Grp94 Inhibitor-1
目录号: PL02132 纯度: ≥98%
CAS No. :2234897-35-7
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中文名称
Grp94 Inhibitor-1
英文名称
Grp94 Inhibitor-1
英文别名
Grp94 Inhibitor-1;Grp94 inhibitor 54;GTPL10118;4'-(propan-2-yl)-4-{[(1r,4r)-4-hydroxycyclohexyl]amino}-[1,1'-biphenyl]-3-carboxamide;rel-4-(((1R,4R)-4-hydroxycyclohexyl)amino)-4'-isopropyl-[1,1'-biphenyl]-3-carboxamide
Cas No.
2234897-35-7
分子式
C22H28N2O2
分子量
352.47
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Grp94 Inhibitor-1 是一种有效的、选择性的 Grp94 抑制剂,IC50 值为 2 nM,对 Grp94 的抑制作用是 Hsp90α 的 1000 倍。
生物活性
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC 50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
性状
Solid
IC50 & Target[1][2]
GRP94 2 nM (IC50)
体外研究(In Vitro)
Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α.
Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Jiang F, et al. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018 Nov 8;61(21):9513-9533.
溶解度数据
In Vitro: DMSO : 250 mg/mL (709.28 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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