SMILES string
OC1=C(C=CC=C1)C(C)=NNC(C2=C(C=CC=C2)O)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
shipped in
ambient
storage temp.
−20°C
Biochem/physiol Actions
C108是一种小分子，具有癌症选择性细胞毒性（使用1 μM C108处理48小时后，存活率 = 100%/MCF-10A，50%/BT-474，67%/4T1，70%/MDA-MB-231 & MDA-MB-453），并且能够与低剂量紫杉醇靶向应激颗粒相关蛋白G3BP2（GAP SH3结构域结合蛋白2），从而协同减少ALDH阳性肿瘤起始细胞（使用药物处理BT474乳腺癌细胞培养物24小时后，TIC群体 = 56.6％/对照，60.6%/0.1 μM紫杉醇单独使用，47.4%/1 μM C108单独使用，7.3%/组合使用）。同样，在异种移植前使用C108预处理，能够在体内大大降低小鼠的BT-474肿瘤起始频率（有限稀释异种移植测定结果显示，从1/175降低至1/1103）。据报道，G3BP2能够结合并稳定SART3 mRNA，从而间接调节核心多能性转录因子Oct-4和Nanog，它们对ESC自我更新和乳腺肿瘤起始至关重要。
G3BP2抑制剂具有癌症选择性细胞毒性，并且能够与低剂量紫杉醇协同减少乳腺癌培养物中的肿瘤起始细胞（TIC）群体。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Nisha Gupta et al.
Proceedings of the National Academy of Sciences of the United States of America, 114(5), 1033-1038 (2017-01-18)
Breast tumors contain tumorigenic cancer cells, termed "tumor-initiating cells" (TICs), which are capable of both replenishing themselves and giving rise to populations of nontumorigenic breast cancer cells (non-TICs). However, the molecular mechanisms responsible for breast tumor initiation remain poorly understood.
Ningning Li et al.
Current pharmaceutical biotechnology, 21(11), 1107-1118 (2020-03-21)
Renal fibrosis is a common pathway leading to the progression of chronic kidney disease. Activated fibroblasts contribute remarkably to the development of renal fibrosis. Although apigenin has been demonstrated to play a protective role from fibrotic diseases, its pharmacological effect
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