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抑制剂/激活剂

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凋亡与自噬

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LY-364947 HTS466284

LY-364947 (HTS466284) 是一种有效的，ATP 竞争性的 TGFβR-I 抑制剂，IC50 值为 59 nM，是对 TGFβR-II 选择性的 7 倍。

货号：
TK0490
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	396129-53-6
生物活性	LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
分子式	C17H12N4
分子量	272.30
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	DMSO : 25 mg/mL (91.81 mM; Need ultrasonic and warming)
体内研究	LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.
体外研究	LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells.
文献	•Oncogene. 2019 Jun;38(23):4637-4654. •Pharmacol Res. 2021 Aug 2;105797. •Cell Biosci. 2019 Jun 14;9:48. •Haematologica. 2020 Mar;105(3):674-686. •J Cell Physiol. 2019 May;234(5):6263-6273. •World J Gastroenterol. 2017 Apr 7;23(13):2330-2336. •Biochem Biophys Res Commun. 2020 Jan 29;522(1):270-277. •Eur Rev Med Pharmacol Sci. 2017 Apr;21(7):1551-1558. •J Cosmet Dermatol. 2021 Jul;20(7):2287-2295. •Int J Clin Exp Pathol 2018;11(12):5592-5601 •Research Square Preprint. 2021 Nov.
纯度及产品资料	98%

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