Reagents and instruments for immunology, cell biology and molecular biology.

GI254023X [260264-93-5]

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Cat# NB-64-41786-5mg

Size : 5mg

Brand : Neo Biotech

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GI254023X

(Synonyms: GI 254023X) Copy Product Info

Synonyms: GI 254023X

Catalog No. T7522 Copy Product Info

Purity: 99.97%

GI254023X is a MMP9 and ADAM10 inhibitor with IC50 values of 2.5 and 5.3 nM, respectively. GI254023X can also significantly inhibit the proliferation of Jurkat cells and induce apoptosis.

Cas No. 260264-93-5

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.97%

Color:White to Red

Product Introduction

Bioactivity

Description	GI254023X is a MMP9 and ADAM10 inhibitor with IC50 values of 2.5 and 5.3 nM, respectively. GI254023X can also significantly inhibit the proliferation of Jurkat cells and induce apoptosis.
Targets & IC50	ADAM10:5.3 nM (cell free), MMP9:2.5 nM (cell free)
In vitro	METHODS: Mouse mesothelioma cells were treated with GI254023X (5 μM, 4, 24, 48, 72 hours), and the proliferation of AB12 and PM27 cells was measured by CYQUANT analysis; the percentage of AB12 or PM27 cells in different phases of the cell cycle (G1, S or G2) was measured by FACS analysis and wound healing assay was performed to study its effects on mesothelioma cell proliferation, migration and invasion. RESULTS GI254023X had no effect on the proliferation of either cell type; mouse mesothelioma cells treated with GI254023X showed weaker migration properties in transwell chambers; GI254023X showed a significant reduction in migration of mouse mesothelioma cells in the scratch assay (4, 6 and 8 hours); and the invasion of AB12 and PM27 cells measured in the spheroid assay was also significantly reduced. [3]
In vivo	METHODS: C57BL/6N mice were subjected to a controlled cortical impact (CCI) model of TBI or sham surgery and received GI254023X or vehicle (40, 100 mg/kg, intraperitoneal injection, 30 minutes and 24 hours after TBI) in the acute phase of injury. The expression of brain mRNA and some inflammatory factors was measured by quantitative PCR to study its effects on neurological and histopathological outcomes in mice after experimental traumatic brain injury (TBI). RESULTS GI254023X treatment did not improve neurological deficits from 1 to 7 days post-injury (DPI), but animals treated with GI254023X showed less brain damage compared with vehicle treatment. Brain mRNA expression measured by quantitative PCR showed that TBI-induced upregulation of Adam10 and Adam17 was not affected by GI254023X, but upregulation of matrix metalloproteinase genes Mmp2 and Mmp9 was attenuated; GI254023X also attenuated upregulation of proinflammatory markers Il6, Trfa, and Lcn2, but not pan-microglial marker Aif1, M2 microglial marker Arg1, and reactive astrocyte marker Gfap.[1]
Synonyms	GI 254023X
Cell Research	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].

Chemical Properties

Molecular Weight	391.5
Formula	C₂₁H₃₃N₃O₄
Cas No.	260264-93-5
Smiles	CNC(=O)[C@@H](NC(=O)[C@H](CCCc1ccccc1)[C@H](C)N(O)C=O)C(C)(C)C
Relative Density.	1.112 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 117.5 mg/mL (300.13 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.22 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5543 mL	12.7714 mL	25.5428 mL	127.7139 mL
5 mM	0.5109 mL	2.5543 mL	5.1086 mL	25.5428 mL
10 mM	0.2554 mL	1.2771 mL	2.5543 mL	12.7714 mL
20 mM	0.1277 mL	0.6386 mL	1.2771 mL	6.3857 mL
50 mM	0.0511 mL	0.2554 mL	0.5109 mL	2.5543 mL
100 mM	0.0255 mL	0.1277 mL	0.2554 mL	1.2771 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SRI-028594SRI028594SRI 028594MMP-9MMPMatrix metalloproteinasesInhibitorinhibitInflammationrelatedInflammation relatedImmunologyrelatedImmunology relatedGI-4023GI4023GI-254023XGI254023XGI 4023ADAM10

Related Tags: GI254023X chemical structure | GI254023X in vivo | GI254023X in vitro | GI254023X formula | GI254023X molecular weight