|2-(4-(3-((4-氧代-3,4-二氢酞嗪-1-基)甲基)苯甲酰基)哌嗪-1-基)烟腈|CsnPharm

CAS No.: 1825345-33-2

AZ9482 is a PARP inhibitor with IC50 values of 1, 1, 46, 640, 9, and 160nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively.

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400-920-2911

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描述Poly(ADP-ribose)polymerase-1 (PARP1) is a DNA repair enzyme highly expressed in the nuclei of mammalian cells. PARP inhibitors, moreover, can be used to induce synthetic lethality in cells where the homologous recombination (HR) pathway is deficient^[2]. PARP enzymes are broadly involved in the cellular response to DNA damage. PARP-1 is the chief human PARP enzyme involved in the DNA damage response, acting as a first responder that detects DNA strand breaks, and contributes to repair pathway choice and the efficiency of repair through modulation of chromatin structure and through interaction with and modification of a multitude of DNA repair factors^[3]. PARP inhibitors can trap the PARP-1 protein at a single-stranded break/DNA lesion and disrupt its catalytic cycle, ultimately leading to replication fork progression and consequent double-strand breaks. ^[4].BRCA1 and BRCA2 proteins are essential for high-fidelity repair of double-strand breaks of DNA through the homologous recombination repair (HRR) pathway. Deficiency in HRR (HRD) is a target for PARP inhibitors^[5]. Inhibition of PARP function results in cell death in HR-deficient tumors, and sensitizes tumor cells to cytotoxic agents that induce DNA damage^[6]. 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^[7].
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CAS号	1825345-33-2	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H22N6O2	运输	蓝冰
分子量	450.49	别名

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