parp

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.

ARTD10 PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7 PARP15, ARTD8 PARP14, ARTD10 PARP10 and poly ADP-ribose polymerase-1 (ARTD1 PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Picolinamide (Picolinoylamide) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11 4 nM). XAV-939 selectively inhibits Wnt β-catenin-mediated transcription.

PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1 2.

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].

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.

AZ6102 is a potent TNKS1 2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

ME0328 is a potent, selective PARP inhibitor with an IC50 of 0.89 μM for PARP3, showing approximately 7-fold selectivity over PARP1.

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM 2.1 nM) is a selective PARP1 PARP2 inhibitor.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor.

PJ34 hydrochloride (PJ34 HCl) is a potent specific inhibitor of PARPl 2.

AZ9482 is a selective and potent inhibitor of PARP featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent activity of centrosome declustering with EC50 of < 18 nM in HeLa cells.

VEGFR PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2 M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [1].

UPF 1069 is a specific PARP2 inhibitor ( IC50: 0.3 μM). It is ~27-fold selective against PARP1.

AZD5305 is a potent, selective and oral active PARP inhibitor.

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].

TIQ-A is a PARP1 inhibitor which involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions includi