GSTO1-IN-3
GSTO1-IN-3 is a potent GSTO1-1 inhibitor with an IC50 of 0.11 μM, and shows selectivity over GSTO2-2, GSTA1-1 and GSTP1-1 (IC50 > 100 μM). GSTO1-IN-3 enhances the cytotoxicity of Cisplatin (HY-17394) against human breast cancer cells. GSTO1-IN-3 inhibits IL-1β release in mouse bone marrow-derived macrophage (BMDM) cells. GSTO1-IN-3 attenuates inflammation in mice. GSTO1-IN-3 can be used for breast cancer and inflammation research.
For research use only. We do not sell to patients.
- CAS No.: 158890-32-5
- Formula: C14H18ClNO
- Molecular Weight:251.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSTO1-1 0.11 μM (IC50) |
GSTO1-IN-3 (compound 5C-1) demonstrates a promising in vitro safety profile with no detectable thiol reactivity (ALARM NMR test), no mutagenicity (Ames test, S. typhimurium strains TA98 and TA100, ≤2 mg/mL), and greater stability in human liver microsomes than in murine systems[1].
GSTO1-IN-3 forms covalent bonds with the Cys32 of GSTO1-1, with kᵢₙₐcₜ/Kᵢ of 3.4 × 104 M-1s-1[1].
GSTO1-IN-3 (5 μM) inhibits IL-1β release in mouse BMDM cells with inhibition of 59.2%[1].
GSTO1-IN-3 (5-50 μM, 24 h) acts synergistically with Cisplatin to significantly enhance cytotoxicity against human breast cancer MDA-MB-231 cells in a concentration-dependent manner[[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:5, 10, and 50 μM
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Incubation Time:24 h
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Result:Showed no particularly cytotoxicity at 5 μM (5.8%) in MDA-MB-231 cells.
Showed a low level of cytotoxicity at 10 μM (13.0%) and a significantly higher level of cytotoxicity (83.2%) at a concentration of 50 μM.
Acted synergistically to significantly raise the cytotoxicity of 20 μM Cisplatin to 55.1%.
Increased the cytotoxicity of Cisplatin to 73.6% at 10 μM.
Achieved a cytotoxicity level of 83.3% at 50 μM when combined with Cisplatin, which was not significantly different from its effect when administered alone.
| Species | Dose | Route | Note | Cmax |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | Male Swiss outbred mice | 5.75 μM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 mice (8 weeks old) intraperitoneally injected with LPS[1]
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Dosage:30 mg/kg
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Administration:i.p., single dose 30 min pre-LPS
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Result:Significantly attenuated the LPS-induced reduction in body temperature at 6 h compared to the LPS-only control.
Showed significant protection against the inflammatory effects of LPS on mice at 4 h.
Significantly suppressed the release of IL-1β up to 4 h, but this suppression was not sustained at 6 h, likely due to the short in vivo half-life of the inhibitors.
Chemical Information
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CAS No. 158890-32-5
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Molecular Weight 251.75
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Formula C14H18ClNO
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SMILES
O=C(N1CCC(CC1)CC2=CC=CC=C2)CCl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSTO1-IN-3 Related Classifications
HY-W615446 Related Classifications
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