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C188-9

CAS No. : 432001-19-9

MCE 站：C188-9

产品活性：C188-9 (TTI-101) 是 Stat3 的抑制剂，其 K_d 值为 4.7 nM。C188-9 抑制 G-CSF 诱导的 STAT3 激活和 STAT3 依赖性基因表达。C188-9 诱导 AML 细胞系和原代标本凋亡，抑制原代 AML 细胞集落形成。

研究领域：JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：STAT  |  Apoptosis

In Vitro: C188-9 is a Stat3 inhibitor, with a K_d of 4.7 nM. The IC₅₀s of C188-9 to inhibit Stat3 activation in AML cell lines are in the range of 4-7 μM, ａnd in primary AML samples the IC₅₀s are in the range of 8-18 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.

In Vivo: 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. In comparison, 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.

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