1. Metabolic Enzyme/Protease
  2. MMP

GI254023X (Synonyms: GI4023; SRI028594)

目录号: HY-19956 纯度: 99.67%
Data Sheet SDS 产品使用指南

GI254023X 是一种有效的MMP9ADAM10 抑制剂, IC50 分别为 2.5 和 5.3 nM。

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GI254023X Chemical Structure

GI254023X Chemical Structure

CAS No. : 260264-93-5

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥2585 In-stock
5 mg ¥2350 In-stock
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Description

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50 of 2.5 and 5.3 nM, respectively.

IC50 & Target

IC50: 2.5 nM (MMP9), 5.3 nM (ADAM10)[1]

In Vitro

In cellular assay 25 µM and even a concentration of 1 µM GI254023X strongly reduced constitutive RAGE shedding; also PACAP-induced 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 compared with ADAM-17. In addition, GI254023x also prevents CXCL16 shedding from the cell membrane and is even more potent than TAPI-2[2]. When applying the specific ADAM10 (α-secretase) inhibitor GI254023X (5 mM) to serum/glucose-deprived slices, PI counts are significantly increased in comparison with DSMO (carrier)-treated controls[3].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.5543 mL 12.7714 mL 25.5428 mL
5 mM 0.5109 mL 2.5543 mL 5.1086 mL
10 mM 0.2554 mL 1.2771 mL 2.5543 mL
Kinase Assay
[3]

Cell cultures are pre-treated with 10–50 nM yeast-derived sAPPa/E1 or 20 nM human IGF1 for 24 h before removal of glucose and/or serum. During starvation for 24–48 h, the same treatments are administered. IGF1 is added every 24 h owing to its short half-life. In the experiment using PTX, 100 μM of the toxin is applied 30 min before sAPPa is added to the medium. Akt kinase activity is measured in vitro with a commercial kit according to the manufacturer’s protocol. Briefly, endogenous levels of pAkt are immunoprecipitated from whole-cell extracts with immobilized pAkt (Ser473) mAb (bead conjugate) overnight. After extensive washing, the kinase assay is performed using 10mM ATP and GSK3 fusion protein (27 kDa) as a substrate. Subsequent inactivation of GSK3 is measured by western blot detecting pGSK3a/b (Ser 21/9, 27 kDa)[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[3]

Cell death is quantified based on plasma membrane permeabilization. When applying 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 ImageJ 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, we applied the live-dead cell staining kit 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

391.5

Formula

C₂₁H₃₃N₃O₄

CAS No.

260264-93-5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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产品名称:
GI254023X
目录号:
HY-19956
需求量: