STAT3-IN-38 (Compound 4m) is a STAT3 inhibitor with a dissociation constant (K_D) of 45.33 µM for rhSTAT3, and is a derivative of Celastrol. It binds to the SH2 domain of the STAT3 protein, inhibiting phosphorylation at the pTyr705 site and suppressing downstream gene expression of Survivin and Mcl-1. STAT3-IN-38 can arrest the cell cycle and induce apoptosis in colorectal cancer cells.

STAT3:45.33 μM (Kd)

STAT3-IN-38 (0.5-1 μM, 6 h) 能够抑制 HCT116 细胞中 STAT3 的磷酸化，并降低 STAT3 靶蛋白 survivin 和髓样细胞白血病 1 (Mcl-1) 的水平。此外，STAT3-IN-38 (0.02-12.5 μM, 48 h) 可有效抑制 A549、HCT116 和 HepG2 细胞的增殖。使用 STAT3-IN-38 (1-5 μM, 48 h) 可诱导 HCT116 细胞发生凋亡并导致细胞周期停滞。STAT3-IN-38 (1-10 µM, 6 天) 还能够降低人结直肠癌类器官 (CCOs) 的活力。