arp-1

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.

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.

ARP-100 (MMP-2 Inhibitor III) is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with the S1' pocket of MMP-2 and exhibits anti-invasive properties in an in vitro invasion Matrigel model. ARP-100 has low inhibitory activity against MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM) and MMP-9 (0.2 μM)[1][2].

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

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 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-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.

ARP 101 is an effective selective matrix metalloproteinase-2 (MMP-2) inhibitor with anti-cancer activity. It induces the inhibition of HCMV through non-classical chelate 1 (SQSTM1) p62-Keap1-Nrf2 pathways and phosphorylation of the C-terminal domain of p62, regulating autophagy and inhibiting melanogenesis.

ARP (Aldehyde reactive probe) is a chemical compound that serves as an aldehyde-reactive probe by specifically tagging AP sites in DNA with biotin residues. It is used to detect abasic sites, which are common forms of DNA damage and intermediates in mutagenesis and carcinogenesis. ARP is highly sensitive, capable of detecting abasic sites at the femtomolar level (fewer than 1 site per 10^4 nucleotides).