An inhibitor of homology-dependent DNA repair
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YU238259

Item No. 25452

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(5-chloro-2-pyridinyl)ethyl]-4-[[[(4-methoxyphenyl)sulfonyl]amino]methyl]-benzamide
CAS Number
1943733-16-1
Molecular Formula
C22H22ClN3O4S
Formula Weight
459.9
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
239 nm
SMILES
ClC1=CC=C(CCNC(C2=CC=C(CNS(C3=CC=C(OC)C=C3)(=O)=O)C=C2)=O)N=C1
InChi Code
InChI=1S/C22H22ClN3O4S/c1-30-20-8-10-21(11-9-20)31(28,29)26-14-16-2-4-17(5-3-16)22(27)24-13-12-19-7-6-18(23)15-25-19/h2-11,15,26H,12-14H2,1H3,(H,24,27)
InChi Key
BIHURSOREGLQBB-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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    10 mg

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    25 mg

    $631

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    Cayman Chemical
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    Product Description

    YU238259 is an inhibitor of homology-dependent DNA repair (HDR) that is lethal to BRCA2-/- but not BRCA2+/+ PEO1/4 cells (LD50s = 8.7 and >100 μM, respectively).1 YU238259 selectively inhibits HDR over non-homologous end joining (NHEJ), decreasing the number of U20S cells with ionizing radiation-induced BRCA1 foci but not 53BP1 or pDNA-PK foci. It also increases the number of ionizing radiation-induced double strand breaks (DSBs) in DLD-1 cells. YU238259 (1-20 μM) is cytotoxic to BRCA2-/- DLD-1, ATM-/- GM05849, and PTEN-/- U251 cells but has no effect on wild-type cells. In vivo, YU238259 (3 mg/kg) delays tumor growth and increases survival in a BRCA2-/-, but not a BRCA+/+, DLD-1 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stachelek, G.C., Peterson-Roth, E., Liu, Y., et al. YU238259 Is a novel inhibitor of homology-dependent DNA repair that exhibits synthetic lethality and radiosensitization in repair-deficient tumors. Mol. Cancer Res. 13(10), 1389-1397 (2015).