HRO761 | WRN helicase allosteric inhibitor

CAS:
 2869954-34-5
Catalog Number:
 10-3981
HRO761 chemical structure

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HRO761 (2869954-34-5) is a potent (IC50 = 9 nM), selective, non-covalent, and allosteric inhibitor of Werner syndrome RecQ helicase (WRN).1  It binds to the D1 and D2 helicase domain interface locking it into the inactive state.  HRO761 selectively inhibits microsatellite instabile (MSI) cancer cells in vitro and in vivo via double-stranded DNA breaks, activation of the DDR, and induction of WRN degradation. It displayed synergistic effects with irinotecan in colorectal cancer cells.

References/Citations:

  1. Ferretti et al. (2024) Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers; Nature 629 443
2869954-34-5, allosteric WRN helicase inhibitor, HR0761, HRO-761, HRO761, HRO761 supplier, non-covalent WRN helicase inhibitor, WRN-helicase inhibitor
CAS:
2869954-34-5
Catalog Number:
10-3981
Activity:
WRN helicase inhibitor
Chemical Names:
N-[2-Chloro-4-(trifluoromethyl)phenyl]-2-[2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-6-[4-(5-hydroxy-6-methylpyrimidine-4-carbonyl)piperazin-1-yl]-7-oxo-[1,2,4]triazolo[1,5-a]pyrimidin-4-yl]acetamide
Molecular Weight:
702.09
Molecular Formula:

C31H31ClF3N9O5

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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HRO761 (2869954-34-5) is a potent (IC50 = 9 nM), selective, non-covalent, and allosteric inhibitor of Werner syndrome RecQ helicase (WRN).1  It binds to the D1 and D2 helicase domain interface locking it into the inactive state.  HRO761 selectively inhibits microsatellite instabile (MSI) cancer cells in vitro and in vivo via double-stranded DNA breaks, activation of the DDR, and induction of WRN degradation. It displayed synergistic effects with irinotecan in colorectal cancer cells.

References/Citations:

  1. Ferretti et al. (2024) Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers; Nature 629 443

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