parp-6

AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. Consistent with this lack of potencytowards tankyrase, AZ0108 is not active in a DLD-1 Wnt luciferase reporter assay.

Rucaparib (PF-01367338) 是一种 PARP 蛋白抑制剂 (PARP-1 Ki=1.4 nM) 和六磷酸己糖脱氢酶 (H6PD) 抑制剂，具有口服活性。Rucaparib 具有抗肿瘤活性，对去势抵抗性前列腺癌 (CRPC) 有活性。

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.

AZ9482 是一种选择性 PARP1 2 6的三重抑制剂，IC50值分别为 1 、1 和640 nM。

PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC 50 values of 0.94 and 0.48 μM, respectively.

5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) 是一种Cudrania tricuspidata 的提取物，通过激活 Nrf2 ARE 信号对 6-OHDA 诱导的氧化应激和细胞凋亡发挥神经保护作用。它抑制 6-OHDA 诱导的 SH-SY5Y 细胞中活化的caspase-3，caspase-9以及切割的PARP 表达。

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]

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP + - NU1085 (10 microM) for 72 h.

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.

6-Methoxypurine-9-β-D-5’(R)-C-methylriboside 是一种嘌呤碱基，属于次黄嘌呤似物，主要在肌肉组织中发现。作为黄嘌呤在嘌呤氧化酶作用下的代谢产物，次黄嘌呤具备显著的抗炎性质，并可作为内源性 poly(ADP-ribose) polymerase (PARP) 的抑制剂。其通过抑制 PARP 活性，防止过氧亚硝酸盐引起的线粒体去极化及次级超氧化物的产生，展现出细胞保护作用。同时，次黄嘌呤也被用作缺氧的生物标志物。

Nudifloramide 是烟酰胺-腺嘌呤二核苷酸 (NAD) 降解的一种最终产物，可显著抑制PARP-1活性。

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) 是一种从蛇麻草中提纯的具有多种生物功能的天然产物。黄腐酚对 HIV-1 有效，可能是一种有趣的先导化合物。它可能代表一种用于 HIV-1 感染的新型化疗药物。