- |
My Account- |
PARP, one of the most abundant proteins in the nucleus, has the principal role in regulating the cellular processes that are most relevant in terms of pathophysiology and experimental therapy. PARP1 which is a 116-kDa protein consists of three main domains is the most important member of the PARP family and can be a DNA-damage sensor and signalling molecule because the ZINC FINGERS of PARP recognize singleand double-stranded DNA breaks. PARP can be cleaved into inactive fragments by caspases or matrix metalloproteinases (MMPs). The phosphorylation of PARP by protein kinase-C (PKC), through the inhibition of its DNA binding, also suppresses PARP activity. PARP, through physical interactions and/or catalytic actions, promotes activator protein-1 (AP1) and nuclear factor-κB (NF-κB)-dependent signal-transduction processes and can suppress the activation of the cytoprotective AKT pathway; therefore, the inhibition of PARP can suppress AP1 and NF-κB activation and induce AKT phosphorylation.
| Cat.No. | Product Name | Information | Publication | Customer Review |
|---|---|---|---|---|
| S1060 | Olaparib (AZD2281) | Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively. |
 (23)
|
 (3)
|
| S1004 | ABT-888 (Veliparib) | ABT-888 (Veliparib, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. |
(9)
|
(8)
|
| S1098 | Rucaparib (AG-014699 , PF-01367338) | Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM. |
(3)
|
(1)
|
| S1087 | Iniparib (BSI-201) | BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor. |
(1)
|
(1)
|
| S2197 | A-966492 | A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
|
|
| S2178 | AG14361 | AG14361 is a potent inhibitor of PARP1 with Ki of < 5 nM. |
|
|
| S1132 | INO-1001 | INO-1001 is a potent inhibitor of PARP with IC50 of 50 nM and a mediator of oxidant-induced myocyte dysfunction during reperfusion. |
|
|
| S7048 | BMN 673 | BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. |
|
|
| S8038 | UPF 1069 | UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. |
|
|
| S2886 | PJ34 | PJ-34 is a potent PARP inhibitor with EC50 of 20 nM. |
|
|
| S2741 | MK-4827 | MK-4827 is an selective inhibitor of PARP1 and PARP2 with IC50 of 3.8 nM and 2.1 nM, respectively. |
|
|
