| DC11779 |
TNKS-IN-41 |
A highly potent and selective tankyrase inhibitor with pIC50 of 8.5 and 8.1 for TNKS1 and TNKS2, respectively. |
|
| DC7046 |
A-966492
Featured
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
|
| DC5106 |
AG14361
Featured
|
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. |
|
| DC7926 |
AZ-6102
Featured
|
AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. |
|
| DC10056 |
AZ9482
Featured
|
AZ9482, a potent and selective PARP inhibitor featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. |
|
| DC1037 |
AZD2461
Featured
|
AZD2461 is a novel PARP inhibitor with potential to bypass Pgp-mediated resistance to Olaparib. |
|
| DC8571 |
BGP-15
Featured
|
BGP-15 is a PARP inhibitor and insulin sensitizer. |
|
| DC8453 |
Talazoparib（BMN-673）tosylate
Featured
|
Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib. |
|
| DC2008 |
Talazoparib(BMN-673)
Featured
|
BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. |
|
| DC8452 |
BMN-673 8R,9S |
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(PARP1). It does not inhibit PARG and is highly sensitive to PTEN mutation. |
|
| DC7378 |
BSI-201 |
BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). |
|
| DC9983 |
E-7449
Featured
|
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors. |
|
| DC8222 |
G007-LK
Featured
|
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. |
|
| DC11504 |
GeA-69
Featured
|
GeA-69(GeA69) is a potent, selective, allosteric, cell-active PARP14 macrodomain 2 (MD2) inhibitor with Kd of 0.86 uM in ITC assays. |
|
| DC11080 |
JPI-289 |
JPI-289 (JPI289) is a novel potent, water soluble PARP-1 inhibitor with IC50 of 18.5 nM, inhibits cellular PAR formation with IC50 of 10.7 nM. |
|
| DC7169 |
JW55
Featured
|
JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). JW55 decreased auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 uM and 830 nM respectively. |
|
| DC7871 |
KCL-440 |
KCL-440 is a a new poly(ADP-ribose) polymerase- PARP inhibitor. |
|
| DC11141 |
ME0328
Featured
|
ME0328 is an inhibitor of PARP3 (IC50 = 0.89 µM), which is a regulator of DNA repair and mitotic progression. |
|
| DC4179 |
Niraparib(MK4827) free base
Featured
|
MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. |
|
| DC9862 |
Niraparib(MK4827) hydrochloride
Featured
|
MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. |
|
| DC9576 |
Niraparib tosylate
Featured
|
MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.
|
|
| DC8659 |
MN-64
Featured
|
MN-64 is a inhibitor of tankyrases, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition. |
|
| DC9936 |
NMS-P118
Featured
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo. |
|
| DC7935 |
NU1025
Featured
|
NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM). |
|
| DC8463 |
NVP-TNKS656
Featured
|
NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2. |
|
| DC4110 |
AZD-2281 (Olaparib)
Featured
|
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively. |
|
| DC11022 |
OUL35
Featured
|
OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family. |
|
| DC11023 |
OUL35 derivative 32 |
OUL35 derivative 32 is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of230 nM, rescues HeLa cells from ARTD10-induced cell death.. |
|
| DC7237 |
PJ34 HCl
Featured
|
PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
|
| DC5151 |
Rucaparib phosphate (AG-14699, PF-01367338)
Featured
|
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2. |
|
