PARP

Cat. No.

A29135

CAS No.

1858179-75-5

Basroparib

Synonyms: STP1002

Basroparib is a selective inhibitor of tankyrase (TNKS1/TNKS2) with IC50 values of 29.94 nM and 3.68 nM, respectively, and exhibits limited activity against PARP1 (IC50 > 10 μM). This compound stabilizes AXIN1/2 proteins and effectively disrupts the Wnt/β-catenin signaling pathway, leading to inhibition of tumor cell proliferation and induction of apoptosis. Basroparib is particularly relevant for research in colorectal cancer (CRC) models bearing KRAS mutations, such as G12V/G12D, and demonstrates potential to overcome resistance to MEK inhibitors, providing synergistic antitumor effects.

Cat. No.

A29136

CAS No.

55-21-0

Benzamide

Synonyms: Benzenecarboxamide; Phenylamide

Benzamide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), demonstrating significant neuroprotective effects. It has been shown to protect against neurotoxicity induced by glutamate and methamphetamine in vitro. In vivo studies indicate that Benzamide can mitigate methamphetamine-induced dopamine depletions in mice without acute effects on striatal dopamine metabolism or body temperature regulation. Its dual role in neuroprotection and PARP inhibition makes it a valuable tool in neuropharmacology research.

Cat. No.

A29137

CAS No.

943119-42-4

OUL232

OUL232 is a potent inhibitor of poly(ADP-ribose) polymerase 10 (PARP10) and other mono-ADP-ribosyl transferases including PARP7, PARP11, PARP12, PARP14, and PARP15. With an IC50 of 7.8 nM, OUL232 represents the most effective PARP10 inhibitor characterized to date and is the first reported inhibitor targeting PARP12. This compound is valuable for studying the biological roles of PARP10 and PARP12 in cellular processes and may facilitate research into therapeutic strategies involving these targets.

Cat. No.

A30560

CAS No.

1212595-23-7

TopBP1-IN-1

TopBP1-IN-1 is a selective inhibitor of TopBP1, a key regulator in DNA damage response pathways. This compound demonstrates synergistic effects when used in conjunction with PARP inhibitors, enhancing their antitumor efficacy. TopBP1-IN-1 is applicable in preclinical research focused on cancer biology and the exploration of combinatorial therapeutic strategies aimed at improving treatment outcomes for tumors with DNA repair deficiencies.

Cat. No.

A30628

CAS No.

1613220-15-7

Niraparib tosylate hydrate

Synonyms: MK-4827 tosylate hydrate

Niraparib tosylate hydrate is a potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 3.8 nM and 2.1 nM, respectively. This compound functions by disrupting the DNA repair mechanism, leading to the accumulation of DNA damage and subsequent activation of apoptosis. Niraparib tosylate hydrate demonstrates significant anti-tumor activity, making it a valuable tool for cancer research, particularly in studies focused on DNA repair pathways and therapeutic resistance.

Cat. No.

A30895

CAS No.

1449746-00-2

Mefuparib hydrochloride

Synonyms: MPH

Mefuparib hydrochloride is a selective inhibitor of PARP1 and PARP2, demonstrating substrate-competitive activity with IC50 values of 3.2 nM and 1.9 nM, respectively. This potent compound induces apoptosis and exhibits significant anticancer effects in both in vitro and in vivo models. It is valuable for research in cancer therapeutics and cellular response mechanisms to DNA damage.

Cat. No.

A30916

CAS No.

2892064-88-7

PARP10/15-IN-3

PARP10/15-IN-3 is a dual inhibitor targeting PARP10 and PARP15, exhibiting IC50 values of 0.14 µM and 0.40 µM, respectively. This compound effectively penetrates cellular membranes and has demonstrated the ability to rescue cells from apoptosis. PARP10/15-IN-3 serves as a valuable tool for investigating the roles of PARP10 and PARP15 in cellular processes and offers potential applications in studies related to cancer therapy and cell survival mechanisms.

Cat. No.

A31137

CAS No.

2892064-99-0

PARP10/15-IN-2

PARP10/15-IN-2 is a potent dual inhibitor of PARP10 and PARP15, exhibiting IC50 values of 0.15 µM and 0.37 µM, respectively. This compound has demonstrated the ability to penetrate cellular membranes and effectively rescue cells from apoptosis. PARP10/15-IN-2 serves as a valuable tool for research into cell survival mechanisms and the modulation of PARP-related signaling pathways.

Cat. No.

A31240

CAS No.

2337386-47-5

PARP/PI3K-IN-1

PARP/PI3K-IN-1 is a potent inhibitor of both PARP and PI3K, exhibiting pIC50 values of 8.22 for PARP-1, 8.44 for PARP-2, and varying activity against PI3K isoforms with values of 8.25 for PI3Kα, 6.54 for PI3Kβ, 8.13 for PI3Kδ, and 6.08 for PI3Kγ. This compound demonstrates significant anticancer activity and is suitable for research applications targeting a variety of oncological disorders. Its dual inhibition may provide insights into therapeutic strategies for cancer treatment.

Cat. No.

A31479

CAS No.

763111-49-5

KU-0058948

KU-0058948 is a potent inhibitor of PARP1, exhibiting an IC50 value of 3.4 nM. This compound induces cell cycle arrest and apoptosis in primary myeloid leukemic cells as well as established myeloid leukemic cell lines. It is suitable for research applications focused on cancer biology and the exploration of PARP1's role in cellular processes.

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.