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抑制剂/激活剂

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凋亡与自噬

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LDN193189 DM-3189

LDN193189 (DM-3189) 是一种选择性的 BMP I 型受体抑制剂，抑制 ALK2 和 ALK3 的 IC50 分别为 5 nM 和 30 nM。对 ALK4，ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。

货号：
TK0486
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1062368-24-4
分子式	C25H22N6
分子量	406.48
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	Ethanol : 1 mg/mL (2.46 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
体内研究	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 (1×10 cells 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. 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.
体外研究	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 (IC50 for 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. LDN-193189 blocks the transcriptional activity induced by either constitutively active ALK2 or ALK2 mutant 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.
文献	•Eur Respir J. 2021 Dec 2;2100327. •Biomaterials. 2020 May;240:119849. •Diabetes. 2020 Apr;69(4):634-646. •Cell Rep. 2017 Aug 29;20(9):2227-2237. •Cell Rep. 2017 Aug 29;20(9):2227-2237. •Cancer Lett. 2020 Jan 28;469:390-398. •Stem Cell Res Ther. 2021 Jun 11;12(1):345. •Front Cell Dev Biol. 13 May 2021. •Oxid Med Cell Longev. 2020 Jun 8;2020:4175613. •iScience. 2019 Sep 27;19:1248-1259. •Front Mol Biosci. 2021 Apr 26;8:663987. •Front Mol Biosci. 2021; 8: 663987. •Transl Oncol. 2019 Dec 19;13(2):125-134 •Prostate. 2021 Sep 23. •Biochim Biophys Acta Gen Subj. 29 October 2021, 130046. •Exp Ther Med. 2019 Apr;17(4):2648-2656. •Cardiovasc Toxicol. 2019 Jun;19(3):264-275. •J Recept Signal Transduct Res. 2017 Oct;37(5):515-521. •Research Square Preprint. 2021 Sep. •Curr Protoc Cell Biol. 2018 Dec;81(1):e62. •Patent. US20180263995A1. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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