ML264

Catalog No.S8196 Batch:S819602

Technical Data

Formula	C₁₇H₂₁ClN₂O₄S
Molecular Weight	384.88	CAS No.	1550008-55-3
Solubility (25°C)*	In vitro	DMSO	77 mg/mL (200.06 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5),potently Inhibits Growth of Colorectal Cancer.

Targets

KLF5 ^[1]
(Cell-based assay for proliferation of DLD-1 cells)

29 nM

In vitro

ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. ML264 has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose^[1].This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile^[2].

In vivo

In an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. this effect is caused by a significant reduction in proliferation and that ML264 potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines DLD-1 and HCT116 colorectal cancer cell lines Concentrations 10μM Incubation Time 24, 48, 72h Method For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10μM 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; In MTS assay, DLD-1 and HCT116 cells are treated with 10μM 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 according to the manufacturer's protocol.
Animal Study:^{^[2]}	Animal Models Nude mice with DLD-1 cells injection to achieve a tumor Dosages 10 or 25 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
DLD-1 and HCT116 colorectal cancer cell lines
Concentrations
10μM
Incubation Time
24, 48, 72h
Method
For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10μM 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; In MTS assay, DLD-1 and HCT116 cells are treated with 10μM 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 according to the manufacturer's protocol.

Animal Study:^{^[2]}

Animal Models
Nude mice with DLD-1 cells injection to achieve a tumor
Dosages
10 or 25 mg/kg
Administration
i.p.

References

Selleck's ML264 has been cited by 8 publications

Heterogeneity-driven phenotypic plasticity and treatment response in branched-organoid models of pancreatic ductal adenocarcinoma [ Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9]	PubMed: 39658630
Histone methyltransferase GLP epigenetically activates GPCPD1 to sustain cancer cell metastasis and invasion [ Genome Instability & Disease , 2023, 4:21–37 ]	PubMed: none
Krüppel-like factor 5 promotes the progression of oral squamous cell carcinoma via the baculoviral IAP repeat containing 5 gene [ Ann Transl Med, 2022, 10(18):969]	PubMed: 36267746
Oxidative Stress-Induced Hypermethylation of KLF5 Promoter Mediated by DNMT3B Impairs Osteogenesis by Diminishing the Interaction with β-Catenin [ Antioxid Redox Signal, 2021, 10.1089/ars.2020.8200]	PubMed: 33588625
Nucleotide variation in histone H2BL drives crossalk of histone modification and promotes tumour cell proliferation by upregulating c-Myc [ Life Sci, 2021, 271:119127]	PubMed: 33515561
Long intergenic noncoding RNA 00908 promotes proliferation and inhibits apoptosis of colorectal cancer cells by regulating KLF5 expression [ J Cell Physiol, 2021, 236(2):889-899]	PubMed: 33020901
Long intergenic noncoding RNA 00908 promotes proliferation and inhibits apoptosis of colorectal cancer cells by regulating KLF5 expression [ J Cell Physiol, 2021, 236(2):889-899]	PubMed: 33020901
Demethylation of G-Protein-Coupled Receptor 151 Promoter Facilitates the Binding of Krüppel-Like Factor 5 and Enhances Neuropathic Pain after Nerve Injury in Mice [ J Neurosci, 2018, 38(49):10535-10551]	PubMed: 30373770

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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