parp1 in 6

PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM for PARP-1.

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

PARP1-IN-33 (Example 6) is a PARP1 inhibitor with an IC50 of 0.41 nM. It demonstrates protective effects on retinal cells, exhibiting an EC50 of 0.02 nM in inhibiting hydrogen peroxide-induced MTS activity in human retinal pigment epithelial cells.

AZ9482 is a selective and potent inhibitor of PARP featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent activity of centrosome declustering with EC50 of < 18 nM in HeLa cells.

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels.

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis. It exhibits anti-cancer activity in triple-negative breast cancer (TNBC) cells and patient-derived organoids, making it useful for TNBC research, including cases with or without BRCA1 mutations [1].