2. Cell Cycle/DNA Damage
  3. Early 2 Factor (E2F)
  4. HLM006474

HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.

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HLM006474 Chemical Structure

HLM006474 Chemical Structure

CAS No. : 353519-63-8

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Customer Review

Based on 5 publication(s) in Google Scholar

HLM006474 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.

IC50 & Target

IC50: 29.8 µM (E2F4 DNA-binding)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HLM006474 Related Antibodies
Molecular Weight

399.48

Formula

C25H25N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1=NC(C)=CC=C1C=C2)=C2C(NC3=NC=CC=C3)C(C=C4C)=CC=C4OCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (41.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5033 mL 12.5163 mL 25.0325 mL
5 mM 0.5007 mL 2.5033 mL 5.0065 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.26 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.57%

COA (253 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5033 mL 12.5163 mL 25.0325 mL 62.5814 mL
5 mM 0.5007 mL 2.5033 mL 5.0065 mL 12.5163 mL
10 mM 0.2503 mL 1.2516 mL 2.5033 mL 6.2581 mL
15 mM 0.1669 mL 0.8344 mL 1.6688 mL 4.1721 mL
20 mM 0.1252 mL 0.6258 mL 1.2516 mL 3.1291 mL
25 mM 0.1001 mL 0.5007 mL 1.0013 mL 2.5033 mL
30 mM 0.0834 mL 0.4172 mL 0.8344 mL 2.0860 mL
40 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5645 mL
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HLM006474 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HLM006474353519-63-8HLM 006474HLM-006474Early 2 Factor (E2F)Inhibitorinhibitorinhibit

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