1104546-89-5

1104546-89-5 structure

Name: BYK204165
Chemical Name: (4Z)-4-[(1-Methyl-1H-pyrrol-2-yl)methylene]-1,3(2H,4H)-isoquinoli nedione
CAS Number: 1104546-89-5
Molecular Formula: C₁₅H₁₂N₂O₂
Molecular Weight: 252.26800
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2016-06-09 06:51:53
Modify Date: 2024-01-15 22:49:34
BYK204165 is a potent PARP inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1[1].

Name	(4Z)-4-[(1-Methyl-1H-pyrrol-2-yl)methylene]-1,3(2H,4H)-isoquinoli nedione
Synonyms	4-(1-methyl-1H-pyrrol-2-ylmethylene)-4H-isoquinolin-1,3-dione

Description	BYK204165 is a potent PARP inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> PARP Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
Target	hPARP-1:7.35 (pIC50) mPARP-2:5.38 (pIC50)
In Vitro	In kinetic experiments with human PARP-1, BYK204165 exhibits potent and competitive inhibition of enzyme activity, yielding a pKi value of 7.05[1]. BYK204165 exhibits low potency of PARP inhibition in C4I cells (pIC50 of 5.75)[1].
In Vivo	BYK204165 is not investigated in vivo because of its short half-time (t1/2) of 23 min measured at rat microsomes in vitro[1].
References	[1]. Eltze 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 Dec;74(6):1587-98.

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H317
Precautionary Statements	P280
Hazard Codes	Xi
RIDADR	NONH for all modes of transport