HLM006474
Based on 10 publication(s) in Google Scholar
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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- Pureza: 98.44%
- No. CAS: 353519-63-8
- Fòrmula: C25H25N3O2
- Peso molecular:399.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
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Publications Citing Use of MedChemExpress (MCE) HLM006474
More- Cancer Res. 2026 Mar 5. [Abstract]
- Nat Commun. 2025 Mar 6;16(1):2239. [Abstract]
- Adv Sci (Weinh). 2025 Nov 30:e14349. [Abstract]
- Int J Biol Sci. 2024 Sep 16;20(12):4978-4998. [Abstract]
- J Transl Med. 2019 Nov 11;17(1):366. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- iScience. 2025 Jan 20;28(2):111853. [Abstract]
- Cell Signal. 2022 Apr:92:110265. [Abstract]
- J Gastroenterol Hepatol. 2025 Apr;40(4):1004-1015. [Abstract]
- bioRxiv. 2024 June 27.
Actividad biológica
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 353519-63-8
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Appearance Solid
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Peso molecular 399.48
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Fòrmula C25H25N3O2
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Color White to off-white
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SMILES
OC(C1=NC(C)=CC=C1C=C2)=C2C(NC3=NC=CC=C3)C(C=C4C)=CC=C4OCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Res
METTL3 Methylation Induces Decay of Endogenous Retroelement Transcripts to Promote Tumor Immune Evasion. [Abstract]2026 Mar 5. PMID: 41784625 -
Nat Commun
Oxidative phosphorylation is a key feature of neonatal monocyte immunometabolism promoting myeloid differentiation after birth. [Abstract]2025 Mar 6;16(1):2239. PMID: 40050264 -
Adv Sci (Weinh)
Microcystin-LR Triggers Renal Tubular Ferroptosis Through Epigenetic Repression of GPX4: Implications for Environmental Nephrotoxicity. [Abstract]2025 Nov 30:e14349. PMID: 41319283 -
Int J Biol Sci
Transcription Factor E2F4 Promote Proliferation, Migration, and Invasion of Gastric Cancer Cells by transcriptionally activating DSCC1. [Abstract]2024 Sep 16;20(12):4978-4998. PMID: 39309429 -
J Transl Med
HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia. [Abstract]2019 Nov 11;17(1):366. PMID: 31711520 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
iScience
A human-specific, concerted repression of microcephaly genes contributes to radiation-induced growth defects in cortical organoids. [Abstract]2025 Jan 20;28(2):111853. PMID: 39967878 -
Cell Signal
NCAPD3 promotes prostate cancer progression by up-regulating EZH2 and MALAT1 through STAT3 and E2F1. [Abstract]2022 Apr:92:110265. PMID: 35085770 -
J Gastroenterol Hepatol
Clonorchis sinensis Promotes Intrahepatic Cholangiocarcinoma Progression by Activating FASN-Mediated Fatty Acid Metabolism. [Abstract]2025 Apr;40(4):1004-1015. PMID: 39806791 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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