LLL-12

LLL12 is a small molecule inhibitor of STAT3 that inhibits STAT3 phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth[1].

Signaling Pathways >> Stem Cell/Wnt >> STAT

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

p-STAT3

LLL12 (0.01-1 μM; 72 h) 在顺铂 (0.5 μM, 2.5 μM) 和紫杉醇 (0.25 μM, 0.5 μM) 作用下均能抑制卵巢癌细胞系的细胞活力[1]。 LLL12 (0.25-1.0μM) 抑制卵巢癌细胞系中 STAT3 磷酸化 (Tyr705)[1]。 Western Blot Analysis[1] Cell Line: A2780, SKOV3, CAOV-3 and OVCAR5 ovarian cancer cell lines Concentration: 0.25, 0.5, and 1 μM for A2780 and OVCAR5; 1, 2.5, and 5 μM for SKOV3 and CAOV-3 Incubation Time: 72 hours Result: Inhibited STAT3 phosphorylation at Tyr705.

LLL12 (5 mg/kg; 腹腔注射; 每天 1 次, 共 13 天) 在小鼠骨肉瘤细胞和肿瘤生长中表现出强大的生长抑制活性[2]。 Animal Model: Mouse xenografts with SJSA or OS-33 osteosarcoma cells[2] Dosage: 5 mg/kg Administration: Intraperitoneal injection; once daily for 13 days Result: Resulted in a significant reduction in tumor volume and tumor mass in the OS-33 and SJSA xenografted mice.

[1]. Zhang R, et al. A small molecule STAT3 inhibitor, LLL12, enhances cisplatin‑ and paclitaxel‑mediated inhibition of cell growth and migration in human ovarian cancer cells. Oncol Rep. 2020 Sep;44(3):1224-1232.  

[2]. Onimoe GI, et al. Small molecules, LLL12 and FLLL32, inhibit STAT3 and exhibit potent growth suppressive activity in osteosarcoma cells and tumor growth in mice. Invest New Drugs. 2012 Jun;30(3):916-26.