT	0.001-10 μM	Function Assay	2 h	inhibits ALK4 and ALK5 with IC50 values of 0.3 μM and 0.5 μM respectively	21740966
hBMSCs	0.2 μM	Function Assay	7 d	abolishes the silibinin-promoted ALP activity partly	24076187
LNCaP	0–500 nM	Function Assay	2 h	reverses rapamycin-induced cell death	22452883
MIA PaCa-2	5-500 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	23969729
OVAC429	2/5 μM	Growth Inhibition Assay	48 h	decreases the percentage of cells in S phas	25227893
OVCA429	2/5 μM	Growth Inhibition Assay	48 h	decreases the percentage of cells in S phas	25227893
PANC-1	5-500 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	23969729
PC3	500 nM	Function Assay	2 h	represses activation of Smad1/5/8 and P-Smad3 levels	22452883
SKOV3	2/5 μM	Growth Inhibition Assay	48 h	decreases the percentage of cells in S phas	25227893

LDN193189 Catalog No. CSN13848

靶点选择性

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