GK921-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGK921Cat. No.: HY-12337CAS No.: 1025015-40-0分式: CHNO分量: 344.41作靶点: Others作通路: Others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 : 30 mg/mL (87.11 mM)* means soluble, but saturation unknow

2、n.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9035 mL 14.5176 mL 29.0352 mL5 mM 0.5807 mL 2.9035 mL 5.8070 mL10 mM 0.2904 mL 1.4518 mL 2.9035 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 GK921转氨酰胺酶2 (TGase2) 抑制剂，对类重 组TGase2的IC50值为7.71 M。IC50 & Target IC50: 7.71 M (TG

3、ase) 1体外研究GK921 inhibits the TGase 2-induced polymerization of I-B and p53 in a dose-dependent manner. Thecytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.0510-7 M. GK9211/2 Master of Small Molecules 您边的抑制剂师www.MedChemErescues p53 levels and consequently induces apopt

4、osis; a concentration-dependent increase in cleavedpoly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed 1.体内研究 A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN andCAKI-1 preclinical xenograft tumor models 1.PROTOCOLKinase Assay 1 TGase 2

5、from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substratesolution containing 2MCE has not independently confirmed the accuracy of these methods. They are for

6、reference only.Cell Assay 1 Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1,2.5, 5 M), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control 1.MCE has not independently c

7、onfirmed the accuracy of these methods. They are for reference only.Animal Mice: GK921 is dissolved in DMSO. Vehicle alone and GK921 (8 mg/kg) are administered orally once perAdministration 1 day, 5 days/week, for 64 days. The size of the primary tumors is measured every 2-3 days using calipers.Tumo

8、r volume is calculated 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 Cancer Res. 2017 Sep 15;77(18):4973-4984.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014May;140(5):757-67.McePdfHeightCaution: Product has not been fully validated for medical applicat