parp1 in 6

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

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) 是一种PARP1抑制剂（IC50: 0.41 nM），具有保护视网膜细胞的功能，其EC50为0.02 nM（抑制过氧化氢诱导的人视网膜色素上皮细胞的MTS活性）。

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。

Phosphoramide mustard cyclohexanamine（磷酰胺氮芥环己胺盐）是cyclophosphamide的活性代谢物，是一种交联DNA链的烷基化剂，组织细胞分裂并导致细胞死亡，具有抗肿瘤活性。

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）是一款针对PARP1的抑制剂，能够抑制坦聚合酶(TNKS)并促进DNA双链断裂损伤。该化合物在诱导肿瘤细胞凋亡(apoptosis)方面具有显著作用，且在三阴性乳腺癌(TNBC)细胞及来源于TNBC患者的类器官中显示出抗癌活性，适用于探究BRCA1突变状态下的TNBC研究。