- Cat. No.
- A10111
Olaparib (AZD2281)
Synonyms: KU-0059436; AZD2281
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
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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: KU-0059436; AZD2281
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
Synonyms: MK4827
MK-4827 is a novel potent, orally bioavailable PARP-1 and PARP-2 inhibitor.
XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).
Synonyms: ABT-888
ABT-888(Veliparib) is a potential anti-cancer drug acting as a PARP inhibitor.
Synonyms: PF-01367338; AG-014447 (as free base)
AG-014699 (Rucaparib) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.
Synonyms: BMN-673; LT-673
BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
Synonyms: PJ34
PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).
AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.
Synonyms: NSC-746045; IND-71677; BSI-201
BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.
Synonyms: 3-AB
3-Aminobenzamide is a novel PARP inhibitor, known to sensitize cells to radiation in vitro by inhibiting the repair of DNA damage.
Synonyms: AG-014699; PF-01367338
Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells.
PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.
G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice,
Synonyms: MK-4827 tosylate
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.
Synonyms: BMN 673ts
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
Synonyms: IN01001
INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor.
A-966492 displayed high potency against the poly(ADP-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay.
TC-E 5001 is dual tankyrase (TNKS) inhibitor (Kd values are 79 and 28 nM for TNKS1 and TNKS2 respectively, IC50 = 33 nM for TNKS2) that is devoid of activity at PARP1 and PARP2 (IC50 >19 uM). Inhibits Wnt signaling and stabilizes Axin2 levels.
AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein.
UPF 1069 is a selective poly(ADP-ribose) polymerase (PARP) 2 inhibitor (IC50 values are 0.3 and 8.0 μM for PARP-2 and PARP-1 respectively).
JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2).
WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2.
ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.
Synonyms: (8R,9S)-BMN-673
BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673. BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM.