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HLM006474

Catalog No. T15486 CAS 353519-63-8

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

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HLM006474, CAS 353519-63-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 88.00
25 mg	In stock	$ 166.00
50 mg	In stock	$ 296.00
100 mg	In stock	$ 490.00
500 mg	In stock	$ 1,090.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.04%

Purity: 98.45%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Molecular Weight	399.48
Formula	C25H25N3O2
CAS No.	353519-63-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 24 mg/mL (60.08 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Apoptosis Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

HLM006474 353519-63-8 Others inhibit Early 2 Factor (E2F) HLM-006474 Inhibitor HLM 006474 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.