An inhibitor of RUNX2-DNA binding
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Product Type

CADD522

Item No. 36679

Technical Information
Formal Name
3-[[(3,4-dichlorophenyl)amino]carbonyl]-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid
CAS Number
199735-88-1
Molecular Formula
C15H13Cl2NO3
Formula Weight
Purity
≥98%
A solid
DMF: 5 mg/mlDMSO: 2 mg/mlEthanol: 3 mg/mlPBS (pH 7.2): insol
λmax
211, 255 nm
SMILES
O=C(C1C2C=CC(C1C(NC3=CC=C(C(Cl)=C3)Cl)=O)C2)O
InChi Code
InChI=1S/C15H13Cl2NO3/c16-10-4-3-9(6-11(10)17)18-14(19)12-7-1-2-8(5-7)13(12)15(20)21/h1-4,6-8,12-13H,5H2,(H,18,19)(H,20,21)
InChi Key
YSDNWNOGHQYWPK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CADD522 is an inhibitor of RUNX family transcription factor 2 (RUNX2) binding to DNA.1 It inhibits RUNX2 binding to osteoblast-specific element 2 (OSE2) oligonucleotides in a cell-free assay, as well as inhibits RUNX2 enrichment on matrix metalloproteinase-13 (MMP-13) promoters in MCF-7 cells when used at concentrations ranging from 100 to 1,000 nM. CADD522 (50 µM) decreases clonogenic survival in a panel of nine breast cancer cell lines. It decreases the expression of the RUNX2 target genes and metastasis markers MMP-13 and VEGF in ectopic RUNX2-expressing T47D-RUNX2 and MCF-7-RUNX2 breast cancer cells. CADD522 (20 mg/kg, i.p.) reduces tumor volume and incidence in the MMTV-PyMT transgenic mouse model of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, M.S., Gernapudi, R., Choi, E.Y., et alCharacterization of CADD522, a small molecule that inhibits RUNX2-DNA binding and exhibits antitumor activity. Oncotarget. 8(41), 70916-70940 (2017).