PARP10 Inhibitor

RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC₅₀ of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC₅₀=7.8 nM), as well as the first PARP12 inhibitor ever reported.

OUL35 (NSC39047) is a potent and selective inhibitor of ARTD10 (PARP-10), with an IC₅₀ of 329 nM.

RBN-3143 is a potent and 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 can be used in research of lung inflammation.

ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC₅₀ of 0.89±0.28 μM.

PARP10-IN-1 is a PARP10 inhibitor with an IC₅₀ of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer.

PARP10/15-IN-1 (compound 8l) is a potent inhibitor of dual inhibitor of PARP10 and PARP15, with IC₅₀s of 160 nM and 370 nM, respectively. PARP10/15-IN-1 can be used for cancer.

PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC₅₀ of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC₅₀s of 1.7 μM for human PARP2 and human PARP15, respectively.

OUL312 is a potent PARP10 inhibitor (IC₅₀ = 20 nM), showing more than 75-fold greater selectivity for PARP15 (IC₅₀ = 1500 nM). OUL312 is also at least 18-fold higher than all other human enzymes in the family. OUL312 has a good ADME profile, is able to enter cells, is not toxic, and effectively rescues human cells from PARP10-induced apoptosis at sub-micromolar concentrations. OUL312 can be used for the study of cervical cancer.

PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC₅₀ values of 0.14 µM and 0.40 µM against PARP10 and PARP15, respectively. PARP10/15-IN-3 is able to enter cells and rescue cells from apoptosis.

PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC₅₀ of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC₅₀s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively.

YCH1899 is an orally active PARP inhibitor, with an IC₅₀< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC₅₀ values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.

TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC₅₀ of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent.

PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC₅₀ values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis.

ART-IN-1 (compound 7) is a selective PARP inhibitor with IC₅₀s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively.

ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC₅₀s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively.

PARP14 inhibitor 1 is an orally active, selective PARP14 inhibitor with an IC₅₀ of 5.52 nM. PARP14 inhibitor 1 exhibits favorable pharmacokinetic properties and in vivo safety. PARP14 inhibitor 1 enhances and stabilizes intracellular endogenous PARP14 protein levels, while effectively reducing the expression levels of IL-4, IL-13 and IL-17A. PARP14 inhibitor 1 can be used in research related to atopic dermatitis.

OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC₅₀=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC₅₀s of 2.9-8.8 μM.

ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC₅₀s of 2.0 μM, and 9.7 μM, respectively.

PARP10-IN-4 (compound 12Z) is a potent PARP10 inhibitor with a pIC₅₀ of 7.95. also shows inhibitory activity against TNKS1, TNKS2, and PARP11 with pIC₅₀ values of 6.95, 7.03, and 7.01, respectively.