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PARP inhibitors block poly(ADP-ribose) polymerases (PARPs), enzymes that mark DNA damage and recruit repair proteins. PARP1 and PARP2 bind DNA single-strand breaks and attach poly(ADP-ribose) chains to themselves and to nearby chromatin proteins. Cells lacking breast cancer susceptibility proteins 1 or 2 (BRCA1, BRCA2), and therefore defective in homologous recombination, are highly sensitive to PARP inhibition. This synthetic lethal relationship, reported in 2005, has shaped much of the research on DNA repair inhibitors. Olaparib, niraparib, veliparib and talazoparib target the catalytic domains of PARP1 and PARP2, and 3-aminobenzamide is an early benzamide inhibitor. XAV 939 instead inhibits tankyrases 1 and 2 (TNKS1, TNKS2), which stabilizes axin in Wnt signaling studies.
Synonyms: 4-Quinazolinol; Quinazolidin-4-one
4-HQN has been shown to inhibit PARP (poly(ADP-ribose) synthetase) which catalyzes covalent attachment of the ADP-ribose moiety of NAD+ to various proteins.
Synonyms: PARP Inhibitor
BYK204165 is a cell-permeable isoquinolinedione compound that potently and selectively inhibits poly (ADP-ribose) polymerase 1 (PARP1).
BYK 49187, PARP-1 and PARP-2 inhibitor (pIC50 values are 8.36 and 7.50 for cell-free recombinant PARP-1 and murine PARP-2 respectively).
Synonyms: SC-202756
PARP Inhibitor XIDR 2313, PARP Inhibitor XI, is a water soluble pyrimidinone compound that functions as a PARP (Poly(ADP-ribose) polymerase) inhibitor.
Synonyms: EB47
EB 47 is a potent inhibitor of PARP1 with IC50 of 45 nM.
NU 1025 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, which potentiates the cytotoxicity of a panel of mechanistically diverse anti-cancer agents in L1210 cells.
Synonyms: TNKS656
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.
AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.
MN-64 is a potent and selective inhibitor of Tankyrase 1 and 2 (IC50 = 6 and 72 nM, respectively).
BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice.
Synonyms: BGB-290
Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. CAS: 1446261-44-1 (free base) 2086689-94-1 (maleate) 2086689-93-0 (hydrate)
Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1, and also shows binding affinity to eight other PARP domains.
Synonyms: MK-4827 hydrochloride; MK4827
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays.
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (??24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively).
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.
BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
Synonyms: ABT-888
Veliparib dihydrochloride is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
Synonyms: E-7449
E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ?50 and ?50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Synonyms: MK 4827 (R-enantiomer); MK4827
Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
