Description
PRT4165 is a small molecule inhibitor of polycomb repressive complex 1, which inhibits ubiquitin signaling at DNA double-strand breaks. PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. The drug also inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs.
Product information
CAS Number: 31083-55-3
Molecular Weight: 235.24
Formula: C15H9NO2
Chemical Name: 2-(pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione
Smiles: O=C1C(=CC2=CN=CC=C2)C(=O)C2=CC=CC=C12
InChiKey: OMHZFEWYVFWVLI-UHFFFAOYSA-N
InChi: InChI=1S/C15H9NO2/c17-14-11-5-1-2-6-12(11)15(18)13(14)8-10-4-3-7-16-9-10/h1-9H
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
PRT4165 was used at 10-50 µM final concentration in various in vitro assays.
References:
- Alchanati I, et al. The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex - a potentially new drug target. (2009) PLoS One. 4(12):e8104.
- Ismail IH, et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. (2013) J Biol Chem. 288(37):26944-54.
Products are for research use only. Not for human use.
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