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How to Cite 1. For In-Text Citation (Materials & Methods): 2. For Key Resources Table: |
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| Formula | C17H21ClN2O4S |
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| Molecular Weight | 384.88 | CAS No. | 1550008-55-3 | ||||
| Solubility (25°C)* | In vitro | DMSO | 200 mg/mL (519.64 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| In vivo (Add solvents to the product individually and in order) |
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* <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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| Description | ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5),potently Inhibits Growth of Colorectal Cancer. | ||
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| In vitro | ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. This compound 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.This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile. | ||
| 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 this compound potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5. |
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| Krüppel-like factor 5 promotes the progression of oral squamous cell carcinoma via the baculoviral IAP repeat containing 5 gene [ Annals of Translational Medicine, September 2022, 969] | PubMed: 36267746 |
| Histone methyltransferase GLP epigenetically activates GPCPD1 to sustain cancer cell metastasis and invasion [ Genome Instability & Disease, September 2022, 21-37] | |
| 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 [ Journal of Neuroscience, December 5, 2018, 10535-10551] | PubMed: 30373770 |
| 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 [ Journal of Neuroscience, December 05, 2018, 10535-10551] | PubMed: 30373770 |
| Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting [ Journal of Translational Medicine, April 30, 2025, 492] | PubMed: 40307891 |
| KLF5 loss sensitizes cells to ATR inhibition and is synthetic lethal with ARID1A deficiency [ Nat Commun, 2025, 16(1):480] | PubMed: 39779698 |
| Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting [ J Transl Med, 2025, 23(1):492] | PubMed: 40307891 |
| Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting [ Journal of Translational Medicine, 2025, 492] | PubMed: 40307891 |
| 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 activatesGPCPD1to sustain cancer cell metastasis and invasion [ Genome Instability & Disease, 2023, 4, 21–37] | PubMed: None |
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