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

GSTO1-IN-3 is a potent GSTO1-1 inhibitor with 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.

GSTO1-IN-3

GSTO1-IN-3 Chemical Structure

CAS No. : 158890-32-5

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GSTO1-IN-3 Related Antibodies

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Description

GSTO1-IN-3 is a potent GSTO1-1 inhibitor with 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[1].

IC50 & Target[1]

GSTO1-1

0.11 μM (IC50)

In Vitro

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.

GSTO1-IN-3 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 5, 10, and 50 μM
Incubation Time: 24 h
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.
In Vivo

GSTO1-IN-3 (30 mg/kg, i.p., single dose 30 min pre-LPS) attenuates inflammation induced by Lipopolysaccharide (LPS) (HY-D1056) in mice[1].

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

Animal Model: Female C57BL/6 mice (8 weeks old) intraperitoneally injected with LPS[1]
Dosage: 30 mg/kg
Administration: i.p., single dose 30 min pre-LPS
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.
Molecular Weight

251.75

Formula

C14H18ClNO
CAS No.
SMILES

O=C(N1CCC(CC1)CC2=CC=CC=C2)CCl
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-3 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-3158890-32-5Glutathione S-transferaseInterleukin RelatedGlutathione transferasesGSTsILGSTO1-1MDA-MB-231IL-1βBMDMbreast cancerinflammationInhibitorinhibitorinhibit

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