GSTP1/M2-IN-1
GSTP1/M2-IN-1 is a GSTP1/GSTM2 inhibitor(IC50 = 1.56 μM/0.09 μM). GSTP1/M2-IN-1 can activate the JNK pathway and induce cell apoptosis. GSTP1/M2-IN-1 can be used for the study of breast cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C16H12N6O8S2
- Molecular Weight:480.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
GSTP1/M2-IN-1 (Compound 5b) exhibits potent anticancer activity, particularly effective against GSTM2-overexpressing cell lines (such as 67NR and 4T1): MDA-MB-231 cells (IC50 = 1.11 μM), MiaPaCa-2 cells (IC50 = 1.81 μM), 4T1 cells (IC50 = 1.90 μM), 67NR cells (IC50 = 1.08 μM)[1].
GSTP1/M2-IN-1 co-treatment with the JNK inhibitor SP600125 (HY-12041) markedly increases IC50 values, confirming that JNK activation is essential for their cytotoxicity in MDA-MB-231 (2.71 to 15.42 μM) and MiaPaCa-2 (1.78 to 15.23 μM) cell lines[1].
GSTP1/M2-IN-1 (24-72 h) significantly increases JNK, p-c-Jun, cleaved caspase-3, and PARP cleavage in MDA-MB-231 and MiaPaCa-2 cell lines[1].
GSTP1/M2-IN-1 and its combination with Gemcitabine (HY-17026) activate apoptotic pathways, as evidenced by increased cleavage of PARP, elevated P-JNK, and P-c-JUN in MIAPaCa-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:500,000 MiaPaCa-2 human pancreatic cancer cells were mixed with Matrigel in a 1:1 ratio and injected into the flank of NSG mice[1].
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Dosage:5 mg/kg; Gemcitabine: 100 mg/kg
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Administration:I.p., once daily for 14 days
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Result:Both tumor volume and mass were significantly reduced.
Protein expression levels of GSTP1 and GSTM2 in tumor tissue were downregulated.
Chemical Information
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Molecular Weight 480.43
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Formula C16H12N6O8S2
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SMILES
O=[N+](C1=CC=C(C2=NON=C12)SC[C@H]([C@H](CSC3=CC=C(C4=NON=C34)[N+]([O-])=O)O)O)[O-]
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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)