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HLM006474

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Chemical Structure| 353519-63-8 同义名 : -
CAS号 : 353519-63-8
货号 : A631764
分子式 : C25H25N3O2
纯度 : 98+%
分子量 : 399.485
MDL号 : MFCD02168344
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(40.05 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 HLM006474 exhibits minimal activity against E2F4 DNA-binding in A375 cells at lower doses (10 and 20 µM), but clearly inhibits E2F4 DNA-binding at higher concentrations (40 µM and above), progressively increasing its suppressive effect at 60 and 80 µM. At 40 µM, HLM006474 hinders E2F4 activity by both blocking its DNA-binding capability and reducing its expression levels. This concentration also significantly triggers apoptosis in A375 and 231 cell lines within 24 hours, significantly cuts down cyclin D3 protein levels, and effectively induces PARP cleavage, demonstrating its potential as a potent apoptotic inducer[1]. HLM006474 reduces the viability of both small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC) lines, with IC50 values ranging between 15 and 75 µM. At 60 µM, it boosts the expression of several E2F-regulated genes after brief exposures in H292 and H1299 cell lines. Although HLM006474 (20 µM) exhibits slight synergistic effects with paclitaxel, it shows antagonistic interactions with cisplatin and gemcitabine in H1299 cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL
参考文献

[1]Ma Y, et al. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9.

[2]Kurtyka CA, et al. E2F inhibition synergizes with paclitaxel in lung cancer cell lines. PLoS One. 2014 May 15;9(5):e96357.