PARP

Cat. No.

A29114

CAS No.

2892065-01-7

PARP10/15-IN-1

PARP10/15-IN-1 is a selective inhibitor targeting both PARP10 and PARP15, exhibiting IC50 values of 160 nM and 370 nM, respectively. This compound serves as a valuable tool for cancer research, enabling the investigation of PARP10 and PARP15's roles in tumorigenesis and therapeutic resistance. Its dual inhibitory properties facilitate studies aimed at understanding the molecular mechanisms of cancer progression and the potential for targeted therapies.

Cat. No.

A29115

CAS No.

2225800-19-9

PARP10-IN-3

PARP10-IN-3 is a selective inhibitor of the mono-ADP-ribosyltransferase PARP10, exhibiting an IC50 of 480 nM against human PARP10. Additionally, it demonstrates significant inhibitory activity towards PARP2 and PARP15 with IC50 values of 1.7 μM. This compound serves as a valuable tool in research applications targeting the role of PARP enzymes in cellular processes and their implications in various diseases, including cancer.

Cat. No.

A29116

CAS No.

1551355-46-4

Simmiparib

Simmiparib is a potent and orally active inhibitor of PARP1 and PARP2, demonstrating IC50 values of 1.75 nM and 0.22 nM, respectively. This compound effectively induces the accumulation of DNA double-strand breaks and triggers G2/M phase arrest in homologous recombination repair-deficient cells, leading to apoptosis. Simmiparib exhibits significant antitumor activity in various cancer models, including xenografts in nude mice, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A29117

CAS No.

2823308-89-8

PARP1-IN-5 dihydrochloride

PARP1-IN-5 dihydrochloride is a potent and selective inhibitor of PARP-1, with an IC50 of 14.7 nM. This compound exhibits low toxicity and is suitable for oral administration. PARP1-IN-5 dihydrochloride is primarily utilized in cancer research to investigate the role of PARP-1 in tumorigenesis and therapy resistance.

Cat. No.

A29118

CAS No.

3024030-10-9

PARP7-IN-17

PARP7-IN-17 is a potent PARP7 inhibitor with an IC50 of 4.5 nM, demonstrating effective oral bioavailability. This compound exhibits significant antitumor activity, making it a valuable tool for research into cancer therapeutics and the biological role of PARP7 in tumorigenesis. Its selective inhibition of PARP7 may aid in the development of targeted cancer treatments.

Cat. No.

A29119

CAS No.

2946705-91-3

PARP7-IN-22

PARP7-IN-22 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. This compound is orally active and enhances type I interferon signaling in vitro, facilitating T cell infiltration into tumor tissues and significantly inhibiting tumor growth. PARP7-IN-22 is of particular interest for research in cancer immunotherapy, providing valuable insights into therapeutic strategies that target immune responses in oncology.

Cat. No.

A29121

CAS No.

2136325-05-6

PARP7-IN-16 free base

PARP7-IN-16 free base is a selective, orally active inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound is valuable for investigating the role of PARP enzymes in DNA repair mechanisms and is particularly relevant in studies focused on breast and prostate cancer. Researchers can utilize PARP7-IN-16 free base to explore therapeutic strategies targeting these types of malignancies.

Cat. No.

A29122

CAS No.

2482484-87-5

PARP1-IN-11

PARP1-IN-11 is a selective inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating a potent inhibitory activity with an IC50 value of 0.082 µM. This compound exhibits complete inhibition of PARP2 and significantly inhibits the activity of PARP3, as well as tankyrases TNKS1 and TNKS2. PARP1-IN-11 is valuable for research applications focused on DNA repair mechanisms, cancer therapeutics, and the study of cellular responses to genotoxic stress.

Cat. No.

A29123

CAS No.

2569517-30-0

RBN012811

RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections.

Cat. No.

A29124

CAS No.

2640677-68-3

PARP1-IN-33

PARP1-IN-33 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.41 nM. This compound demonstrates significant cytoprotective effects on retinal cells, with an EC50 of 0.02 nM in inhibiting MTS activity in H2O2-induced human retinal pigment epithelial cells. PARP1-IN-33 is valuable for research applications aimed at understanding retinal oxidative stress and developing therapeutic strategies for retinal diseases.

Cat. No.

A29125

CAS No.

420849-22-5

TIQ-A

TIQ-A is a potent inhibitor of TNKS2 (tankyrase 2), exhibiting an IC50 of 24 nM. This compound has shown promise as an anti-ischemic agent, potentially modulating pathways involved in ischemic injury. It serves as a valuable tool for research focused on cellular stress responses and the role of TNKS2 in various diseases.

Cat. No.

A29128

CAS No.

272769-49-0

A-620223

A-620223 is a potent inhibitor of PARP-1, exhibiting a Ki of 8 nM and an EC50 of 3 nM in whole cell assays. This compound demonstrates significant in vivo efficacy in murine models, particularly in the B16F10 melanoma model when used in combination with Temozolomide and in the MX-1 breast xenograft model with Cisplatin. A-620223 is suitable for research applications focusing on melanoma and breast cancer therapy.

Cat. No.

A29129

CAS No.

2589531-76-8

Saruparib

Synonyms: AZD5305

Saruparib is a potent and selective PARP inhibitor, primarily targeting PARP1 with an IC50 value of 3 nM and PARP2 with an IC50 of 1400 nM. This orally active compound demonstrates significant anti-proliferative effects and is particularly effective in inhibiting the growth of cells exhibiting deficiencies in DNA repair mechanisms. Saruparib is commonly utilized in research focused on cancer treatment strategies, particularly in the context of homologous recombination repair-deficient tumors.

Cat. No.

A29131

CAS No.

1358715-18-0

Fluzoparib

Synonyms: SHR3162; Fuzuloparib

Fluzoparib is a highly potent oral inhibitor of PARP1, demonstrating an IC50 of 1.46 ± 0.72 nM in cell-free enzymatic assays. This compound selectively targets homologous recombination repair (HR)-deficient cells while sensitizing both HR-deficient and HR-proficient cells to cytotoxic agents. With favorable pharmacokinetic properties in vivo, Fluzoparib is an important reagent for studying BRCA1/2-mutant relapsed ovarian cancer and related therapeutic strategies.

Cat. No.

A29133

CAS No.

2360851-29-0

RBN012759

RBN012759 is a potent and selective inhibitor of PARP14, exhibiting an IC50 of less than 3 nM. It demonstrates 300-fold selectivity for monoPARPs and 1000-fold selectivity for polyPARPs. RBN012759 has been shown to diminish pro-tumor macrophage activity and trigger inflammatory responses in tumor explants, making it a valuable tool for research in cancer biology and immune modulation.

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.