2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Glutathione S-transferase Interleukin Related
  4. GSTO1-IN-6

GSTO1-IN-6 is an allosteric and covalent GSTO1 inhibitor with an IC50 of 457 nM. GSTO1-IN-6 markedly reduces Lipopolysaccharides (LPS) (HY-D1056)-induced IL-1β (IC50 of 1.9 μM) and IL-18 (IC50 of 10. μM) secretion in human monocyte-derived macrophages. GSTO1-IN-6 covalently modifies GSTO1-Cys32, inducing conformational changes and protein destabilization. GSTO1-IN-6 can be used for the research of inflammatory diseases.

For research use only. We do not sell to patients.

GSTO1-IN-6

GSTO1-IN-6 Chemical Structure

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GSTO1-IN-6 Related Antibodies

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

GSTO1-IN-6 is an allosteric and covalent GSTO1 inhibitor with an IC50 of 457 nM. GSTO1-IN-6 markedly reduces Lipopolysaccharides (LPS) (HY-D1056)-induced IL-1β (IC50 of 1.9 μM) and IL-18 (IC50 of 10. μM) secretion in human monocyte-derived macrophages. GSTO1-IN-6 covalently modifies GSTO1-Cys32, inducing conformational changes and protein destabilization. GSTO1-IN-6 can be used for the research of inflammatory diseases[1].

IC50 & Target[1]

GSTO1

457 nM (IC50)

IL-1β

 

IL-18

 

In Vitro

GSTO1-IN-6 (compound A13) (1 μM; 5-60 minutes) demonstrates good metabolic stability in human and rat liver microsomes and good permeability in Caco-2 cells[1].
GSTO1-IN-6 (2-10 μM; for 2 h) inhibits LPS- and Nigericin (HY-127019)-induced IL-1β secretion in mouse BMDMs[1].
GSTO1-IN-6 (16 hours) inhibits LPS- and Nigericin-induced IL-1β and IL-18 release in human PBMC-derived macrophages[1].

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

GSTO1-IN-6 Related Antibodies
Parmacokinetics
Species Dose Route Note Cmax AUC0-t T1/2 Tmax F
Mice[1] 1 mg/kg i.v. 文献审核 175 ng/mL 55.7 ng·h/mL 0.448 h 0.083 h /
Mice[1] 10 mg/kg i.p. 文献审核 817 ng/mL 199 ng·h/mL 0.261 h 0.083 h 34.3 %
Mice[1] 10 mg/kg p.o. 文献审核 85.9 ng/mL 37 ng·h/mL 0.7 h 0.194 h 6.69 %
Molecular Weight

353.36

Formula

C16H14F3N3OS
SMILES

O=C(N1CCC[C@@H]1C2=NN=C(S2)C3=CC=C(C=C3)C(F)(F)F)C=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSTO1-IN-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSTO1-IN-6Glutathione S-transferaseInterleukin RelatedGlutathione transferasesGSTsILCys32NEK7Cys253GSTO1covalentinflammatorymetabolicpocketinhibitorPRM-basedsecretionliverNLRP3iodoacetamideABPPinflammasomehydrophobicdesthiobiotinselectivitytargetedspectrometrydiseasescysteineproinflammatoryhumanmacrophagesLPS-inducedmonocyte-derivedmassIL-1βIL-18microsomesstabilityInhibitorinhibit

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HY-179635
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