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LDN193189 Tetrahydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDN193189 Tetrahydrochloride图片
CAS NO:2310134-98-4
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
LDN193189 Tetrahydrochloride 是一种选择性的BMPI 型受体抑制剂,抑制ALK2ALK3IC50分别为 5 nM 和 30 nM。对 ALK4,ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。
生物活性

LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibitsALK2andALK3(IC50=5 nM and 30 nM, respectively), with weaker effects onALK4,ALK5andALK7(IC50≥500 nM)[1].

IC50& Target[1]

ACVR1

5 nM (IC50)

BMPR1A

30 nM (IC50)

体外研究
(In Vitro)

LDN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with greater potency than did dorsomorphin (IC50=5 nM versus 470 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50for TGF-β ≥1,000 nM). LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound. LDN193189 blocks the transcriptional activity induced by either constitutively active ALK2R206Hor ALK2Q207Dmutant proteins. These findings suggest that LDN193189 might affect BMP-induced osteoblast differentiation. In fact, LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation, indicating sustained BMP signaling activity is needed for osteogenic differentiation[1].

体内研究
(In Vivo)

In the first experiment, LDN193189 (3 mg/kg) is injected intraperitoneally twice a day after tumors became palpable 7 days post-implantation. The growth rates between the control vehicle- and LDN193189-treated mice are not significantly different after the first 5 weeks, but differences in the growth rates are detected after 6 and 7 weeks post-treatment. In the second experiment, cells are isolated from PCa-118b tumors and injected subcutaneously into SCID mice (1×106cells per mouse). LDN193189 or vehicle is applied to mice 5 days post-tumor cell injection before tumors are palpable. The differences in the average growth rates between these two groups, as measured by tumor size, are significant at 6 and 7 weeks post-treatment. The tumor weights also show significant differences at the termination of the study at week 7. The X-ray of the tumors shows that the ectopic bone volume and bone density are reduced in the tumors of LDN193189-treated group compared to that of controls[2]. Co-incubation of pulmonary arterial smooth muscle cells (PASMCs) from the pulmonary arterial hypertension (PAH) rats with UK-92480 and LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression by the UK-92480[3].

分子量

552.33

性状

Solid

Formula

C25H26Cl4N6

CAS 号

2310134-98-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 33.33 mg/mL(60.34 mM;Need ultrasonic)

DMSO : 4.17 mg/mL(7.55 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8105 mL9.0526 mL18.1051 mL
5 mM0.3621 mL1.8105 mL3.6210 mL
10 mM0.1811 mL0.9053 mL1.8105 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。