GI-Y2
GI-Y2 is an orally active, selective Gasdermin D (GSDMD) inhibitor (Kd = 36.0 μM) with anti-pyroptosis activity. GI-Y2 targets GSDMD, impairs membrane anchoring of GSDMD-NT, and blocks GSDMD‑dependent lipid binding and pore formation. GI-Y2 suppresses GSDMD‑dependent pyroptosis and inflammation, mitigates atherosclerosis and cardiac injury, boosts cell survival, and reduces IL‑1β/IL‑18 secretion. GI-Y2 can be used for the research of atherosclerosis and septic myocardial injury.
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- CAS No.: 1008710-58-4
- Formule: C18H14N2O6S
- Masse moléculaire:386.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
IL-18 |
IL-1β |
In Vitro
GI-Y2 suppresses LPS+Nigericin (HY-127019)-induced pyroptosis in PMA-differentiated THP-1 cells with an IC50 of 35.40 μM by binding to the Arg10 residue of GSDMD via hydrogen bonding to reduce GSDMD-NT membrane localization[1][2].
GI-Y2 (2.5-40 μM) directly binds to purified GST-GSDMD protein with a Kd value of 36.0 μM[1].
GI-Y2 (10 μM; 1 h) directly interacts with Flag-GSDMD expressed in HEK/293T cells, as evidenced by reduced pronase-mediated degradation of GSDMD at 10 μM[1].
GI-Y2 inhibits GSDMD-mediated pyroptosis in human AC16, HEK-293T, and HepG2 cell lines[1].
GI-Y2 (10 μM; 1 h) reduces GSDMD-N membrane binding and pyroptotic LDH release in HEK/293T cells expressing wild-type Flag-GSDMD, but not in cells expressing the GSDMDR10A mutant, confirming Arg10 as the critical binding site[1].
GI-Y2 (10-20 μM; 1 h) dose-dependently inhibits ox-LDL-induced pyroptosis in ApoE−/− mouse primary peritoneal macrophages, reducing lipid uptake, inflammatory cytokine production, and GSDMD-N activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK/293T cells
HEK/293T cells expressing wild-type Flag-GSDMD and GSDMDR10A mutant -
Concentration:0, 10 μM
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Incubation Time:1h
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Result:Reduced pronase-mediated degradation of GSDMD at 10 μM.
Reduced GSDMD-N membrane binding and pyroptotic LDH release in HEK/293T cells expressing wild-type Flag-GSDMD, but not in cells expressing the GSDMDR10A mutant.
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Cell Line:ApoE−/− mouse primary peritoneal macrophages
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Concentration:0, 10, 20 μM
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Incubation Time:1h
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Result:Inhibits ox-LDL-induced pyroptosis.
Reduced lipid uptake, inflammatory cytokine production, and GSDMD-N activation.
In Vivo
GI-Y2 (10-20 mg/kg; i.g.; every 2 days; 6 weeks) dose-dependently reduces atherosclerotic plaque formation, pyroptotic inflammation, and immune cell infiltration in ApoE−/− mice fed a high-fat diet[1].
GI-Y2 (20 mg/kg; i.g.; every 2 days; 6 weeks) does not provide additional protection against atherosclerosis in Gsdmd-deficient ApoE−/− mice, confirming its effects are mediated via targeting GSDMD[1].
GI-Y2 (0.03 mg/kg; i.v.; every 3 days; 4 weeks) reduces atherosclerotic plaque formation in ApoE−/− mice, with enhanced efficacy when delivered via macrophage membrane-coated nanoparticles[1].
GI-Y2 improves survival and decreases pro-inflammatory cytokine levels in septic mice. GI-Y2 attenuates atherosclerotic lesions and septic myocardial injury by targeting GSDMD-mediated pyroptosis, and its therapeutic efficacy is significantly enhanced by macrophage membrane-coated nanoparticle delivery[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1008710-58-4
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Masse moléculaire 386.38
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Formule C18H14N2O6S
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SMILES
OC(C1=CC=C(CN2C(SC(NC3=CC=C(C(O)=O)C=C3)C2=O)=O)C=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)