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GI254023X

产品编号 T7522 CAS 260264-93-5

别名: GI 254023X

GI254023X 是MMP9和ADAM10抑制剂，它们的IC50s 分别为 2.5 和 5.3 nM。

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GI254023X, CAS 260264-93-5

规格	价格/CNY	货期
1 mg	￥ 678	现货
2 mg	￥ 980	现货
5 mg	￥ 1,470	现货
10 mg	￥ 1,980	现货
25 mg	￥ 3,820	现货
50 mg	￥ 5,560	现货
100 mg	￥ 7,780	现货
1 mL * 10 mM (in DMSO)	￥ 1,620	现货

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纯度: 98.56%

纯度: 98.21%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GI254023X is a potent MMP9 and ADAM10 inhibitor (IC50s: 2.5 and 5.3 nM) with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells. Its mechanism may be associated with inbihition of Notch1 activation.
靶点活性	MMP9:2.5 nM (cell free), ADAM10:5.3 nM (cell free)
体外活性	In the cellular assay, GI254023X (1-25 μM) strongly reduces constitutive RAGE shedding and also PACAP-inducing shedding of RAGE is significantly reduced. At a concentration of 100 nM, a slight inhibition of RAGE shedding is still observed. In in vitro assays with recombinant proteinases, GI254023X discriminates between ADAM17 (IC50: 541 nM) and ADAM10 (IC50: 5.3 nM)/MMP9 (IC50: 2.5 nM) [1]. CXCL16 shedding is inhibited by GI254023x. A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM10-selective inhibitor GI254023x, as the level of expressed ADAM10, is on average 9.8-fold higher on mRNA level compare with ADAM17. In addition, GI254023x also prevents CXCL16 shedding from the cell membrane and is even more potent than TAPI-2[2]. When apply the specific ADAM10 (α-secretase) inhibitor GI254023X (5 mM) to serum/glucose-deprived slices, PI counts are significantly increased in comparison with DMSO (carrier)-treated controls [3].
体内活性	在AD小鼠模型中进行的急性GI254023X处理显著减少了大脑LRP1的剥落，并在血浆中增加了Aβ40水平，这表明从大脑到外围的Aβ转运得到了增强[4]。
细胞实验	Cell death is quantified based on plasma membrane permeabilization. When applying the ADAM10 (a-secretase) inhibitor GI254023X (5 mM), slices are cultured in the serum-/glucose-free medium for 48 h containing the inhibitor or its respective carrier (DMSO) as control. Round circles of identical size (? 500mm) are positioned in equivalent locations within the CA1 region of each hippocampus image and all PI-stained cells are counted using the software. Cell viability assays are performed with a commercial kit according to the manufacturer's instructions. The assay quantitates ATP levels, an indicator of metabolically active cells, photometrically with a fluorescence plate reader. Additionally, the live-dead cell staining kit are applied according to the manual. Cells are simultaneously stained with green fluorescent calcein-AM (4mM; ex/em: 495/515 nm) to detect intracellular esterase activity (viable cells) and red fluorescent ethidium homodimer-3 (2mM; ex/em: 530/635 nm) to indicate loss of plasma membrane integrity (dead cells) [3].

别名	GI 254023X
分子量	391.5
分子式	C21H33N3O4
CAS No.	260264-93-5

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (255.43 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5543 mL	12.7714 mL	25.5428 mL	63.857 mL
	5 mM	0.5109 mL	2.5543 mL	5.1086 mL	12.7714 mL
	10 mM	0.2554 mL	1.2771 mL	2.5543 mL	6.3857 mL
	20 mM	0.1277 mL	0.6386 mL	1.2771 mL	3.1928 mL
	50 mM	0.0511 mL	0.2554 mL	0.5109 mL	1.2771 mL
	100 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6386 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012. 2. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544. 3. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391. 4. Shackleton B, et al. Inhibition of ADAM10 promotes the clearance of Aβ across the BBB by reducing LRP1 ectodomain shedding. Fluids Barriers CNS. 2016 Aug 8;13(1):14.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GI254023X 260264-93-5 Immunology/Inflammation Proteases/Proteasome MMP Immunology/Inflammation related SRI 028594 SRI028594 GI 4023 inhibit GI-254023X Matrix metalloproteinases GI 254023X SRI-028594 Inhibitor GI4023 GI-4023 inhibitor

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GI254023X

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords