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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C16H12N6O8S2
- 分子量:480.43
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
-
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.
化学情報
-
分子量 480.43
-
分子式 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-]
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)