assay
≥98% (HPLC)
form
powder
potency
2-5 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
Quality Level
General description
一种可渗透细胞的氯苯乙炔基磺酰胺化合物,可直接与热休克蛋白70(HSP70)的底物结合域结合并破坏其与客户蛋白质的相互作用。损害无细胞提取物中后期促进复合物/环体(APC/C)的活性。将细胞周期阻滞在G2/M期,并优先诱导癌症细胞的基因组不稳定性(在黑色素瘤细胞系中IC50=2至5 µM)。在非转化细胞中表现出大大降低的毒性(在原代黑素细胞中IC50为>100 µM)。诱导凋亡并抑制自噬,如p62SQSTM1和LC3积累增加所证明。 此外,在前B细胞淋巴瘤的鼠模型中显示出延长寿命。
请注意,由于变化的含水量,该化合物的分子量是批次特异性的。
请注意,由于变化的含水量,该化合物的分子量是批次特异性的。
Biochem/physiol Actions
主要靶标
HSP70
HSP70
可逆性:是
细胞可渗透性:具有
Packaging
用惰性气体包装
Preparation Note
复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。
Other Notes
Balaburski, G., et al. 2013. Mol.Cancer Res.11, 1.
Budina-Kolomets, A. et al. 2013. Cancer Biol. Ther.15, 194.
Budina-Kolomets, A. et al. 2013. Cancer Biol. Ther.15, 194.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性:标准处理(A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Anna Budina-Kolomets et al.
Cancer biology & therapy, 15(2), 194-199 (2013-10-09)
The chaperone HSP70 promotes the survival of cells exposed to many different types of stresses, and is also potently anti-apoptotic. The major stress-induced form of this protein, HSP70-1, is overexpressed in a number of human cancers, yet is negligibly expressed
Gregor M Balaburski et al.
Molecular cancer research : MCR, 11(3), 219-229 (2013-01-11)
The stress-induced HSP70 is an ATP-dependent molecular chaperone that plays a key role in refolding misfolded proteins and promoting cell survival following stress. HSP70 is marginally expressed in nontransformed cells, but is greatly overexpressed in tumor cells. Silencing HSP70 is
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