AZ6102 - PARP 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZ6102Cat. No.: HY-12975CAS No.: 1645286-75-4分式: CHNO分量: 428.53作靶点: PARP作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 29 mg/mL (67.67 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3336 mL 11.6678 mL 23.3356 mL5 mM 0.4667 mL 2.3336 mL 4.6671 mL10 mM 0.2334 mL 1.1668 mL 2.3336 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 AZ6102种有效的 TNKS1 和 TNKS2 双重 抑制剂，IC50 值分别为 3 nM 和 1 nM

3、，选择性是对 PARP 家族其他蛋的 100 多倍，对 PARP1，PARP2 和 PARP6 的 IC50 值分别为 2.0 M，0.5 M 和 3 M。IC50 & Target TNKS2 TNKS1 PARP1 PARP22 nM (IC50) 3 nM (IC50) 2 M (IC50) 0.5 M (IC50)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, resp

4、ectively. AZ6102alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 M, 0.5 M, and 3 M,for PARP1, PARP2, and PARP6, respectively. AZ6102 shows Wnt pathway inhibition in DLD-1 cells 1.PROTOCOLKinase Assay 1 The assay is conducted using 0.11 M of tankyrase-1 protein and 3

5、 M nicotinamide adenine dinucleotide(NAD+, 2.12 M 3H-NAD+ with a specific radioactivity of 1690 Ci/mol, 0.88 M biotin- NAD+), in pH 7.5 Trisbuffer (60 mM Tris, 1 mM DTT, 0.01% (v/v) Tween-20, 2.5 mM MgCl2, 0.3 mg/mL BSA). For IC50determination, 10 mM DMSO stock solution of a compound (AZ6102) is seq

6、uentially diluted by two-fold inDMSO, and aliquots of the diluted solutions are transferred to 384-well assay plates and mixed withTankyrase-1 solution 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Mol Med (Berl). 2019 Jun 14.See more

7、customer validations on HYPERLINK / www.MedChemEREFERENCES1. Johannes JW, et al. Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivopharmacology. ACS Med Chem Lett. 2015 Jan 13;6(3):254-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use