PARP

Cat. No.

A28963

CAS No.

101494-95-5

8-Chloroquinazolin-4-ol

8-Chloroquinazolin-4-ol is a potent inhibitor of the PARP-1 enzyme, exhibiting an IC50 value of 5.65 μM. This compound serves as a nicotinamide mimic and plays a significant role in research focused on DNA repair mechanisms and cancer therapies. Its ability to modulate PARP-1 activity makes it a valuable tool for exploring therapeutic strategies in various disease models.

Cat. No.

A28964

CAS No.

53439-81-9

Benzo[c][1,8]naphthyridin-6(5H)-one

Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies.

Cat. No.

A28965

CAS No.

873075-19-5

TNKS modulator-1

TNKS modulator-1 is a small molecule targeting tankyrase (TNKS) enzymes. This compound inhibits TNKS activities, resulting in the stabilization of β-catenin and modulation of Wnt signaling pathways. Its primary applications include research in cancer biology and regenerative medicine, particularly in studying tumor growth and cellular signaling mechanisms.

Cat. No.

A28966

CAS No.

142404-10-2

BSI-401

BSI-401 is an orally active inhibitor of PARP-1, a key enzyme involved in DNA repair processes. This compound demonstrates significant anti-cancer activity, particularly in pancreatic cancer, both as a monotherapy and in combination with Oxaliplatin. BSI-401 is valuable for research into therapeutic strategies targeting DNA damage response pathways in cancer treatment.

Cat. No.

A28968

CAS No.

370872-09-6

UPF-1035

UPF-1035 is a selective inhibitor of PARP-2, exhibiting an IC50 value of 0.15 μM. This compound has been shown to increase CA1 pyramidal cell loss in the hippocampus, indicating its role in neuroprotection. UPF-1035 can be utilized in research focused on neurodegenerative diseases and the mechanisms of neuronal cell survival.

Cat. No.

A28971

CAS No.

1460285-69-1

Tankyrase-IN-5

Tankyrase-IN-5 is a potent inhibitor of tankyrase proteins TNKS1 and TNKS2, demonstrating IC50 values of 2.3 nM and 7.9 nM, respectively. This compound can effectively disrupt the poly(ADP-ribosyl)ation process, influencing various cellular functions and signaling pathways. It is primarily used in research related to cancer biology and cellular regulation, offering valuable insights into the role of tankyrases in disease mechanisms.

Cat. No.

A28972

CAS No.

2756337-27-4

PARP1-IN-19

PARP1-IN-19 is a potent inhibitor of poly (ADP-ribose) polymerase 1 (PARP1), a key enzyme involved in DNA repair mechanisms. This compound exhibits significant antitumor activity, making it a valuable tool in cancer research and therapeutic development. It is primarily utilized in studies focusing on the modulation of DNA damage response pathways and the exploration of combination therapies in oncology.

Cat. No.

A28973

CAS No.

63916-38-1

NU1064 dihydrochloride

NU1064 dihydrochloride is a selective inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair mechanisms. This compound enhances the cytotoxic effects of DNA-methylating agents, such as MTIC, in a concentration-dependent manner. It is valuable for research in cancer biology, particularly in studies focusing on enhancing the efficacy of chemotherapeutic agents and understanding mechanisms of DNA repair inhibition.

Cat. No.

A28974

CAS No.

623578-11-0

KU-0058684

KU-0058684 is a selective PARP inhibitor, exhibiting an IC50 of 3.2 nM for PARP-1. This reagent effectively impairs DNA double strand break repair, making it a valuable tool for investigating DNA damage response mechanisms. Its application extends to studying the therapeutic potential of PARP inhibition in various cancer models.

Cat. No.

A28976

CAS No.

283172-68-9

WD2000-012547

WD2000-012547 is a selective inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1), demonstrating a pKi value of 8.221. This compound effectively interferes with PARP-1 activity, which plays a crucial role in DNA repair and cellular response to DNA damage. WD2000-012547 is instrumental in research applications involving cancer therapeutics, where modulation of DNA repair pathways is of significant interest.

Cat. No.

A28977

CAS No.

1023814-45-0

OUL245

OUL245 is a selective inhibitor of PARP2, exhibiting an IC50 of 44 nM. It also demonstrates inhibitory activity against other PARP family members and TNKS enzymes, with IC50 values ranging from 2.9 to 8.8 μM. This compound is valuable for research into DNA repair mechanisms and the therapeutic potential of targeting PARP enzymes in various cancer models.

Cat. No.

A28978

CAS No.

93117-07-8

5-AIQ hydrochloride

Synonyms: 5-Aminoisoquinolin-1-one hydrochloride

5-AIQ hydrochloride is a selective inhibitor of PARP-1, an important enzyme involved in DNA repair. This compound exhibits protective effects against ischemia-reperfusion injury in liver tissue, making it a valuable tool for studying conditions related to hepatic ischemia-reperfusion. Its applications extend to research focused on oxidative stress and cell survival mechanisms, providing insights into potential therapeutic strategies for liver protection.

Cat. No.

A28979

CAS No.

3033649-17-8

PARP1-IN-22

PARP1-IN-22 is a highly potent inhibitor of poly (ADP-ribose) polymerase 1 (PARP1) with an IC50 of less than 10 nM. This compound is utilized in research focused on DNA damage repair pathways and cellular responses to oxidative stress. Its ability to inhibit PARP1 makes it valuable for studies in cancer therapy and neurodegenerative diseases, where modulation of DNA repair mechanisms is crucial.

Cat. No.

A28980

CAS No.

943650-25-7

A-620223 succinate

Synonyms: ABT-472

A-620223 succinate is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), targeting the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in cellular assays. Its excellent selectivity and bioavailability make it an invaluable tool for cancer research, enabling investigations into DNA repair mechanisms and potential therapeutic strategies. This compound is particularly useful in studies focused on the efficacy of PARP inhibition in various cancer models.

Cat. No.

A28981

CAS No.

2523017-04-9

SK-575-NEG

SK-575-NEG is a PARP1 degrader designed as a methylated counterpart of SK-575, synthesized through the methylation of the amino group in piperidine-2,6-dione. It demonstrates a strong binding affinity to PARP1, with an IC50 of 2.64 nM. However, SK-575-NEG does not induce PARP1 degradation in MDA-MB-436 and Capan-1 cell lines at concentrations up to 1 μM. This compound is valuable for research focusing on the mechanistic understanding of PARP1 inhibition and degradation pathways.

Cat. No.

A28982

CAS No.

3064731-00-3

PARP14 inhibitor 2

PARP14 Inhibitor 2 is a highly selective inhibitor targeting PARP14 with an IC50 value of less than 30 nM. This compound effectively inhibits the mono-ADP-ribosyltransferase activity of PARP14, thereby modulating signaling pathways associated with IFN-γ and IL-4. By reversing protumor macrophage polarization and inhibiting pro-inflammatory responses, PARP14 Inhibitor 2 holds promise for the investigation of diseases related to PARP14, including tumors, atopic dermatitis, and autoimmune disorders.

Cat. No.

A28983

CAS No.

1606996-12-6

PARP1-IN-36

PARP1-IN-36 is a selective inhibitor of PARP-1, characterized as a 4-carboxamido-isoindolinone derivative with a Kd value of less than 0.01 μM. This compound exhibits significant biological activity in the modulation of cellular processes associated with DNA repair, making it a valuable tool in research focused on cancer, cardiovascular diseases, nervous system injury, and inflammation. Its potent inhibition of PARP-1 serves to elucidate the role of this enzyme in various pathological contexts.

Cat. No.

A28984

CAS No.

1015-89-0

6(5H)-Phenanthridinone

6(5H)-Phenanthridinone is a potent inhibitor of PARP-1, a key enzyme involved in DNA repair processes. This compound exhibits significant immunomodulatory effects and has been shown to inhibit cell proliferation. It is employed in cancer research to explore therapeutic strategies targeting DNA repair pathways and to enhance the efficacy of chemotherapeutic agents.

Cat. No.

A28985

CAS No.

3032451-58-1

PARP1/2-IN-3

PARP1/2-IN-3 is a potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 0.2235 nM and

Cat. No.

A28987

CAS No.

116764-24-0

UNPD139734

UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology.

Cat. No.

A28988

CAS No.

3034665-49-8

PARP-1/2/7-IN-1

PARP-1/2/7-IN-1 is a highly potent inhibitor of poly (ADP-ribose) polymerases PARP-1, PARP-2, and PARP-7, demonstrating an IC50 of less than 10 nM. This compound is valuable for research applications focused on cancer biology, DNA repair mechanisms, and cellular stress responses. Its multifunctional inhibition can aid in the exploration of therapeutic strategies targeting PARP-mediated pathways in various diseases.

Cat. No.

A28989

CAS No.

3085256-81-8

PARP1-IN-48

PARP1-IN-48 is a potent and selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), exhibiting an IC50 of 3 nM against PARP1 and 170 nM against PARP2. This compound is valuable for research in oncology, virology, and metabolic disorders, facilitating investigations into the role of PARP1 in DNA repair and cellular stress responses. Its selective action makes it an essential tool for studying therapeutic pathways in cancer treatment and other disease models.

Cat. No.

A28990

CAS No.

908803-38-3

PARP1-IN-30

PARP1-IN-30 is a potent, selective inhibitor of PARP1 that exhibits cytotoxic effects in tumor cells. It effectively targets cancer cells with deficiencies in the breast cancer 1 protein (BRCA1) or BRCA2, offering a valuable tool for elucidating the role of PARP1 in DNA repair and cancer biology. This compound is particularly relevant for research applications focused on targeted cancer therapies and synthetic lethality in oncology.

Cat. No.

A28991

CAS No.

1708103-69-8

ARTD10/PARP10-IN-2

ARTD10/PARP10-IN-2 is a potent and non-selective inhibitor of the poly(ADP-ribose) polymerases, specifically targeting ARTD10/PARP10 and ARTD1/PARP1. With IC50 values of 2.0 μM and 9.7 μM, respectively, this compound effectively modulates mono-ADP-ribosyltransferase and poly(ADP-ribose) polymerase activities. Its ability to inhibit these pathways makes ARTD10/PARP10-IN-2 valuable for research on DNA repair mechanisms and therapeutic approaches in cancer treatment.

Cat. No.

A28992

CAS No.

1424500-13-9

ZINC000081009201

ZINC000081009201 is a potent inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) with an IC50 value of 1.4767 μM. This compound demonstrates significant potential for the study of triple-negative breast cancer (TNBC) by targeting PARP1-mediated repair pathways. Its inhibition may aid in elucidating the mechanisms of resistance and sensitivity in cancer treatment, making it a valuable tool for cancer research applications.