An activator of KLF4
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LOR253

Item No. 36773

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(5-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
CAS Number
916151-99-0
Synonyms
  • APTO-253
Molecular Formula
C22H14FN5
Formula Weight
367.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/ml
λmax
230, 262, 284 nm
SMILES
FC1=CC2=C(NC(C)=C2C3=NC4=C(N3)C5=C(N=CC=C5)C6=C4C=CC=N6)C=C1
InChi Code
InChI=1S/C22H14FN5/c1-11-17(15-10-12(23)6-7-16(15)26-11)22-27-20-13-4-2-8-24-18(13)19-14(21(20)28-22)5-3-9-25-19/h2-10,26H,1H3,(H,27,28)
InChi Key
NIRXBXIPHUTNNI-UHFFFAOYSA-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

    $306

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    25 mg

    $538

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    Cayman Chemical
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    Product Description

    LOR253 is an activator of the transcription factor Kruppel-like factor 4 (KLF4).1 It increases levels of KLF4 and induces apoptosis in HCC1187, HCC38, and MDA-MB-468 cancer cells when used at concentrations of 5 and 10 µM. It is cytotoxic in a panel of 16 acute myeloid leukemia (AML) and lymphoma cell lines (IC50s = 0.057-1.75 µM) and induces cell cycle arrest at the G0/G1 phase in MV4-11, KG-1, and EoL-1 cells.2 LOR253 (1 mg/kg) accelerates wound healing, as well as increases plasma levels of KLF4 and wound site myeloid-derived suppressor cell (MDSC) accumulation, in an ob/ob mouse model of diabetic wound healing.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakajima, W., Miyazaki, K., Asano, Y., et al. Krüppel-like factor 4 and its activator APTO-253 induce NOXA-mediated, p53-independent apoptosis in triple-negative breast cancer cells. Genes (Basel) 12(4), 539 (2021).

    2. Local, A., Zhang, H., Benbatoul, K.D., et al. APTO-253 stabilizes G-quadruplex DNA, inhibits MYC expression, and induces DNA damage in acute myeloid leukemia cells. Mol. Cancer Ther. 17(6), 1177-1186 (2018).

    3. Yang, X., Mathis, B.J., Huang, Y., et al. KLF4 promotes diabetic chronic wound healing by suppressing Th17 cell differentiation in an MDSC-dependent manner. J. Diabetes Res. 7945117 (2021).