parp7

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor aimed at PARP7 and HDAC, exhibiting antitumor properties. It demonstrates inhibition of various PARPs and HDACs with IC50 values of 83.3 nM for PARP1, 3.1 nM for PARP7, 35 nM for HDAC1, 30.3 nM for HDAC2, 35.4 nM for HDAC3, and 6.4 nM for HDAC6.

PARP7-IN-24 (compound 44) is a potent inhibitor of PARP7, demonstrating an EC50 of 0.375 nM for pSTAT1 in NCI-H1373 cells. It shows potential for use in cancer research.

PARP7-IN-23 (compound 56) is a potent PARP7 inhibitor with an EC50 of 0.915 nM for pSTAT1 in NCI-H1373 cells, indicating its potential for cancer research.

PARP7-IN-17 is a potent PARP7 inhibitor with an IC50 of 4.5 nM and is orally active. [PARP7-IN-17] exhibits antitumor effects.

PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 with an IC50 of ≤10 nM, suitable for oncology research.

PARP7-IN-12, a potent inhibitor targeting PARP7, exhibits an IC50 of 7.836 nM. This compound is applicable in cancer research.

PARP7-probe-1, a chemiluminescent-labeled and biotinylated probe, selectively binds to the PARP7 active site, facilitating research into PARP7 function [1].

PARP7-IN-16 (compound 36) is a potent, selective, and orally active inhibitor of PARP-1/2/7, with IC50 values of 0.94, 0.87, and 0.21 nM, respectively, and holds potential applications in breast and prostate cancer research [1].

PARP7-IN-15 (Compound 18) is a potent PARP7 inhibitor with an IC50 of 0.56 nM and demonstrates antitumor activity [1].

Parp7-in-18 (Compound 8) is a selective PARP7 inhibitor with an IC50 of 0.11 nM, demonstrating strong anticancer activity and favorable pharmacokinetic properties [1].

PARP7-IN-21 (compound 128) acts as a potent PARP7 inhibitor, demonstrating an IC50 of less than 10 nM.

XYL-1 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. It has the capability to enhance type I interferon signaling in vitro, positioning it as a potential candidate for the development of cancer immunotherapy drugs.

Antitumor agent-169 (Compound B3) is a dual inhibitor of PD-1/PD-L1 interaction and PARP7, with IC50 values of 0.426 μM and 2.50 nM, respectively. It exhibits affinity for human PD-L1 with a Ki of 20.2 nM and can restore T cell function by increasing IFN-γ secretion. Antitumor agent-169 inhibits cell viability in MDA-MB-231 and Jurkat T cells, demonstrates antitumor activity against melanoma in mouse models, and possesses favorable pharmacokinetic properties.

Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.

KMR-206 is a potent and selective PARP7 inhibitor with an IC50 of 13.7 nM. It enhances the expression of STAT1 and phosphorylated Tyr701 site STAT1 (pSTAT1). KMR-206 induces STING degradation and elevates type I IFN receptor levels, showing anticancer activity against lung adenocarcinoma and is applicable in colon cancer research.

TIPARP-IN-1 (Compound 15) is a selective inhibitor of PARP7 (TIPARP, also known as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) inducible PARP) with an IC50 value of 2.15 nM. By inhibiting TIPARP, TIPARP-IN-1 can restore the IFN signaling pathway in tumors. In the tumor microenvironment, it selectively activates anti-tumor immune responses while avoiding the systemic production of cytokines. TIPARP-IN-1 is applicable for research in head and neck squamous cell carcinoma.

RBN012759 inhibits PARP14 protein with an IC50 value of 0.003 μM and is more than 300-fold selective over all PARP family members.[2]

OUL232 is a potent single ARTs PARP7, PARP10, PARP11, PARP12, PARP14 and PARP15 inhibitor for cancer and tumour research.

YCH1899, an orally active PARP inhibitor, demonstrates potent inhibition of PARP1/2 with an IC50 of less than 0.001 nM. It shows marked antiproliferative efficacy against Olaparib-resistant (Capan-1/OP) and Talazoparib-resistant (Capan-1/TP) cells with IC50 values of 0.89 nM and 1.13 nM, respectively. Moreover, YCH1899 possesses favorable pharmacokinetic attributes in rats [1].

OUL243 is a potent and selective inhibitor of mono-ADP-ribosyltransferase (ARTs), effectively suppressing PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15.

RBN010860 (example 150) is a potent PARP7 inhibitor with an IC50 of less than 0.1 μM, suitable for cancer research.

PARP1-IN-44 is a derivative of Olaparib and functions as an orally active PARP1 inhibitor with an IC50 of 0.6 nM. It also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 demonstrates selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. It induces G2/M phase arrest, promotes apoptosis, increases reactive oxygen species (ROS) levels, and disrupts mitochondrial membrane potential. Additionally, PARP1-IN-44 inhibits PARylation and leads to the accumulation of γH2AX. It activates the cGAS-STING pathway, enhancing the expression of IFN-β and CXCL10. In a CT26 tumor mouse model, PARP1-IN-44 enhances CD8+ T cell infiltration, showcasing significant in vivo antitumor activity.