PARP7
PARP7 (TIPARP, ARTD14) is a mono-ADP-ribosyltransferase that regulates innate immunity, transcription factor activity, and cellular stress responses through mono-ADP-ribosylation of protein substrates[1]. Mechanistically, PARP7 is a transcriptional target of the aryl hydrocarbon receptor (AHR) and functions as a negative feedback regulator of AHR signaling by mono-ADP-ribosylating AHR-associated substrates, thereby restricting AHR-dependent transcriptional programs[1][2]. PARP7 also participates in type I interferon (IFN-I) regulation and acts as a negative regulator of IFN signaling pathways in tumor cells, linking ADP-ribosylation to immune surveillance and antitumor responses[3][4]. In disease models, inhibition of PARP7 restores IFN-I signaling, suppresses tumor growth, and promotes antitumor immunity, supporting PARP7 as a therapeutic target in cancer research[3][4]. Beyond AHR signaling, PARP7 modulates the activity of nuclear receptors, including estrogen receptor α (ERα), through mono-ADP-ribosylation, resulting in reduced receptor-dependent transcription and proliferation in estrogen-responsive breast cancer models[1][5]. Compared with poly(ADP-ribose) polymerases that catalyze poly-ADP-ribosylation, PARP7 belongs to the mono-ADP-ribosyltransferase subgroup and exerts distinct regulatory effects on transcription factors and immune signaling pathways[1]. For experimental applications, selective PARP7 inhibitors such as RBN-2397 enhance IFN-I signaling and have demonstrated antitumor activity in preclinical cancer models, making them valuable tools for investigating PARP7-dependent immune and transcriptional mechanisms[1][3].
References:
- [1]. Rasmussen M, et al. PARP7 and Mono-ADP-Ribosylation Negatively Regulate Estrogen Receptor α Signaling in Human Breast Cancer Cells. Cells. 2021 Mar 11;10(3):623. [Content Brief]
- [2]. Steen CB, et al. The landscape of tumor cell states and ecosystems in diffuse large B cell lymphoma. Cancer Cell. 2021 Oct 11;39(10):1422-1437.e10. [Content Brief]
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PARP7 Related Products (25)
Related Products (25)
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TIPARP-IN-1
0 ImagesCat. No.: HY-181027CAS No.: 3106183-96-1TIPARP-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.
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PARP7-IN-24
0 ImagesCat. No.: HY-173262CAS No.: 3072866-54-4
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PARP-1/2/7-IN-1
0 ImagesCat. No.: HY-161606CAS No.: 3034665-49-8PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with the IC50 of ＜ 10 nM.
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PARP7-IN-18
0 ImagesCat. No.: HY-162172CAS No.: 2819999-00-1PARP7-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.
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PARP7-IN-21
0 ImagesCat. No.: HY-161607CAS No.: 3034666-02-6PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC50 of ＜ 10 nM.
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