ML264
Based on 16 publication(s) in Google Scholar
ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 1550008-55-3
- Formula: C17H21ClN2O4S
- Molecular Weight:384.88
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML264
More- Cancer Res. 2022 Apr 15;82(8):1575-1588. [Abstract]
- Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
- Redox Biol. 2024 Sep:75:103246. [Abstract]
- Sci Adv. 2025 Dec 12;11(50):eaea9074. [Abstract]
- Cell Death Dis. 2025 Jan 18;16(1):28. [Abstract]
- Cell Commun Signal. 2024 Mar 21;22(1):187. [Abstract]
- Int J Surg. 2025 Oct 7. [Abstract]
- Alzheimers Res Ther. 2022 Jul 26;14(1):103. [Abstract]
- PLoS Biol. 2020 Aug 20;18(8):e3000808. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2019 Sep 1;1865(9):2490-2503. [Abstract]
- J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]
- Cell Cycle. 2021 May;20(9):874-893. [Abstract]
- Cell Biol Int. 2022 Sep;46(9):1519-1529. [Abstract]
- Hum Cell. 2025 Feb 8;38(2):51. [Abstract]
- J Pharm Innov. 2026 May 16;21(5):522.
- J Pediatr Surg. 2022 Sep;57(9):192-201. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biological Activity
KLF5[1]
ML264 is highly active (IC50=29 nM is a cell-based assay for proliferation of DLD-1 cells, IC50=81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC50>50 μM, <50% inhibition is observed at 100 μM). Robust activity is also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC50=560 nM; HT29, IC50=130 nM; SW620, IC50=430 nM). Western blot analysis shows that ML264 significantly reduces KLF5 expression[1]. The effects of ML264 are tested on the rate of cell proliferation of colon cancer cells lines DLD-1 and HCT116 over 72 hours. ML264 efficiently inhibits the rate of proliferation of both cell lines. A significant decrease in proliferation is evident within 24 hours of treatment and by 72 hours the live cell numbers of ML264-treated and vehicle-treated cells differed by 15- to 30- fold. An MTS assay that allows the quantification of metabolically active cells is performed. ML264 treatment significantly reduces the number of cells undergoing mitosis in DLD-1 cells at 24, 48 and 72 hours[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1550008-55-3
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Appearance Solid
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Molecular Weight 384.88
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Formula C17H21ClN2O4S
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Color White to off-white
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SMILES
O=C(NCC(N(C)C(CC1)CCS1(=O)=O)=O)/C=C/C2=CC=CC(Cl)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Cancer Res
Ketogenesis Attenuates KLF5-Dependent Production of CXCL12 to Overcome the Immunosuppressive Tumor Microenvironment in Colorectal Cancer. [Abstract]2022 Apr 15;82(8):1575-1588. PMID: 35247887 -
Protein Cell
Integrative analysis of transcriptome, DNA methylome and chromatin accessibility reveals candidate therapeutic targets in hypertrophic cardiomyopathy. [Abstract]2024 Nov 1;15(11):796-817. PMID: 38780967
ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
ML264 (20 mg/kg; i.p.; every other day for 4-6 weeks) significantly alleviated the HCM phenotypes, as shown by a marked reduction in LVPWd thickness in the treated HCM mice compared to that in the untreated HCM (hypertrophic cardiomyopathy) mice.
ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
ML264 (20 mg/kg; i.p.; every other day) significantly decreased the cardiomyocyte cross-sectional area in HCM (hypertrophic cardiomyopathy) mice.
ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
ML264 (20 mg/kg; i.p.; every other day) significantly reduced myocardial fibrosis in HCM (hypertrophic cardiomyopathy) mice.
ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
The transcriptomes of the HCM (hypertrophic cardiomyopathy) mice treated with ML264 (20 mg/kg; i.p.; every other day) were more similar to those of the WT mice than those of the untreated mutants.
ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 Nov 1;15(11):796-817. [Abstract]
ML264 (20 mg/kg; i.p.; every other day) reversed 74 of 88 (84%) co-upregulated DEGs and 217 of 275 (79%) co-downregulated DEGs in HCM (hypertrophic cardiomyopathy) mice.
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Redox Biol
Lactate drives epithelial-mesenchymal transition in diabetic kidney disease via the H3K14la/KLF5 pathway. [Abstract]2024 Sep:75:103246. PMID: 38925041 -
Sci Adv
HERVH-derived eRNA activates a super-enhancer-driven ALDH1A3/SAT1 axis to promote ferroptosis escape and pancreatic cancer development. [Abstract]2025 Dec 12;11(50):eaea9074. PMID: 41370380 -
Cell Death Dis
Inhibition of KLF5 promotes ferroptosis via the ZEB1/HMOX1 axis to enhance sensitivity to oxaliplatin in cancer cells. [Abstract]2025 Jan 18;16(1):28. PMID: 39827156 -
Cell Commun Signal
Acetyl-CoA synthetase 2 induces pyroptosis and inflammation of renal epithelial tubular cells in sepsis-induced acute kidney injury by upregulating the KLF5/NF-κB pathway. [Abstract]2024 Mar 21;22(1):187. PMID: 38515158 -
Int J Surg
Potential regulators and metabolic networks of muscle fatty infiltration: genomic and radiomics investigation based on 33 300 participants. [Abstract]2025 Oct 7. PMID: 41056018 -
Alzheimers Res Ther
Krüppel-like factor 5 accelerates the pathogenesis of Alzheimer's disease via BACE1-mediated APP processing. [Abstract]2022 Jul 26;14(1):103. PMID: 35883144 -
PLoS Biol
Klf5 down-regulation induces vascular senescence through eIF5a depletion and mitochondrial fission. [Abstract]2020 Aug 20;18(8):e3000808. PMID: 32817651 -
Biochim Biophys Acta Mol Basis Dis
EGR1 promotes the cartilage degeneration and hypertrophy by activating the Krüppel-like factor 5 and β-catenin signaling. [Abstract]2019 Sep 1;1865(9):2490-2503. PMID: 31201921 -
J Mol Cell Cardiol
Induction of GLI1 by miR-27b-3p/FBXW7/KLF5 pathway contributes to pulmonary arterial hypertension. [Abstract]2022 Oct:171:16-29. PMID: 35810662 -
Cell Cycle
Promoting roles of KLF5 in myocardial infarction in mice involving microRNA-27a suppression and the following GFPT2/TGF-β/Smad2/3 axis activation. [Abstract]2021 May;20(9):874-893. PMID: 33910455 -
Cell Biol Int
2022 Sep;46(9):1519-1529. PMID: 35731168 -
Hum Cell
The miR-1305/KLF5 negative regulatory loop affects pancreatic cancer cell proliferation and apoptosis. [Abstract]2025 Feb 8;38(2):51. PMID: 39921786 -
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J Pediatr Surg
KLF5 promotes KIF1A expression through transcriptional repression of microRNA-338 in the development of pediatric neuroblastoma. [Abstract]2022 Sep;57(9):192-201. PMID: 35033353
Solvent & Solubility
DMSO : ≥ 100 mg/mL (259.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (25.98 mM); Suspended solution; Need ultrasonic
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.
Protocol
For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter. Each experiment is done in triplicate. In MTS assay, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution is added to each well and an analysis is performed. The measurement of the control (cells with medium and DMSO) is defined as 100% and the results from other measurements are calculated accordingly. Each experiment is done in sextuplicate. A cell cycle progression assay is performed. Each experiment is done in triplicate. The apoptosis rate is determined using the Alexa Fluor 488 Annexin V/Dead Cell Apoptosis Kit with analysis by flow cytometry. Each experiment is done in triplicate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Nude mice are housed under specific pathogen-free conditions in ventilated and filtered cages under positive pressure. Xenograft tumors are generated by injecting subcutaneously 5×106 DLD-1 human colorectal cells into the right flank of 6-7 week old male nude mice. Tumor volume is determined by caliper measurement and calculated by established methods. When tumors reach a volume of about 100 mm6, mice are treated intraperitoneally (i.p.) with varying doses of ML264: 10 mg/kg daily, 10 mg/kg twice per day and 25 mg/kg twice per day, with each treatment regimen lasting for a duration of 10 days. The vehicle solution is used as the control treatment. Mice are monitored and weighed every two days. Experiments are terminated when the tumor’s greatest measurement reaches 2 cm. Tumors are excised and retained for further analyses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bialkowska A, et al. ML264: An Antitumor Agent that Potently and Selectively Inhibits Krüppel-like Factor Five (KLF5) Expression: A Probe for Studying Colon Cancer Development and Progression. [Content Brief]
[2]. Ruiz de Sabando A, et al. ML264, A Novel Small-Molecule Compound That Potently Inhibits Growth of Colorectal Cancer. Mol Cancer Ther. 2016 Jan;15(1):72-83. [Content Brief]
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 | 2.5982 mL | 12.9911 mL | 25.9821 mL | 64.9553 mL |
| 5 mM | 0.5196 mL | 2.5982 mL | 5.1964 mL | 12.9911 mL | |
| 10 mM | 0.2598 mL | 1.2991 mL | 2.5982 mL | 6.4955 mL | |
| 15 mM | 0.1732 mL | 0.8661 mL | 1.7321 mL | 4.3304 mL | |
| 20 mM | 0.1299 mL | 0.6496 mL | 1.2991 mL | 3.2478 mL | |
| 25 mM | 0.1039 mL | 0.5196 mL | 1.0393 mL | 2.5982 mL | |
| 30 mM | 0.0866 mL | 0.4330 mL | 0.8661 mL | 2.1652 mL | |
| 40 mM | 0.0650 mL | 0.3248 mL | 0.6496 mL | 1.6239 mL | |
| 50 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2991 mL | |
| 60 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0826 mL | |
| 80 mM | 0.0325 mL | 0.1624 mL | 0.3248 mL | 0.8119 mL | |
| 100 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6496 mL |
ML264 Related Classifications
HY-19994 Related Classifications
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