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Cat. No.: HY-178372

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GSTO1-IN-4

GSTO1-IN-4 is a selective, potent GSTO1-1 inhibitor (IC₅₀ = 0.04 μM; K_I = 0.16 μM). GSTO1-IN-4 shows low inhibition to GSTO2-2, GSTA1-1 and GSTP1-1. GSTO1-IN-4 shows a capacity to attenuate inflammation in mice and to significantly enhance the cytotoxicity of Cisplatin (HY-17394). GSTO1-IN-4 can be used for the study of inflammation and breast cancer.

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

CAS No.: 158890-33-6
Formula: C₁₆H₂₂ClNO
Molecular Weight:279.80

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (244 KB)

GSTO1-IN-4 Chemical Structure

CAS No.: 158890-33-6

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

GSTO1-IN-4 (5 μM, 2 h) (Compound 10u) effectively inhibits intracellular GSTO1-1 activity, thereby suppressing NLRP3 inflammasome activation and IL-1β release in BMDMs^[1].
GSTO1-IN-4 (10 μM) exhibits high selectivity for GSTO1-1, but low inhibition levels against GSTA1-1 and GSTP1-1^[1].
GSTO1-IN-4 (5-50 μM, 24 h) shows low cytotoxicity at 5 μM (6.3 %) and 10 μM (13.9 %), and a significantly higher cytotoxicity at 50 μM (74.3 %) in MDA-MB 231 cells^[1].

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

ELISA Assay^[1]

Cell Line:

BMDMs stimulated with 200 ng/mL LPS for 3 h, then incubated in serum-free DMEM containing the test compound and incubated in DMEM containing 5 mM ATP for another 1 h.
Concentration:

5 μM
Incubation Time:

2 h
Result:

Significantly reduced IL-1β release, decreasing the release level to 2.6 ± 0.5% (relative to untreated cells), with an inhibition rate of 97.4%.

Cell Cytotoxicity Assay^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

5 μM, 10 μM, 50 μM
Incubation Time:

24 h
Result:

Showed low cytotoxicity at 5 μM (6.3 %) and 10 μM (13.9 %), and a significantly higher cytotoxicity at 50 μM (74.3 %).
Significantly raise the cytotoxicity of 20 μM Cisplatin (42.2 %) to 68.8 %, 68.0 %, and 88.7 % at 5 μM, 10 μM, and 50 μM, respectively.
The cytotoxicity of 20 μM Cisplatin in combination with 50 μM test compound was also not significantly different from that of 50 μM test compound alone.

In Vivo

GSTO1-IN-4 (50 mg/kg, I.p., once) can resist the inflammatory effect induced by Lipopolysaccharides (LPS) (HY-D1056) in mice^[1].

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

Animal Model:

C57BL/6 female mice, 8 weeks of age^[1].
Dosage:

50 mg/kg
Administration:

I.p., injection 0.5 h before LPS administration
Result:

Did not show a decrease in body temperature at 6 h and were not significantly different from normal control mice that were not treated with LPS.
Significantly suppressed the release of IL-1β up to 4 h, but after 6 h, the level of IL-1β had risen to levels that were not significantly different from the control wild-type mice treated with LPS.

Chemical Information

CAS No. 158890-33-6
Molecular Weight 279.80
Formula C₁₆H₂₂ClNO
SMILES

O=C(N1CCC(CC1)CCCC2=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.