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HLM006474
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HLM006474图片
CAS NO:353519-63-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
HLM006474 是光谱的E2F抑制剂,在 A375 细胞中,可抑制 E2F4 DAN 结合(IC50:29.8 μM)。

产品描述

HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).

体外活性

HLM006474 causes the viability of both SCLC and NSCLC lines (IC50 ranging from 15 to 75 μM). HLM006474 displays little activities against E2F4 DNA-binding in A375 cells at 10 and 20 μM, apparently inhibits E2F4 DNA-binding at 40 μM, and increasingly suppresses the effect at 60 and 80 μM concentrations. HLM006474 dramatically causes cyclin D3 protein expression and is a potent inducer of PARP cleavage[1]. HLM006474 (20 μM) weakly synergizes with paclitaxel, but there is antagonism between HLM006474 and cisplatin and gemcitabine in H1299 cells[2]. HLM006474 (40 μM) inhibits E2F4 activity via suppression of its DNA-binding activity and down regulation of its expression and HLM006474 (40 μM) also obviously causes apoptosis in A375 and 231 cell lines for 24 hours. HLM006474 (60 μM) enhances the expression of several known E2F-regulated genes after short treatments in H292 and H1299 cell lines. HLM006474 leads to a reduction in the mRNA levels of MAD2. 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.

Cas No.

353519-63-8

分子式

C25H25N3O2

分子量

399.48

储存和溶解度

DMSO:24 mg/mL (60.08 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years