HLM006474 |
Catalog No.GC36236
One-Click Copy Product Info
|
An E2F inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 353519-63-8
Sample solution is provided at 25 µL, 10mM.
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HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells. IC50: 29.8 µM (E2F4 DNA-binding)[1]
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[1]. 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[2]. 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[3].
[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.
Cell experiment: | The antiproliferative activity of compounds and their combinations is evaluated using a high-throughput CellTiter-Blue cell viability assay. For the assays, 1000 cells in 24 µL are plated in 384-well plates and incubated overnight at 37°C, 5% CO2. The next day, the drugs are diluted in media and 6 µL of these dilutions added to appropriate wells using an automated pipetting station. Four replicate wells are used for each drug concentration. The cells are incubated with the drug for 120 hours, at which time, 5 µL CellTiter-Blue reagent is added. Cell viability is assessed by the ability of the remaining treated cells to bioreduce resazurin to resorufin (579 nm Ex/584 nm Em). Fluorescence is read with a Synergy HT microplate reader. IC50s are determined using a sigmoidal equilibrium model regression using XLfit version 4.3.2 and is defined as the concentration of drug required for a 50% reduction in growth/viability. For 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays, CellTiter 96 AQueous One Solution is added according to vendor instructions to cells for 2 hours following treatment with drug at the noted dose for 72 hours. All experiments are performed in triplicate and repeated at least three times[2]. |
References: [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. | |
| Cas No. | 353519-63-8 | SDF | |
| Canonical SMILES | OC(C1=NC(C)=CC=C1C=C2)=C2C(NC3=NC=CC=C3)C(C=C4C)=CC=C4OCC | ||
| Formula | C25H25N3O2 | M.Wt | 399.48 |
| Solubility | DMSO: 25 mg/mL (62.58 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL |
| 5 mM | 500.7 μL | 2.5033 mL | 5.0065 mL |
| 10 mM | 250.3 μL | 1.2516 mL | 2.5033 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)