Product Details
| Product Name:
GI254023X |
CAS No.:
260264-93-5 |
| Purity:
98.56% |
Supply Ability:
10g |
| Release date:
2025/11/10 |
Product Introduction
Bioactivity
| Name | GI254023X |
| 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. |
| 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]. |
| 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] |
| 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 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.22 mM), Sonication is recommended.
DMSO : 100 mg/mL (255.43 mM), Sonication is recommended.
|
| Keywords | SRI-028594 | SRI028594 | SRI 028594 | MMP-9 | MMP | Matrix metalloproteinases | Inhibitor | inhibit | Inflammationrelated | Inflammation related | Immunologyrelated | Immunology related | GI-4023 | GI4023 | GI-254023X | GI254023X | GI 4023 | ADAM10 |
| Inhibitors Related | Stigmasterol | Benzyl cinnamate | Ethyl gallate | Doxycycline (hyclate) | Astragaloside IV | Doxycycline | Edaravone | Glucosamine | Bovine Type II Collagen | Triolein | Arctigenin | Glucosamine sulfate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States