parp-7

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

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

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.

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].

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.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid exhibiting anti-inflammatory and anti-cancer activities and can enhance the activation of p38 MAPK.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

USP1-IN-9 (Compound 1m) is a reversible and non-competitive inhibitor of ubiquitin-specific protease (USP1) with an IC50 value of 8.8 nM. It is synthesized based on the structures of ML323 and KSQ-4279 as a pyrido[2,3-d]pyrimidin-7(8H)-one derivative. USP1-IN-9 exhibits excellent inhibition of USP1/UAF and demonstrates strong antiproliferative effects on breast cancer cells. When combined with the PARP inhibitor olaparib, USP1-IN-9 enhances the cytotoxic effect on MDA-MB-436/OP cells. USP1-IN-9 holds potential for research in the field of cancer.

1. Dehydrocorydaline(DHC) not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergic reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC. 2. Dehydrocorydal

ART-IN-1 (compound 7) is a selective inhibitor of PARP with IC50 values of 19 μM for PARP2, 22 μM for TNKS2, 2.4 μM for PARP10, >100 μM for PARP14, and 1.1 μM for PARP15 [1].