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
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
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
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