An inhibitor of homology-dependent DNA repair; lethal to BRCA2-/- but not BRCA2+/+ PEO1/4 cells (LD50s = 8.7 and >100 μM

YU238259 – 1 mg

Brand:
Cayman
CAS:
1943733-16-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{42297} 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.  

 

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SKU: 25452 - 1 mg Category:

Description

An inhibitor of homology-dependent DNA repair; lethal to BRCA2-/- but not BRCA2+/+ PEO1/4 cells (LD50s = 8.7 and >100 μM, respectively); selectively inhibits HDR over NHEJ; decreases the number of U20S cells with ionizing radiation-induced BRCA1 foci but not 53BP1 or pDNA-PK foci; increases the number of ionizing radiation-induced DSBs in DLD-1 cells; cytotoxic to BRCA2-/- DLD-1, ATM-/- GM05849, and PTEN-/- U251 cells from 1-20 μM; delays tumor growth and increases survival in a BRCA2-/-, but not a BRCA+/+, DLD-1 mouse xenograft model at 3 mg/kg ,

Formal name: N-[2-(5-chloro-2-pyridinyl)ethyl]-4-[[[(4-methoxyphenyl)sulfonyl]amino]methyl]-benzamide

Synonyms: 

Molecular weight: 459.9

CAS: 1943733-16-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair

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