PARP

Cat. No.

A29082

CAS No.

489457-75-2

PARP-1/2-IN-5

PARP-1/2-IN-5 is a potent inhibitor of PARP-1 and PARP-2, with IC50 values of 118 nM and 11 nM, respectively. This compound is ideal for investigating its role in inflammatory diseases and neurodegenerative disorders, providing valuable insights into the therapeutic potential of PARP inhibition in these conditions. Researchers can utilize PARP-1/2-IN-5 to explore the molecular mechanisms underlying these diseases and assess potential treatment strategies.

Cat. No.

A29083

CAS No.

1201832-32-7

HYDAMTIQ

HYDAMTIQ is a potent inhibitor of PARP-1 and PARP-2, exhibiting an IC50 range of 29-38 nM. It demonstrates significant anticancer activity, targeting various malignancies such as ovarian, breast, prostate, pancreatic cancers, and glioblastoma multiforme. Additionally, HYDAMTIQ shows anti-inflammatory properties by reducing pulmonary PARP activity and can alleviate symptoms associated with allergen-induced cough and dyspnea. It also exhibits protective effects in in vivo models of cerebral ischemia, asthma, and cancer.

Cat. No.

A29084

CAS No.

1207454-56-5

(rac)-Talazoparib

Synonyms: (rac)-BMN-673; (rac)-LT-673

(rac)-Talazoparib is a potent inhibitor of PARP1 and PARP2, with Ki values of 1.2 nM and 0.87 nM, respectively. This orally active compound effectively inhibits cellular PARylation, demonstrating an EC50 of 2.51 nM. It induces DNA damage accumulation and significantly suppresses the proliferation of BRCA1/2-mutated cell lines, including MX-1 and Capan-1, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib shows antitumor efficacy in various mouse models, making it a valuable tool for cancer research.

Cat. No.

A29085

CAS No.

836640-15-4

PARP1-IN-8

PARP1-IN-8 is a potent inhibitor of the PARP1 enzyme, exhibiting an IC50 of 97 nM. This compound demonstrates significant anti-proliferative effects on the human lung adenocarcinoma cell line A549. It is suitable for research applications focused on cancer biology and the therapeutic potential of PARP1 modulation in oncology.

Cat. No.

A29086

CAS No.

1606995-47-4

Itareparib

Itareparib is a PARP inhibitor that demonstrates significant antineoplastic activity by preventing the repair of DNA damage in cancer cells. This mechanism enhances cell death in tumor tissues, making it a valuable reagent for cancer research, particularly in studies involving homologous recombination repair deficiencies. Its application extends to exploring combination therapies and resistance mechanisms in oncology.

Cat. No.

A29088

CAS No.

1584646-59-2

TNKS-IN-2

TNKS-IN-2 is a potent and selective inhibitor of tankyrase (TNKS), exhibiting pIC50 values of 8.1 and 7.0 for TNKS and Wnt, respectively. This compound effectively modulates the Wnt signaling pathway by targeting TNKS, making it a valuable tool for research involving cellular growth and differentiation. TNKS-IN-2 is useful for studies investigating the role of tankyrases in cancer biology and other diseases associated with altered Wnt signaling.

Cat. No.

A29090

CAS No.

2411890-36-1

PARP11 inhibitor ITK7

Synonyms: ITK7

PARP11 inhibitor ITK7 is a potent and selective inhibitor targeting PARP11. It demonstrates strong inhibitory activity with an IC50 of 14 nM, making it a valuable tool for investigating the biological roles of PARP11. This compound can be utilized in research exploring cellular localization and the functional implications of PARP11 in various cellular contexts.

Cat. No.

A29091

CAS No.

133314-07-5

FeTMPyP

FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor that exerts protective effects against cell death and mitochondrial dysfunction. It significantly mitigates nitrotyrosine formation and depolarization of the mitochondrial transmembrane potential. FeTMPyP has been shown to alleviate homocysteine-induced nitrosative stress, improve functional and behavioral outcomes in neuropathic pain models, and reduce acute cerebral infarction in ischemic conditions. This compound is valuable for research related to renal aging, ischemic penumbra, and hyperglycemic strokes.

Cat. No.

A29092

CAS No.

2360853-16-1

RBN-3143

RBN-3143 is a potent NAD+-competitive inhibitor of PARP14, exhibiting an IC50 of 4 nM. This compound effectively inhibits PARP14-mediated ADP-ribosylation and stabilizes the enzyme in cellular contexts. RBN-3143 is ideal for investigating the role of PARP14 in lung inflammation and other related research applications.

Cat. No.

A29093

CAS No.

2991637-98-8

DB008

DB008 is a selective inhibitor of the enzyme PARP16, demonstrating a potent inhibitory effect with an IC50 value of 0.27 μM. This compound features a membrane-permeable acrylamide electrophilic moiety, enabling specific targeting of PARP16. Additionally, DB008 contains an alkyne group that allows for click chemistry applications, specifically facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its unique properties make it a valuable tool for biochemical and molecular biology research involving PARP16.

Cat. No.

A29094

CAS No.

129075-73-6

DPQ

DPQ is a selective inhibitor of PARP-1, effectively blocking PARP-1-mediated DNA repair mechanisms and reducing the consumption of NAD+ and ATP. This inhibition leads to a decrease in NF-κB pathway activation, resulting in lowered expression of pro-inflammatory cytokines such as TNF-α and IL-6, along with a reduction in oxidative stress levels. DPQ is applicable in research focused on inflammation-related conditions including acute lung injury, myocardial infarction, and neurodegenerative diseases.

Cat. No.

A29095

CAS No.

1401682-78-7

Senaparib

Synonyms: IMP4297; JS109

Senaparib is a potent and selective inhibitor of PARP1 and PARP2, functioning through the inhibition of DNA repair pathways. Its mechanism disrupts the ability of cancer cells to repair DNA damage, leading to increased antitumor activity. Senaparib has demonstrated significant efficacy in various preclinical cancer models, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A29096

CAS No.

2406278-81-5

OM-153

OM-153 is a potent inhibitor of tankyrase 1 and tankyrase 2 (TNKS1/2), exhibiting IC50 values of 13 nM and 2 nM, respectively. This compound effectively inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 of 0.63 nM. Research applications include the investigation of Wnt/β-catenin signaling pathways and the effects of proliferation in COLO 320DM cells.

Cat. No.

A29097

CAS No.

1681017-83-3

Venadaparib

Synonyms: IDX-1197

Venadaparib is a selective and potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 1.4 nM and 1.0 nM, respectively. This orally active compound effectively impedes the repair of DNA single-strand breaks (SSB). Venadaparib is relevant for research applications targeting solid tumors and investigating the role of PARP in DNA damage response pathways.

Cat. No.

A29098

CAS No.

5154-02-9

1,5-Isoquinolinediol

1,5-Isoquinolinediol is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), exhibiting an IC50 range of 0.18-0.37 μM. This compound is particularly effective in mitigating diabetes-induced oxidative stress through the inhibition of NADPH oxidase in retinal tissues. Its ability to modulate cellular responses to oxidative stress makes it a valuable tool for research into diabetes-related complications and neuroprotection.

Cat. No.

A29099

CAS No.

1460286-21-8

MSC2504877

Synonyms: M2912

MSC2504877 is a potent and orally active tankyrase inhibitor, exhibiting IC50 values of 0.0007 µM for TNKS, 0.0008 µM for TNKS2, and 0.54 µM for PARP1. This compound effectively increases AXIN2 and TNKS protein expression while decreasing β-catenin levels, indicating its role in the regulation of key signaling pathways. MSC2504877 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies targeting the Wnt signaling pathway.

Cat. No.

A29100

CAS No.

763111-47-3

N-Descyclopropanecarbaldehyde Olaparib

N-Descyclopropanecarbaldehyde Olaparib is a potent PARP inhibitor, serving as an analogue of Olaparib with a DOTA moiety. This compound is utilized in the synthesis of novel dual EGFR and PARP PROTAC, designated as DP-C-4. Additionally, N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophores, enabling its application in positron emission tomography (PET) and optical imaging for various tumor types.

Cat. No.

A29101

CAS No.

1380359-84-1

PARPi-FL

Synonyms: Olaparib-bodipy FL

PARPi-FL is a small-molecule fluorescent inhibitor targeting PARP1. It binds selectively to PARP1 and is utilized as a fluorescent imaging agent, facilitating tumor detection, diagnosis, and surgical guidance. This compound serves as a valuable tool in cancer research, offering insights into PARP1 activity in various biological contexts.

Cat. No.

A29102

CAS No.

2819998-97-3

PARP7-IN-15

PARP7-IN-15 is a selective inhibitor of PARP7, exhibiting an IC50 of 0.56 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its potency in inhibiting PARP7 can facilitate studies focused on DNA repair mechanisms and cancer cell proliferation.

Cat. No.

A29103

CAS No.

2055357-64-5

Nesuparib

Synonyms: JPI-547/OCN-201

Nesuparib is a potent inhibitor of PARP 1 and 2, as well as Tankyrase 1 and 2, with IC50 values of 5 nM, 1 nM, and 2 nM, respectively. This orally bioavailable compound demonstrates significant antitumor activity, making it a valuable tool for researching advanced solid tumors. Its selective inhibition of critical DNA repair pathways highlights its potential in cancer therapy and provides important insights into targeted treatment strategies.

Cat. No.

A29104

CAS No.

1825345-33-2

AZ9482

AZ9482 is a potent inhibitor of PARP1, PARP2, and PARP6, exhibiting IC50 values of 1 nM for both PARP1 and PARP2, and 640 nM for PARP6. This compound effectively disrupts the DNA repair pathway in cancer cells, making it a valuable tool for studying cellular response to DNA damage. AZ9482 is appropriate for applications in cancer research, particularly in the context of synthetic lethality and therapeutic resistance.

Cat. No.

A29106

CAS No.

2435657-10-4

PARP7-IN-16

PARP7-IN-16 is a selective and orally bioavailable 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 serves as a valuable research tool for investigating the roles of PARP enzymes in cellular processes and their implications in oncogenesis. It is particularly relevant for studies focusing on breast cancer and prostate cancer, providing insights into therapeutic strategies that target DNA repair mechanisms.

Cat. No.

A29107

CAS No.

2171388-28-4

RK-582

RK-582 is a potent tankyrase inhibitor that demonstrates antitumor activity with an IC50 of 36.1 nM against human tankyrase-1 and 39.2 nM against human tankyrase-2. This compound specifically targets APC-mutated colorectal cancer cells, where its efficacy is linked to levels of active β-catenin, while resistance is associated with PIK3CA mutations. RK-582 is valuable for research focused on colorectal cancer mechanisms and therapeutic strategies.

Cat. No.

A29109

CAS No.

3032324-56-1

PROTAC PARP1 degrader-1

PROTAC PARP1 degrader-1 is a potent degrader targeting PARP1 through the PROTAC mechanism. This compound facilitates the activation of the cGAS/STING immune pathway, enhancing T cell-mediated cytotoxicity against tumor cells. Additionally, by inhibiting DNA damage repair, PROTAC PARP1 degrader-1 promotes the accumulation of cytosolic DNA fragments, making it a valuable tool for research in cancer immunotherapy and the study of DNA repair mechanisms.

Cat. No.

A29110

CAS No.

130017-40-2

K-756

K-756 is a selective tankyrase (TNKS) inhibitor that effectively inhibits the ADP-ribosylation activity of TNKS1 and TNKS2, exhibiting IC50 values of 31 nM and 36 nM, respectively. This compound plays a significant role in the study of various cancer-related pathways and cellular processes influenced by tankyrase activity. K-756 is applicable in research focused on DNA repair mechanisms, cellular signaling, and the modulation of Wnt signaling pathways.