parp-1

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

Verminoside is a natural iridoid isolated from Kigelia africana, with anti-inflammatory and remarkable antioxidant activity.

WD2000-012547 is a selective inhibitor of poly(ADP-ribose)-polymerase (PARP-1) (pKi: 8.221).

NMS-P515 is an effective, orally active, and stereospecific PARP-1 inhibitor (Kd: 16 nM and an IC50: 27 nM (in Hela cells)). It has anti-tumor activity.

Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

PARP-1-IN-4 is a potent PARP-1 inhibitor with potential anti-tumor activity, where inhibition of PARP-1 may be applied in cancer treatment.

Phytic acid dipotassium salt is an endogenous metabolite that inhibits β-secretase 1 (BACE1).

PARP-1-IN-32 (compound 15) is an inhibitor of poly (ADPribose) polymerase-1 (PARP-1), specifically designed for use in cancer research.

TOPOI/PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI/PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.

PARP-1/Proteasome-IN-1 (compound 42i) is a dual inhibitor of PARP-1 and the proteasome, demonstrating significant inhibitory effects on breast cancer. By downregulating the expression of BRCA1 and RAD51, it impairs homologous recombination repair and induces apoptosis (cellular death).

PARP-1-IN-1 is a highly selective and orally active inhibitor of the enzyme PARP-1 with an IC50 of 0.96 nM, exhibiting excellent tolerance and significant activity in a single dose in the MDA-MB-436 xenotransplantation model [1].

PARP-1/HDAC-IN-1 is an effective dual inhibitor of PARP-1 and HDAC6, with IC50 values of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 exhibits anti-cancer, anti-migration, and anti-angiogenesis activities.

PARP-1-/2-IN-1 is a potent inhibitor of PARP-1 (IC50: 0.51 nM) and PARP-2 (IC50: 23.11 nM).

PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair and inducing cell cycle arrest and apoptosis. This compound also hampers the proliferation of TNBC cells and the growth of TNBC xenograft tumors [1].

PARP-1-IN-13 (Compound 19c) is a potent PARP-1 inhibitor with an IC50 of 26 nM, hindering DNA single-strand break repair and exacerbating double-strand breaks, leading to apoptosis in cancer cells via the mitochondrial pathway [1].

Compound B6, also known as TOPOI/PARP-1-IN-1, is a dual inhibitor targeting TOPOI and PARP, exhibiting low cytotoxicity and oral activity with a PARP1 IC 50 of 0.09 μM. This compound effectively inhibits cancer cell proliferation and migration, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. In murine models, TOPOI/PARP-1-IN-1 demonstrated a tumor growth inhibition rate (TGI) of 75.4% [1].

PARP-1-IN-23 (Compound I16) is an orally bioavailable, selective inhibitor of PARP-1, exhibiting an IC50 of 12.38 nM. This compound demonstrates efficacy in inhibiting tumor growth in vivo.

PARP-1/2/7-IN-1 (compound 86) is a highly effective inhibitor of PARP-1/2/7, demonstrating an IC50 value of less than 10 nM .

PARP-2-IN-1 is a potent and selective inhibitor of PARP-2 (IC50 of 11.5 nM).

PARP/NAMPT-IN-1 (Compound 13j) is a dual-target inhibitor of PARP and NAMPT, with IC50 values of 0.8 nM for PARP1 and 18 nM for NAMPT. It suppresses breast cancer cell proliferation and migration, inducing apoptosis. PARP/NAMPT-IN-1 is applicable for research on triple-negative breast cancer.

CDK9/PARP-IN-1 (compound 37) is an inhibitor of CDK9 and PARP. It demonstrates IC50 values of 118 nM for CDK9 and 107 nM for PARP1. This compound exhibits a broad-spectrum anti-proliferative effect across various cancer cell lines.

(Rac)-PROTAC PARP/EGFR ligand 1 is a compound that includes ligands for target proteins PARP and EGFR, along with a PROTAC linker that recruits E3 ligases such as VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC DP-C-4, a dual CRBN-based PROTAC designed for the concurrent degradation of EGFR and PARP.