BYK204165

Names

[ Name ]:
BYK204165

[Synonym ]:
4-(1-methyl-1H-pyrrol-2-ylmethylene)-4H-isoquinolin-1,3-dione

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₅H₁₂N₂O₂

[ Molecular Weight ]:
252.26800

[ Exact Mass ]:
252.09000

[ PSA ]:
54.59000

[ LogP ]:
1.84610

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H317

[ Precautionary Statements ]:
P280

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Articles

Alternative NHEJ Pathway Components Are Therapeutic Targets in High-Risk Neuroblastoma.

Mol. Cancer Res. 13(3) , 470-82, (2015)

In neuroblastoma, MYCN genomic amplification and segmental chromosomal alterations including 1p or 11q loss of heterozygocity and/or 17q gain are associated with progression and poor clinical outcome....

Related Compounds

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