A selective KLF5 inhibitor
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ML-264

Item No. 18880

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide
CAS Number
1550008-55-3
Molecular Formula
C17H21ClN2O4S
Formula Weight
384.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 10 mg/ml
λmax
219, 268 nm
SMILES
ClC1=CC=CC(/C=C/C(NCC(N(C)C2CCS(CC2)(=O)=O)=O)=O)=C1
InChi Code
InChI=1S/C17H21ClN2O4S/c1-20(15-7-9-25(23,24)10-8-15)17(22)12-19-16(21)6-5-13-3-2-4-14(18)11-13/h2-6,11,15H,7-10,12H2,1H3,(H,19,21)/b6-5+
InChi Key
AJCDZIDKYKCOMZ-AATRIKPKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    ML-264 is a selective inhibitor of Krüppel-like factor 5 (KLF5), a zinc finger-containing transcription factor that is highly expressed in rapidly dividing intestinal epithelial cells. It displays an IC50 value of 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells and an IC50 value of 81 nM in a cell-based luciferase assay but does not inhibit kinases associated with the KLF5 pathway, as determined using a panel of 47 selected kinases.1 ML-264 induces death in most colon cancer cell lines (HCT116, IC50 = 560 nM; HT-29, IC50 = 130 nM; SW620, IC50 = 430 nM), with cytotoxicity toward an established xenograft mouse model of colon cancer as well.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bialkowska, A., Crisp, M., Maddoux, 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. Probe Reports from the NIH Molecular Libraries Program (2011).

    2. de Sabando, A.R., Wang, C., He, Y., et al. ML264, a novel small-molecule compound that potently inhibits growth of colorectal cancer. Mol. Cancer Ther. 15(1), 72-83 (2016).