C188-9 是一种STAT3抑制剂，其Kd值为 4.7 nM。它诱导 AML 细胞系和原代标本凋亡，抑制原代 AML 细胞集落形成。它抑制 G-CSF 诱导的 STAT3 激活和 STAT3 依赖性基因表达。

C188-9 is a Stat3 inhibitor with an IC50 of 4-7 μM.

For apoptosis studies, AML cell lines and primary samples are treated for 24 hours with C188-9, then apoptotic cells are quantified by FACS analysis for annexin V-labeled cells. The EC50s for apoptosis induction are quite variable, ranging from 6 μM to over 50 μM

Of the approximately 13,528 discernible genes, levels of 37 gene transcripts are altered by C188 (17 down and 20 up-regulated, fdr<0.01, fold change≥1.5), of which 7 are known STAT3 gene targets. By contrast, C188-9 affects a much greater number of genes involved in oncogenesis (384 total, 95 down- and 289 up-regulated), including 76 genes previously reported as regulated by STAT3 (38 down-regulated and 38 up-regulated). Among the 38 genes previously shown to be upregulated by STAT3, 24 (63%) genes are downregulated by C188-9 treatment, as expected. Additionally, 10 more genes downregulated by C188-9 (fdr<0.01, fold change≥1.5) that previously are shown to be upregulated by STAT1. Thus, 40 of 48 (83.3%) genes downregulated by C188-9 previously are shown to be positively regulated by STAT1, including sixteen genes shown to be co-regulated by STAT3 and STAT1. This analysis raises the possibility that the effect of C188-9 on gene transcript levels in HNSCC tumors is mediated by its effects on both STAT3 and STAT1[2].

432001-19-9

C27H21NO5S

471.53

TTI-101

DMSO:62 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years