ML-264 |
Catalog No.GC11307
One-Click Copy Product Info
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ML-264 is a novel selective Krüppel-like factor 5 (KLF5) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1550008-55-3
Sample solution is provided at 25 µL, 10mM.
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ML-264 is a novel selective Krüppel-like factor 5 (KLF5) inhibitor. ML-264 inhibits cancer cell proliferation. ML-264 downregulates KLF5/EGR1 expression. ML-264 alters cell cycle to inhibit proliferation. ML-264 is useful for studies on colorectal cancer and KLF5-related tumor mechanisms[1-4].
In vitro, HK-2 cells were treated with 5-20µM ML-264 for 24h. ML-264 aggravated TGF-β-induced apoptosis, aggravated TGF-β-induced fibrosis and G2/M phase cell cycle stalling[5]. Colorectal cancer cell lines and patient-derived colorectal cancer organoids were treated with 10µM ML-264 for 1-7 days. ML-264 decreased Bcl-2 expression, increased Bax expression, ncreased cleaved caspase-3 expression, promoted apoptosis, enhanced oxaliplatin-induced apoptotic response[6]. 143B and U2OS cells were treated with 0.5-2µM ML-264 for 24-96h. ML-264 inhibited cell migration, cell invasion, induced G0/G1 phase cell cycle arrest, inhibited cell proliferation, colony formation[7].
In vivo, nude mice subcutaneously inoculated with DLD-1 cells were intraperitoneally injected with 10-25mg/kg ML-264 twice daily for 10 days. ML-264 inhibited DLD-1 xenograft tumor growth and reduced mitotic figures[8]. BALB/c nude mice were intraperitoneally injected with 10mg/kg ML-264 every 2 days for 32 days. ML-264 inhibited A2780-olaR xenograft tumor growth, decreased Vimentin, KLF4, Ki-67 expression, enhanced Olaparib-induced tumor cell apoptosis[9]. C57BL/6 mice were administered ML-264 every 12h for 28 days starting 12h after permanent left coronary artery ligation. ML-264 improved ejection fraction, reduced ventricular volume, heart weight, early postoperative mortality[10].
References:[1] Bialkowska A, Crisp M, Madoux F, 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. 2011 Oct 31.
[2] Lu J, Hou Y, Liu SX, et al. 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. Cell Commun Signal. 2024 Mar 21;22(1):187.
[3] Bhargava D, Rusakow D, Zheng W, et al. KLF5 inhibition initiates epithelial-mesenchymal transition in non-transformed human squamous epithelial cells. Biochim Biophys Acta Mol Cell Res. 2024 Oct;1871(7):119789.
[4] Xie Z, Jie Z, Wang G, et al. TGF-β synergizes with ML264 to block IL-1β-induced matrix degradation mediated by Krüppel-like factor 5 in the nucleus pulposus. Biochim Biophys Acta Mol Basis Dis. 2018 Feb;1864(2):579-589.
[5] Lin L, Shen D, Su Y, et al. Magnesium Lithospermate B protects against ischemic AKI-to-CKD progression via regulating the KLF5/CDK1/Cyclin B1 pathway. Phytomedicine. 2025;142:156765.
[6] Shen X, Zhang Y, Xu Z, et al. KLF5 inhibition overcomes oxaliplatin resistance in patient-derived colorectal cancer organoids by restoring apoptotic response. Cell Death Dis. 2022;13:303.
[7] Huang H, Han Y, Chen Z, et al. ML264 inhibits osteosarcoma growth and metastasis via inhibition of JAK2/STAT3 and WNT/β-catenin signalling pathways. J Cell Mol Med. 2020;24(10):5652-5664.
[8] Ruiz de Sabando A, Wang C, He Y, et al. ML264, a novel small-molecule compound that potently inhibits growth of colorectal cancer. Mol Cancer Ther. 2016 Jan;15(1):72-83.
[9] Xiao H, Cheng G, Zhang H, et al. Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting. J Transl Med. 2025;23:492.
[10] Hoffman M, Palioura D, Kyriazis ID, et al. Cardiomyocyte Krüppel-like factor 5 promotes de novo ceramide biosynthesis and contributes to eccentric remodeling in ischemic cardiomyopathy. Circulation. 2021 Mar 16;143(11):1139-1156.
| Cell experiment [1]: | |
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Cell lines |
HK-2 cells (human proximal tubular epithelial cell line) |
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Preparation Method |
HK-2 cells were treated with ML-264 at 5µM, 10µM or 20µM together with TGF-β (10ng/mL) and Magnesium Lithospermate B (100µM) for 24h, then protein and RNA were harvested for Western blot, RT-qPCR and flow cytometry to assess fibrosis, apoptosis and G2/M cell cycle stalling. |
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Reaction Conditions |
5-20µM; 24h |
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Applications |
ML-264 intensified apoptosis, fibrosis and G2/M phase cell cycle stalling in TGF-β-stimulated HK-2 cells. ML-264 reduced CDK1/Cyclin B1 expression and reinstated G2/M phase cell cycle stalling. |
| Animal experiment [2]: | |
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Animal models |
BALB/c nude mice |
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Preparation Method |
DLD-1 human colorectal cancer cells were subcutaneously injected into the right flank of 6-7 week old male nude mice. When tumor volume reached about 100mm3, mice were intraperitoneally injected with ML-264 at 10mg/kg or 25mg/kg twice daily for 10 days. Tumors were excised for analysis of proliferation, histology and protein expression. |
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Dosage form |
10mg/kg or 25mg/kg; i.p.; twice daily; 10 days |
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Applications |
ML-264 inhibited DLD-1 xenograft tumor growth, reduced the number of mitotic figures and Ki-67 staining, increased vimentin-positive fibroblasts and Mac-3-positive mononuclear phagocytes, decreased KLF5 and EGR1 expression in tumor tissues. |
| References: [1] Lin L, Shen D, Su Y, et al. Magnesium Lithospermate B Protects Against Ischemic AKI-to-CKD progression via regulating the KLF5/CDK1/Cyclin B1 pathway. Phytomedicine. 2025;142:156765. [2] Ruiz de Sabando A, Wang C, He Y, et al. ML264, a novel small-molecule compound that potently inhibits growth of colorectal cancer. Mol Cancer Ther. 2016 Jan;15(1):72-83. | |
| Cas No. | 1550008-55-3 | SDF | |
| Chemical Name | (2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide | ||
| Canonical SMILES | ClC1=CC=CC(/C=C/C(NCC(N(C)C2CCS(CC2)(=O)=O)=O)=O)=C1 | ||
| Formula | C17H21ClN2O4S | M.Wt | 384.9 |
| Solubility | ≤10mg/ml in DMSO;15mg/ml in dimethyl formamide | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5981 mL | 12.9904 mL | 25.9808 mL |
| 5 mM | 519.6 μL | 2.5981 mL | 5.1962 mL |
| 10 mM | 259.8 μL | 1.299 mL | 2.5981 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)