inS3-54A18

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

Research Areas >> Cancer

STAT3

inS3-54A18 (5 μM) reduces wound healing to 64% and 76% for A549 and MDA-MB-231 cells, respectively. inS3-54A18 at 10 μM further reduces the healing to 47% and 39%, respectively. inS3-54A18 inhibits the expression of STAT3 downstream target genes and the binding of STAT3 to its endogenous target sequences. inS3-54A18 does not affect the constitutive or IL-6-induced STAT3 activation (Tyr705 phosphorylation) but represses STAT3 target gene (survivin) expression[1].

inS3-54A18 (200 mg/kg, p.o.) inhibits tumor growth, metastasis and expression of STAT3 target genes in a mouse xenograft model of A549 cells[1].

Briefly, 5×106 A549 cells are injected subcutaneously in the flanks of 5-6-week-old male NOD/SCID mice. When the tumor volume reach about 50.0 mm3, the mice are randomized using online program into two different groups (6/group) with one group treated by formulation vehicle control and the other by A18 at 200 mg/kg with oral dosing 2-3 times a week for 4 weeks. One mouse in each group dies during the study and is eliminated. Tumor volume and body weight of the remaining five mice in each group are measured twice a week without blinding. On the thirty-fifth day after implant, mice are euthanized and the tumor tissues are harvested and weighed. Necropsy is also performed to determine changes in the heart, lungs, kidneys, liver and spleen.

[1]. Huang W, et al. Small-molecule inhibitors targeting the DNA-binding domain of STAT3 suppress tumor growth, metastasis and STAT3 target gene expression in vivo. Oncogene. 2016 Feb 11;35(6):783-92

Tyrphostin B42 (AG-490) | Stattic | AS1517499 | S3I-201 | Cryptotanshinone | Napabucasin | Homoharringtonine | STAT5-IN-1 | WP1066 | Niclosamide | BP-1-102 | Scutellarin | SH-4-54 | HO-3867 | Artesunate