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Chemical Probes Portal PDD00017273.pdf
PDD00017273

Reagent Authentication Certificate:

Protein target name:
PARGMechanism of action:
PolyADP ribose (PAR) competitive inhibitorRecommended Concentration for use in cells:
Up to 10 uM, or 10X the cellular IC50 depending on the cell line
Probe Availability
Probe Information
In vitro validation
Potency:
IC5026 nM
Potency assay:
Biochemical PAR chain persistence assayOff target protein and potency:
PARP1 IC50 >30µMARH3 IC50 >30µMPotency assay (off target):
Biochemical PAR chain persistence assayProbe Selectivity in Vitro:
Biochemical selectivity against safety targets (% inhibition at 10 µM, binding assay Eurofins Panlabs):
Adenosine A1=1%,
Adenosine A2A=-1%,
Adrenergic a1A=-5%,
Adrenergic a1B=7%,
Adrenergic a2A=10%,
Adrenergic β1=-9%,
Adrenergic β2=-9%,
Calcium Channel=L Type=16%,
Cannabinoid CB1=21%,
Dopamine D1=6%,
Dopamine D2S=-9%,
GABAA=Flunitrazepam Central=4%,
GABAA=Muscimol Central=3%,
Glutamate=NMDA=4%,
Histamine H1=-6%,
Imidazoline I2=Central=-18%,
Muscarinic M2 =-1%,
Muscarinic M3 =3%,
Nicotinic Acetylcholine=3%,
Nicotinic Acetylcholine=a1=-3%,
Opiate µ(OP3=MOP)=-6%,
Phorbol Ester=-11%,
Potassium Channel [KATP]=5%,
Potassium Channel hERG=12%,
Prostanoid EP4=11%,
Rolipram=16%,
Serotonin (5-Hydroxytryptamine) 5-HT2B=4%,
Sigma σ1=15%,
Sodium Channel site 2=6%,
Transporter=Norepinephrine (NET)=20%,
Acetyl Cholinesterase=-1%,
Cyclooxegenase COX-2=-2%,
Phosphodiesterase PDE4=17%,
In cell validation
Potency in cells:
IC5037 nM
Potency assay (cells):
Whole-cell PAR chain-persistence assay in HeLa cells after MMS challenge.Target engagement assay (cells):
Antibody-based PAR chain-persistence assayToxicity
Cytoxicity assay:
YesNotes on cytotoxicity:
On target: Yes, in clonogenic assays, depending on the genetic background (7-21-day assay, dependent upon cell line and replicative rate). Example data: ZR-75-1 cells, IC50=200 nM; MDA-MB436 cells, IC50=800 nM; HCC1937 cells, IC50>10 µM)
In the absence of a DNA-damaging agent, the compound is not cytotoxic below 30 µM in HeLa cells, for up to 72 hrs.