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BYK 204165PARP-1 inhibitor,potent and selective

BYK 204165

Catalog No. A4525
Size Price Stock Qty
10mg $171.00 In stock
50mg $721.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BYK 204165

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Chemical Properties

Cas No. 1104546-89-5 SDF Download SDF
Chemical Name (4E)-4-[(1-methylpyrrol-2-yl)methylidene]isoquinoline-1,3-dione
Canonical SMILES CN1C=CC=C1C=C2C3=CC=CC=C3C(=O)NC2=O
Formula C15H12N2O2 M.Wt 252.27
Solubility Soluble in DMSO > 10 mM Storage Desiccate at 4°C
General tips N/A
Shipping Condition N/A

Background

BYK 204165 is a potent and selective poly(ADP-ribose) polymerase (PARP)-1 inhibitor with pIC50 values of 5.38 and 7.35 for PARP-2 and PARP-1 respectively [1].
PARP1 is a nuclear enzyme activated by strand breaks in DNA and involved in the regulation of various cell processes such as DNA repair, apoptosis, organ dysfunction or necrosis [1].
BYK 204165 (PARP inhibitor XIV) is a cell-permeable isoquinolinedione compound that potently and selectively inhibits PARP1. BYK 204165’s potency is similar or higher than most current standard PARP-1 inhibitors (just slightly lower than PJ34), and it is 100-fold selective for PARP-1 over PARP-2 [1].
BYK 204165 was not tested in vivo because of BYK its poor water solubility.
References:
[1]. Eltze T, Boer R, Wagner T, et al. Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. Mol Pharmacol, 2008, 74(6): 1587-98.