PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.CAS 번호128-52-56-8

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.

PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has potential anti-tumor activity and induces apoptosis.

PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis. It exhibits robust anti-proliferative activity [1].

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.

PARP7-IN-16 (compound 36) is a potent, selective, and orally active PARP-1/2/7 inhibitor, exhibiting IC50 values of 0.94, 0.87, and 0.21 nM , respectively. It has potential applications in breast and prostate cancer research [1].

3-Aminobenzamide (PARP-IN-1) is an effective inhibitor of PARP (IC50<50 nM in CHO cells) and a mediator of oxidant-induced myocyte dysfunction during reperfusion.

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

PARP-1-IN-4 is a potent PARP-1 inhibitor with potential see anti-tumor activity, and inhibition of PARP-1 may be used in cancer development.

PARP10-IN-3 is a potent and selective mono-Adp-ribotransferase PARP10 inhibitor that inhibits human PARP10 (IC50:480 nM). PARP10-IN-3 also inhibited human PARP2 and human PARP15 with IC50 values of 1.7 μM.

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

ARTD3/PARP3-IN-1 is a non-selective inhibitor targeting diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3 [1].

PARP1-IN-16 (compound 12a) serves as a potent PARP1 inhibitor, exhibiting an IC50 value of 1.89 nM. It possesses the capability to halt the cell cycle at the S phase and stimulate apoptosis in HCT-116 cells [1].

PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC 50 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].

PARP1-IN-5 is a potent, selective, orally active, low-toxicity PARP-1 inhibitor with an IC50 value of 14.7 nM. PARP1-IN-5 can be used in cancer research.

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

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

PARP/EZH2-IN-1 is a novel compound that functions as a dual inhibitor for both PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for the treatment of triple-negative breast cancer with wild-type BRCA.

PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

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

PARP-2/1-IN-2, an enantiomer of Veliparib, serves as a potent inhibitor of PARP, demonstrating inhibition constants (Kis) of 2 nM for PARP-2 and 5 nM for PARP-1. This compound exhibits a half-maximal effective concentration (EC50) of 3 nM in cell-based assays evaluating PARP activity [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.

PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM for PARP-1.

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].

PROTAC PARP/EGFR ligand 1 is a potent compound utilized in the creation of dual PARP-EGFR degraders through Proteolytic Targeting Chimera (PROTAC) technology [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 DNA double-strand breaks. It induces apoptosis in cancer cells via the mitochondrial pathway [1].

ARTD10/PARP10-IN-2 is a potent, non-selective inhibitor of mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1, exhibiting IC50 values of 2.0 μM and 9.7 μM, respectively.

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-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.

PARP1-IN-9 (Compound 5c) is a potent PARP1 inhibitor, displaying an IC 50 of 30.51 nM. With its ability to induce cell apoptosis and exhibit anticancer activity, PARP1-IN-9 surpasses Olaparib in terms of efficacy [1].

PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM. It shows an antiproliferative effect on MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells, with IC50 values under 0.3 nM [1].

PARP1-IN-12, a potent inhibitor of PARP1, demonstrates an IC50 value of 2.99 nM. It exhibits antiproliferative effects, induces apoptosis, and causes cell cycle arrest in the G2/M phase. Additionally, PARP1-IN-12 induces DNA double-strand breaks (DSBs) in BRCA-deficient cells.

PARP10-IN-2 is a potent inhibitor of PARP10, a mono-ADP-ribosyltransferase, with an IC50 value of 3.64 μM for human PARP10.PARP10-IN-2 also inhibited PARP2 and PARP15, with IC50 values of 27 μM and 11 μM, respectively.

PARP1-IN-11 (compound 49) is a potent inhibitor of PARP1 with IC50 value of 0.082 μM which shows complete inhibition of PARP1 and substantially inhibits PARP3, TNKS1 and TNKS2 [1].

PARP1/BRD4-IN-1 is a highly selective and potent inhibitor of PARP1 (IC50: 49 nM) and BRD4 (IC50: 202 nM).PARP1/BRD4-IN-1 inhibits the expression and activity of PARP1 and BRD4, thereby synergistically suppressing the malignant growth of pancreatic cancer cells.

PARP11 Inhibitor ITK7 (ITK7) is a potent, selective inhibitor of PARP11, demonstrating significant efficacy with an IC50 value of 14 nM. It is primarily utilized in research focused on cellular localization.

PARP1-IN-10 (compound 12c) is a highly potent and non-cytotoxic PARP1 inhibitor, displaying an in vitro IC50 value of 50.62 nM. This compound effectively induces cell cycle arrest at the G2/M phase and apoptosis, while also significantly augmenting the cytotoxic effects of temozolomide (TMZ) [1].

PARP1/BRD4-IN-2 is a potent and selective inhibitor of PARP1 (IC50: 197 nM) and BRD4 (IC50: 238 nM).PARP1/BRD4-IN-2 inhibits DNA damage repair, blocks the G0/G1 cell cycle transition, and induces apoptosis.PARP1/BRD4-IN-2 exhibits antitumor effects in the MDA-MB-468 mouse xenograft tumor model.PARP1/BRD4-IN-2 has been used to study the antitumor effects of PARP1/BRD4-IN-2 in triple-negative breast cancer (MDA-MB-468). PARP1/BRD4-IN-2 exhibits antitumor effects in the MDA-MB-468 mouse xenograft tumor model.PARP1/BRD4-IN-2 can be used to study triple-negative breast cancer (TNBC).

PARP7-probe-1, a chemiluminescent-labeled and biotinylated probe, selectively binds to the PARP7 active site, facilitating research into PARP7 function [1].

PARP1-IN-7 functions as an anticancer agent by inhibiting poly(ADP-ribose) polymerase-1 (PARP1).

PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC 50 values of 0.14 μM and 0.40 μM against PARP10 and PARP15, respectively. PARP10/15-IN-3 can enter cells and rescue cells from apoptosis [1].

PARP10/15-IN-1 (compound 8l) is a dual PARP10 and PARP15 inhibitor with IC50s of 160 nM and 370 nM, respectively. It can be used in cancer research[1].

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis. It exhibits anti-cancer activity in triple-negative breast cancer (TNBC) cells and patient-derived organoids, making it useful for TNBC research, including cases with or without BRCA1 mutations [1].

PARP7-IN-12, a potent inhibitor targeting PARP7, exhibits an IC50 of 7.836 nM. This compound is applicable in cancer research.

PARP10/15-IN-2 (Compound 8h) is a dual inhibitor of PARP10 and PARP15 with IC 50 values of 0.15 μM and 0.37 μM, respectively. PARP10/15-IN-2 can enter cells and rescue cells from apoptosis [1].

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.

RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

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.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]