1. Metabolic Enzyme/Protease
  2. MMP

GI254023X (Synonyms: GI4023; SRI028594)

目录号: HY-19956 纯度: 99.67%

GI254023X 是一种有效的 MMP9ADAM10 抑制剂, IC50s 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 ¥2024 In-stock
1 mg ¥1200 In-stock
5 mg ¥2350 In-stock
10 mg   Get quote  
50 mg   Get quote  

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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]

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].

Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility


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

Purity: 99.67%


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