PARP

E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.

PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549.

PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.

PROTAC PARP1 degrader is a bifunctional small molecule composed of a PARP1-binding ligand covalently linked via a linker to an E3 ubiquitin ligase ligand, which can potently induce PARP1 cleavage and programmed cell death.

Nesuparib is a potent inhibitor of PARP.

AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).

KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530).

PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.

DB008 is an effective selective inhibitor of PARP16 with an IC50 value of 0.27 μM and contains acrylamide electrophile. DB008 has membrane permeability and can selectively label PARP16.

Olaparib-d8 is the deuterated form of Olaparib (AZD2281). Olaparib is an orally effective PARP inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 5 and 1 nM, respectively. Olaparib is also an activator of autophagy and mitophagy.

PARP10/15-IN-2 (Compound 8h) is an effective dual inhibitor of PARP10 and PARP15, with IC50 values of 0.15 μM and 0.37 μM, respectively. It can enter cells and prevent apoptosis.

PARP10/15-IN-3 (Compound 8a) is an effective dual inhibitor of PARP10 and PARP15, with IC50 values of 0.14 μM and 0.40 μM, respectively. It can enter cells and prevent apoptosis.

PARP10-IN-2 is an effective inhibitor of mono-ADP-ribosyltransferase PARP10, with an IC50 of 3.64 μM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 27 μM and 11 μM for human PARP2 and human PARP15, respectively.

PARP10-IN-3 is a selective mono-ADP-ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 1.7 μM for both human PARP2 and human PARP15.

PARP11 inhibitor ITK7 (ITK7) is an effective and selective inhibitor of PARP11. It can effectively inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for research on cellular localization.

PARP1-IN-7 is an inhibitor of poly ADP-ribose polymerase-1 (PARP1), used as an anticancer agent.

PARP7-IN-14 (I-1) is an effective selective PARP7 inhibitor with an IC50 value of 7.6 nM. PARP7-IN-14 has anti-cancer activity.

RBN-3143 is an effective NAD+ competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 is used for research on lung inflammation.

SK-575 is an efficient and specific protein-hydrolyzing targeted chimeric molecule (PROTAC) PARP1 degrader with an IC50 of 2.30 nM. SK-575 can effectively inhibit the growth of cancer cells carrying BRCA1/2 mutations.