2. MAPK/ERK Pathway Apoptosis
  3. JNK Apoptosis
  4. 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.

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GSTP1/M2-IN-1

GSTP1/M2-IN-1 Chemical Structure

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GSTP1/M2-IN-1 Related Antibodies

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Description

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[1].

In Vitro

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.

GSTP1/M2-IN-1 Related Antibodies
In Vivo

GSTP1/M2-IN-1 (Compound 5b) (5 mg/kg, once daily for 14 days) in combination with Gemcitabine exhibits potent synergistic antitumor activity in the MiaPaCa-2 pancreatic cancer xenograft mice model and downregulates the protein expression levels of GSTP1 and GSTM2 in tumor tissues[1].

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

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].
Dosage: 5 mg/kg; Gemcitabine: 100 mg/kg
Administration: I.p., once daily for 14 days
Result: Both tumor volume and mass were significantly reduced.
Protein expression levels of GSTP1 and GSTM2 in tumor tissue were downregulated.
Molecular Weight

480.43

Formula

C16H12N6O8S2
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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Room temperature in continental US; may vary elsewhere.
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References
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GSTP1/M2-IN-1 Related Classifications

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  • 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/M2-IN-1JNKApoptosisc-Jun N-terminal kinaseAnticancer agentsOxidative stressGSTP1GSTM2Gemcitabine resistanceInhibitorinhibitorinhibit

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