化合物C188-9 T4650

Product Introduction
Bioactivity


英文名: C188-9

描述: C188-9 (TTI-101) 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。

体外活性: 在凋亡研究中，AML细胞株和原始样本经C188-9处理24小时后，通过FACS分析量化标记Annexin V的细胞来确定凋亡细胞的数量。凋亡诱导的EC50值变化较大，范围从6 μM到超过50 μM不等。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (127.25 mM)


关键字: C1889 | Apoptosis | STAT | TTI101 | Inhibitor | C188 9 | C-188-9 | C188-9 | inhibit | TTI 101

相关产品: APE1-IN-2 | Novobiocin | Ac-​IETD-​CHO | Azadirachtin | Polyphyllin II | Niraparib hydrochloride | Domatinostat tosylate | Pladienolide B | TAS6417 | Puerarin 6''-O-Xyloside

相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Cancer Cell Differentiation Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Target-Focused Phenotypic Screening Library

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