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.
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- CAS No.: 3114128-67-2
- 화학식: C16H14F3N3OS
- 분자량:353.36
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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GSTO1 457 nM (IC50) |
IL-1β |
IL-18 |
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.
Chemical Information
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CAS No. 3114128-67-2
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분자량 353.36
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화학식 C16H14F3N3OS
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SMILES
O=C(N1CCC[C@@H]1C2=NN=C(S2)C3=CC=C(C=C3)C(F)(F)F)C=C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- GSTO1-IN-6
- 3114128-67-2
- Glutathione S-transferase
- Interleukin Related
- Cys32
- NEK7
- Cys253
- GSTO1
- covalent
- inflammatory
- metabolic
- inhibitor
- PRM-based
- secretion
- liver
- NLRP3
- iodoacetamide
- ABPP
- inflammasome
- hydrophobic
- desthiobiotin
- selectivity
- targeted
- spectrometry
- diseases
- cysteine
- proinflammatory
- human
- macrophages
- LPS-induced
- monocyte-derived
- mass
- IL-1β
- IL-18
- microsomes
- stability
- Inhibitor
- inhibit