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Cat. No.: HY-182059

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GSTP1-IN-1

GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC₅₀ of 0.79 μM and a K_d 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.

Formula: C₃₀H₂₈F₃N₇O₇S
Molecular Weight:687.65

Storage:

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

GSTP1-IN-1 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

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.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-∞	CL	V_ss	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.

Chemical Information

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

Handling Instructions (2659 KB)

References

[1]. Xie W, et al. Discovery of 1-(Azetidin-3-ylmethyl)-1H-benzo[d]imidazole Derivatives as Efficient GSTP1 Inhibitors for Gastric Cancer Treatment via Warhead Removal Strategy. J Med Chem. 2026;69(5):5622-5647. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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