STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.
STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway[1].STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50 values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively[1].STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells[1].
STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts[1].
References:
[1]. Deng L, et, al. Boronic Acid: A Novel Pharmacophore Targeting Src Homology 2 (SH2) Domain of STAT3. J Med Chem. 2022 Oct 13;65(19):13094-13111.