产品信息
商品描述
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
分子量
399.48
纯度
98%
可溶性
DMSO : 25 mg/mL (62.58 mM; Need ultrasonic)
外观
Off-white solid
In vitro(体外研究)
HLM006474 shows little activities against E2F4 DNA-binding in A375 cells at 10 and 20 µM, apparently inhibits E2F4 DNA-binding at 40 µM, and increasingly suppressses the effect at 60 and 80 µM concentrations. HLM006474 (40 µM) inhibits E2F4 activity via suppression of its DNA-binding activity and down regulation of its expression. HLM006474 (40 µM) also significantly induces apoptosis in A375 and 231 cell lines for 24 hours. HLM006474 dramaticly reduces cyclin D3 protein expression, and is a potent inducer of PARP cleavage. HLM006474 reduces the viability of both SCLC and NSCLC lines with IC50 ranging from 15 to 75 µM. HLM006474 (60 µM) increases the expression of several known E2F-regulated genes after short treatments in H292 and H1299 cell lines. HLM006474 (20 µM) weakly synergizes with paclitaxel, but there is antagonism between HLM006474 and cisplatin and gemcitabine in H1299 cells. HLM006474 leads to a decrease in the mRNA levels of MAD2. Furthmore, HLM006474 apparently suppresses the increase of Mad2 protein and pRb-S780 signal but not the level of Skp2 protein in human lung cancer A549 cellss.
背景
分子式
C25H25N3O2
CAS号
353519-63-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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