LDN193189 | DM-3189 | ALK2/3 Inhibitor | AmBeed-信号通路专用抑制剂

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LDN193189 {[allProObj[0].p_purity_real_show]}

货号：A125436 同义名： DM-3189

LDN193189是一种有效的选择性BMP I型受体（BMP I）抑制剂，有效抑制BMP I型受体ALK2和ALK3的转录活性，IC50值分别为5 nM和30 nM。它用于研究骨形态发生蛋白信号传导，如进行性纤维发育性骨化症。

LDN193189 化学结构
CAS号：1062368-24-4

LDN193189 3D分子结构
CAS号：1062368-24-4

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LDN193189 纯度/质量文件产品仅供科研

货号：A125436 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

转化生长因子-β 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

LDN193189 生物活性

靶点	ALK1 ALK1, IC50:0.8 nM ALK2 ALK2, IC50:0.8 nM ALK6 ALK6, IC50:16.7 nM ALK3 ALK3, IC50:5.3 nM
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].

LDN193189 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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

LDN193189 动物研究

Dose

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

Administration

i.p., p.o.

Pharmacokinetics

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

LDN193189 参考文献

[1]Williams E, Bullock AN, et al. Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2. Bone. 2018 Apr;109:251-258.

[2]Yu PB, Deng DY, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9.

[3]Zhao J, Li S, et al. Small molecule-directed specification of sclerotome-like chondroprogenitors and induction of a somitic chondrogenesis program from embryonic stem cells. Development. 2014 Oct;141(20):3848-58.

[4]Myers CT, Krieg PA, et al. BMP-mediated specification of the erythroid lineage suppresses endothelial development in blood island precursors. Blood. 2013 Dec 5;122(24):3929-39.

[5]Derwall M, Malhotra R, et al. Inhibition of bone morphogenetic protein signaling reduces vascular calcification and atherosclerosis. Arterioscler Thromb Vasc Biol. 2012 Mar;32(3):613-22.

[6]Inubushi T, Nozawa S, et al. Aberrant perichondrial BMP signaling mediates multiple osteochondromagenesis in mice. JCI Insight. 2017 Aug 3;2(15). pii: 90049.

[7]Carvalho D, Taylor KR, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019 May 9;2:156.

[8]Cuny GD, Yu PB, et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4388-92.

LDN193189 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

LDN193189 技术信息

CAS号	1062368-24-4
分子式	C₂₅H₂₂N₆
分子量	406.482

别名	DM-3189
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 9 mg/mL(22.14 mM)，配合低频超声，水浴加热至45℃，并调节pH至2，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

PO 0.5% CMC-Na 38 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

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 {[allProObj[0].p_purity_real_show]}

LDN193189 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

LDN193189 质控信息

LDN193189 生物活性

LDN193189 细胞研究

LDN193189 动物研究

LDN193189 参考文献

LDN193189 实验方案

LDN193189 技术信息

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ALK1	ALK1, IC50:0.8 nM
ALK2	ALK2, IC50:0.8 nM
ALK6	ALK6, IC50:16.7 nM
ALK3	ALK3, IC50:5.3 nM

LDN193189 {[allProObj[0].p_purity_real_show]}

LDN193189 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

LDN193189 质控信息

LDN193189 生物活性

LDN193189 细胞研究

LDN193189 动物研究

LDN193189 参考文献

LDN193189 实验方案

LDN193189 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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LDN193189 纯度/质量文件产品仅供科研