PARP7 Inhibitor

TIPARP-IN-1 (Compound 15) is a selective PARP7 (TIPARP) (2,3,7,8-Tetrachlorodiben-zo-p-dioxin(TCDD)-inducible PARP) inhibitor with an IC₅₀ of 2.15 nM. TIPARP-IN-1 can restore IFN signaling pathway in tumors by inhibiting TIPARP. TIPARP-IN-1 selectively activates the anti-tumor immune response in the tumor microenvironment and avoids the production of systemic cytokines. TIPARP-IN-1 can be used for research of head and neck squamous cell carcinoma.

PARP7-IN-24 (compound 44) is a potent PARP7 inhibitor with an EC₅₀ of 0.375 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-24 has the potential for cancer research.

PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with the IC₅₀ of ＜ 10 nM.

PARP7-IN-18 is a potent, highly selective, and orally active PARP7 inhibitor with an IC₅₀ of 0.11 nM. PARP7-IN-18 exhibits >1000-fold selectivity over other PARP family members. PARP7-IN-18 inhibits NCI-H1373 lung cancer cell proliferation with an IC₅₀ of 2.5 nM and promotes IFN-β expression. PARP7-IN-18 exhibits favorable pharmacokinetic properties and can be used in research on PARP7-sensitive tumors, such as lung cancer.

PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC₅₀ of ＜ 10 nM.