PARP

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.

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.

Cat. No.

B22007

CAS No.

1574367-80-8

PARP1-IN-56

PARP1-IN-56 is a potent inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), a key enzyme involved in DNA repair mechanisms. This compound can be radiolabeled with isotopes such as 211At or 125I, facilitating its application as an α-emitting radiotherapeutic agent in oncological research. PARP1-IN-56 has significant potential for studying cancer therapy by targeting PARP1's role in tumor survival and proliferation.

Cat. No.

B22026

CAS No.

1301757-19-6

MC2050

MC2050 is a selective inhibitor of PARP-1, exhibiting an IC50 of 119 nM. This compound effectively reduces hyperactivation of PARP-1 prompted by oxidative stress and lowers the levels of poly(ADP-ribosyl)ation on histone H1. MC2050 demonstrates protective effects against oxidative stress-mediated cell death in neuroblastoma cells induced by hydrogen peroxide. It is particularly valuable for research in the areas of neuroblastoma and Burkitt lymphoma.