2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Glutathione S-transferase Reactive Oxygen Species (ROS)
  4. GSTP1-IN-1

GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC50 of 0.79 μM and a Kd of 0.63 μM. GSTP1-IN-1 inhibits the proliferation of gastric cancer cells, induces ROS production and depletes glutathione. GSTP1-IN-1 achieves systemic exposure and is well tolerated in xenograft mouse models, while inhibiting tumor growth. GSTP1-IN-1 can be used in gastric cancer-related research.

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

GSTP1-IN-1

GSTP1-IN-1 Chemical Structure

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GSTP1-IN-1 Related Antibodies

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Description

GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC50 of 0.79 μM and a Kd of 0.63 μM. GSTP1-IN-1 inhibits the proliferation of gastric cancer cells, induces ROS production and depletes glutathione. GSTP1-IN-1 achieves systemic exposure and is well tolerated in xenograft mouse models, while inhibiting tumor growth. GSTP1-IN-1 can be used in gastric cancer-related research[1].

In Vitro

GSTP1-IN-1 (Compound 16n) (72 h) selectively inhibits the viability of human gastric cancer cells dependent on GSTP1 expression, with an IC50 value of < 10 μM in sensitive cell lines; moreover, after 72 h of treatment, it shows no toxicity to non-cancerous cells THLE-2 and MRC-9 even at concentrations as high as 50 μM[1].
GSTP1-IN-1 (10 μM; 3 h) directly binds to endogenous GSTP1 in human AGS and HGC27 gastric cancer cells, and increases its thermal stability after pre-incubation at 10 μM for 3 h[1].
GSTP1-IN-1 (0-10 μM; 1 h) inhibits GST activity in human AGS gastric cancer cells in a dose-dependent manner, and significant inhibitory effects are observed at concentrations ≥ 3 μM after 1 hour of treatment[1].
GSTP1-IN-1 (0-10 μM; 1 h) reduces glutathione levels in human AGS gastric cancer cells in a dose-dependent manner, with a significant decrease observed at concentrations ≥ 3 μM after 1 hour of treatment[1].
GSTP1-IN-1 (0-10 μM; 1 h) dose-dependently increases the reactive oxygen species level in human AGS, HGC27 and NUGC-3 gastric cancer cells, and a significant inductive effect is observed at concentrations ≥ 1 μM after 1 hour of treatment[1].

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

GSTP1-IN-1 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ CL Vss Bioavailability
Mice[1] 10 mg/kg i.v. 1.1 h 0.083 h 4927 ng/mL 5207 ng·h/mL 2003 mL/h/kg 2383 mL/kg /
Mice[1] 30 mg/kg i.p. 2.5 h 0.33 h 5850 ng/mL 11937 ng·h/mL 2526 mL/h/kg / 76 %
In Vivo

GSTP1-IN-1 (Compound 16n) (100-200 mg/kg; i.p.; twice daily for 18 consecutive days) achieves 58% tumor growth inhibition in HGC27 gastric cancer xenograft mice at the dose of 200 mg/kg, while reducing the proliferative activity of tumor cells and exhibiting good tolerability[1].

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

Animal Model: BALB/c-nude (female, body weight 16-20 g, HGC27 human gastric cancer cells xenograft)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: i.p.; twice a day; for 18 consecutive days
Result: Achieved 58% tumor growth inhibition at 200 mg/kg.
Decreased the number of Ki67-positive proliferating cells in tumors at 100 mg/kg and 200 mg/kg.
Caused no significant body weight loss.
Molecular Weight

687.65

Formula

C30H28F3N7O7S
SMILES

O=S(C1=C(C=CC=C1)OC(F)(F)F)(N2CC(C2)CN3C4=C(N=C3C5=CC=C(CN6N=C(C)C([N+]([O-])=O)=C6C)O5)C=C(C(NC)=O)C=C4)=O
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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GSTP1-IN-1 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:

GSTP1-IN-1Glutathione S-transferaseReactive Oxygen Species (ROS)Glutathione transferasesGSTsAGS gastric cancer cellsGSTZ1GSTP1gastric cancer cellsGSTM2GSTT1glutathionexenograft mouse modelsGSTA1GSTO1Inhibitorinhibitorinhibit

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