PARP

Cat. No.

A31667

CAS No.

2915650-86-9

PARP-2-IN-3

PARP-2-IN-3 is a potent inhibitor of PARP-2, exhibiting an IC50 of 0.07 μM. This compound effectively induces apoptosis and necrosis in cancer cells, making it a valuable tool for cancer research. Additionally, PARP-2-IN-3 demonstrates favorable pharmacokinetic properties and oral bioavailability, supporting its potential use in therapeutic applications targeting PARP-2 related pathways.

Cat. No.

A31827

CAS No.

2758117-74-5

PARP1/BRD4-IN-1

PARP1/BRD4-IN-1 is a selective inhibitor targeting both PARP1 and BRD4, demonstrating IC50 values of 49 nM and 202 nM, respectively. This compound effectively represses the expression and activity of these proteins, leading to synergistic inhibition of malignant pancreatic cancer cell growth. PARP1/BRD4-IN-1 is a valuable tool for exploring therapeutic strategies in cancer research, particularly in the context of PARP and BRD4 signaling pathways.

Cat. No.

A32084

CAS No.

3037993-97-5

PARP1/BRD4-IN-2

PARP1/BRD4-IN-2 is a selective inhibitor of PARP1 and BRD4, demonstrating IC50 values of 197 nM and 238 nM, respectively. This compound effectively impedes DNA damage repair mechanisms, inhibits the G0/G1 cell cycle transition, and induces apoptotic cell death. PARP1/BRD4-IN-2 has shown significant anti-tumor efficacy in the MDA-MB-468 xenograft mouse model, making it a valuable tool for research in triple-negative breast cancer (TNBC).

Cat. No.

A32162

CAS No.

2098639-70-2

PARP1-IN-14

PARP1-IN-14 is a potent inhibitor of PARP1, displaying an IC50 of 0.6 ± 0.1 nM. It demonstrates significant antiproliferative effects on MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cell lines, with IC50 values below 0.3 nM. This compound is valuable for cancer research, particularly in studies focused on DNA repair mechanisms and therapeutic strategies for BRCA-deficient tumors.

Cat. No.

A32171

CAS No.

2505146-00-7

PARP1-IN-46

PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM, targeting the PARP-1 enzyme to modulate DNA damage response pathways. It exhibits significant anti-proliferative effects in both rat (C6) and human (U87MG) glioma cell lines by promoting PARP cleavage and inducing reactive oxygen species (ROS), ultimately leading to increased cell apoptosis. Additionally, PARP1-IN-46 effectively inhibits glioma cell migration, invasion, and colony formation, making it a valuable tool for research on glioma biology and potential therapeutic strategies.

Cat. No.

A32295

CAS No.

2915651-00-0

PARP-2-IN-2

PARP-2-IN-2 is a potent inhibitor of PARP-2, exhibiting an IC50 value of 0.057 μM. This compound effectively induces cell cycle arrest and apoptosis in MCF-7 breast cancer cells, highlighting its potential as a therapeutic agent in cancer research. PARP-2-IN-2 is valuable for investigations into cancer biology and therapeutic strategies targeting DNA repair mechanisms.

Cat. No.

A32333

CAS No.

2108829-86-1

KU-0058948 hydrochloride

KU-0058948 hydrochloride is a highly selective inhibitor of PARP1, exhibiting an IC50 of 3.4 nM. It is demonstrated to induce cell cycle arrest and apoptosis in primary myeloid leukemic cells and various myeloid leukemic cell lines. This reagent is valuable for research into the mechanisms of leukemia and the therapeutic potential of PARP inhibition in hematological malignancies.

Cat. No.

A32400

CAS No.

3084810-86-3

PARP1/NAMPT-IN-1

PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research on triple-negative breast cancer (TNBC).

Cat. No.

A32457

CAS No.

2944101-99-7

PARP1/c-Met-IN-1

PARP1/c-Met-IN-1 is a selective dual inhibitor targeting PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest in the G2/M phase in MDA-MB-231 cells. Additionally, PARP1/c-Met-IN-1 has shown significant antitumor activity in murine models, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A32498

CAS No.

2494001-21-5

PARP1-IN-10

PARP1-IN-10 is a potent inhibitor of PARP1, exhibiting an IC50 value of 50.62 nM in vitro without inducing cytotoxic effects. This compound induces cell cycle arrest at the G2/M phase and promotes apoptosis, thereby enhancing the cytotoxic efficacy of temozolomide (TMZ). PARP1-IN-10 is valuable for research in cancer biology and therapeutics, particularly in understanding the interplay between DNA repair mechanisms and chemotherapeutic sensitivity.

Cat. No.

A32501

CAS No.

3109617-69-5

PARP1-IN-55

PARP1-IN-55 is a selective inhibitor of PARP1, demonstrating potent activity with an IC50 of 0.019 μM. It exhibits considerable anti-proliferative effects on MCF-7 breast cancer cells, with an IC50 of 3.6 μM. By inhibiting the PARP1-mediated DNA damage repair pathway, PARP1-IN-55 induces reactive oxygen species accumulation, disrupts mitochondrial membrane potential, and promotes apoptosis while inhibiting cancer cell migration, invasion, and colony formation. This compound serves as a valuable tool for investigating breast cancer biology and therapeutic strategies.

Cat. No.

A32526

CAS No.

2243453-32-7

PARP1/2/TNKS1/2-IN-1

PARP1/2/TNKS1/2-IN-1 is an inhibitor targeting PARP-1, PARP-2, TNKS1, and TNKS2, with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM, and 4.15 nM, respectively. This compound demonstrates significant antitumor activity and promotes apoptosis, making it a valuable tool for research focused on cancer biology and therapeutic strategies. Its dual inhibitory action can facilitate the exploration of cellular repair mechanisms and enhance the understanding of poly(ADP-ribose) polymerases in cancer treatment.

Cat. No.

A32650

CAS No.

3010256-54-6

VEGFR/PARP-IN-1

VEGFR/PARP-IN-1 is a dual inhibitor targeting Vascular Endothelial Growth Factor Receptor (VEGFR) and Poly(ADP-ribose) Polymerase (PARP), with IC50 values of 191 nM and 60.9 nM, respectively. This compound inhibits DNA damage repair mechanisms, induces apoptosis, and causes G2/M phase cell cycle arrest. It demonstrates significant antiproliferative activity against BRCA wild-type breast cancer cell lines, specifically MDA-MB-231 and MCF-7, with IC50 values of 4.1 μM and 3.5 μM, respectively. VEGFR/PARP-IN-1 is an effective antitumor and anti-metastatic agent, making it valuable for cancer research applications.

Cat. No.

A32730

CAS No.

2948352-16-5

TOPOI/PARP-1-IN-1

TOPOI/PARP-1-IN-1 is a dual inhibitor targeting topoisomerase I and PARP-1, demonstrating an IC50 value of 0.09 μM for PARP-1. This compound exhibits significant anti-proliferative and anti-migratory effects on cancer cells, leading to G0/G1 phase cell cycle arrest and apoptosis. In preclinical studies, TOPOI/PARP-1-IN-1 achieved a tumor growth inhibition rate of 75.4% in mice, highlighting its potential for cancer therapy research applications.

Cat. No.

A32763

CAS No.

2755825-45-5

PARP1/NAMPT-IN-2

PARP1/NAMPT-IN-2 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 0.8 nM and 18 nM, respectively. This compound effectively inhibits cell proliferation and migration, while inducing apoptosis in breast cancer cells. PARP1/NAMPT-IN-2 is particularly relevant for investigating therapeutic strategies in triple-negative breast cancer research.

Cat. No.

A32806

CAS No.

3052304-23-8

PARP-1/2-IN-2

PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A32919

CAS No.

3052259-89-6

DiPT-4

DiPT-4 is a dual inhibitor of topoisomerase I (TOP1) and poly (ADP-ribose) polymerase 1 (PARP1). This compound induces substantial DNA double-strand breaks, leading to cell cycle arrest and apoptosis in various cancer cell lines. DiPT-4 is particularly valuable for research focused on overcoming mechanisms of cancer drug resistance.

Cat. No.

A32995

CAS No.

55511-14-3

Schisandronic acid

Synonyms: Ganwuweizic acid

Schisandronic acid is a potent PARP inhibitor derived from the triterpenoid compound found in Schisandra chinensis. This compound exhibits significant cytotoxicity against human breast cancer cells, particularly MCF-7, with an IC50 value of 8.06 μM. Schisandronic acid effectively induces apoptosis through the upregulation of active caspase-3 and cleavage of PARP, while also reducing reactive oxygen species generation, thereby demonstrating notable antioxidant properties. Its mechanisms of action make Schisandronic acid a valuable tool for cancer research and therapeutic investigations.

Cat. No.

A37130

CAS No.

1645286-58-3

AZ1366

AZ1366 is a potent orally active inhibitor of tankyrase, a key regulator of the Wnt signaling pathway. By stabilizing Axin2 and reducing NuMA levels, AZ1366 disrupts the tankyrase-NuMA interaction, leading to G2/M phase arrest and downregulation of β-catenin-dependent gene expression. This compound has demonstrated the ability to inhibit tumor growth in colorectal cancer xenograft models, as well as synergistically impair the proliferation of non-small cell lung cancer cells, enhancing tumor control and survival in orthotopic mouse models. AZ1366 is particularly valuable for research focused on colorectal cancer and non-small cell lung cancer.

Cat. No.

A37759

CAS No.

3056709-95-3

Polθ/PARP-IN-1

Polθ/PARP-IN-1 is a potent dual inhibitor targeting DNA polymerase theta (Polθ) and poly (ADP-ribose) polymerase (PARP), exhibiting IC50 values of 45.6 nM and 5.4 nM, respectively. This compound demonstrates significant antiproliferative activity by inducing apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage. Polθ/PARP-IN-1 is applicable in cancer research and may contribute to therapeutic strategies targeting tumorigenesis.

Cat. No.

A39902

CAS No.

2756333-39-6

Palacaparib

Synonyms: AZD-9574

Palacaparib is a potent inhibitor of PARP1, demonstrating over 8000-fold selectivity for PARP1 relative to PARP2, PARP3, PARP5a, and PARP6. It functions by selectively inhibiting PARP1 and trapping it at sites of single-strand breaks (SSBs), impeding DNA repair. This compound is investigated primarily for its anti-cancer properties, particularly in research related to HRD+ breast cancer and various advanced solid tumors.

Cat. No.

A56926

CAS No.

374069-33-7

PARP-1-IN-32

PARP-1-IN-32 is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). This compound is utilized in cancer research to investigate the mechanisms of DNA repair and cellular response to genotoxic stress. Its ability to selectively inhibit PARP-1 makes it a valuable tool for studying the role of this enzyme in tumor biology and therapeutic resistance.

Cat. No.

A79665

CAS No.

684276-17-3

L-2286

L-2286 is a potent orally active inhibitor of PARP-1. This compound demonstrates significant biological activity by alleviating carotid artery remodeling, reducing oxidative stress and inflammation in spontaneously hypertensive rats, while also providing neuroprotective effects in the dorsal hippocampus. L-2286 is applicable in research focused on hypertension and its associated vascular and neurological complications.

Cat. No.

A84556

CAS No.

2661609-36-3

DP-C-4

DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies.

Cat. No.

B21981

CAS No.

2819998-77-9

PARP7-IN-25

PARP7-IN-25 is a potent PARP7 inhibitor, exhibiting an IC50 of 1.582 nM. This compound effectively inhibits the enzymatic activity of PARP7, leading to reduced proliferation in lung cancer cells. PARP7-IN-25 is valuable for research focused on PARP7-related cancer pathways and therapeutic strategies targeting this enzyme.