上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
GI254023X (Synonyms: GI4023; SRI028594) 纯度: 99.84%
GI254023X 是一种有效的 MMP9 和 ADAM10 抑制剂, IC50s 分别为 2.5 和 5.3 nM。
GI254023X Chemical Structure
CAS No. : 260264-93-5
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1 mg | ¥1200 | In-stock | |
5 mg | ¥1780 | In-stock | |
10 mg | ¥2400 | In-stock | |
25 mg | ¥4600 | In-stock | |
50 mg | ¥7200 | In-stock | |
100 mg | ¥11500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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GI254023X 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Metabolism/Protease Compound Library
- Anti-Cancer Compound Library
- Differentiation Inducing Compound Library
- Anti-Pancreatic Cancer Compound Library
- Angiogenesis Related Compound Library
生物活性 |
GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively. |
IC50 & Target |
IC50: 2.5 nM (MMP9), 5.3 nM (ADAM10)[1] |
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体外研究 (In Vitro) |
In cellular assay 25 µM and even a concentration of 1 µM GI254023X strongly reduces constitutive RAGE shedding; 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 ADAM protease inhibitors (e.g GI254023x). A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM-10-selective inhibitor GI254023x, as the level of expressed ADAM-10 is on average 9.8-fold higher on mRNA level compare with ADAM-17. 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
391.50 |
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Formula |
C21H33N3O4 |
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CAS 号 |
260264-93-5 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (255.43 mM; Need ultrasonic) 配制储备液
*
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请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [3] |
Cell death is quantified based on plasma membrane permeabilization. When apply the ADAM10 (a-secretase) inhibitor GI254023X (5 mM), slices are cultured in serum-/glucose-free medium for 48 h containing the inhibitor or its respective carrier (DMSO) as control. Round circles of identical size (Ø 500mm) are positioned in equivalent locations within the CA1 region of each hippocampus image and all PI-stained cells are counted using 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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