HAMNO-NSC111847-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHAMNOCat. No.: HY-111285CAS No.: 138736-73-9Synonyms: NSC111847分式: CHNO分量: 263.29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 : 155 mg/mL (588.70 mM; Need ultrasonic

2、and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.7981 mL 18.9905 mL 37.9809 mL5 mM 0.7596 mL 3.7981 mL 7.5962 mL10 mM 0.3798 mL 1.8990 mL 3.7981 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 HAMNO复制蛋 A (RPA) 的新型蛋质相互作抑制剂。IC50 & Target RPA 1体外研究HAMNO is a novel p

3、rotein interaction inhibitor of replication protein A (RPA). RPA is involved in theATR/Chk1 pathway. HAMNO alone inhibits colony formation in both HNSCC cell lines in the low micromolar1/2 Master of Small Molecules 您边的抑制剂师www.MedChemErange. HAMNO combined with etoposide significantly inhibits colony

4、 formation to a greater degree thanHAMNO alone. After UMSCC38 cells are exposed to HAMNO, increased pan-nuclear -H2AX stainingoccurs in a dose dependent manner. Cancer derived UMSCC38 cells, as well as another cancer cell line,UMSCC11B, have prominent -H2AX staining, particularly after incubation wi

5、th 20 M HAMNO. BothUMSCC38 and OKF4 cells present increased -H2AX staining after addition of HAMNO, with the greatestincrease in signal occurring in S-phase 1.体内研究 In mice, HAMNO slows the progression of UMSCC11B tumors. Ser33 of RPA32, an ATR substrate, is highlyphosphorylated after two hours of tr

6、eatment with 20 M of etoposide, which is reduced with the addition of 2M HAMNO, and is nearly absent at higher concentrations, demonstrating an in vivo effect of HAMNO as aninhibitor of RPA32 phosphorylation by ATR 1.PROTOCOLCell Assay 1 Cell cycle assessment and -H2AX staining are monitored in UMSC

7、C38 and OKF4 cells after 2 h incubationwith HAMNO (2, 20, 50 M) and fixed in 70% ethanol overnight. Cells are washed with PBS and incubatedovernight in PBS containing 1% BSA, 10% goat serum and PS139-H2AX antibodies, washed and incubatedin goat anti-mouse Alexa Fluor 647 antibody for 30 min at room

8、temperature. Cells are incubated in 50 g/mLpropidium iodide and 100 g/mL RNase A for 30 min, and 10,000 cells per sample are analyzed 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Athymic nude mice are used in this study. UMSCC38 and UMSCC11B

9、 cells are implanted into 6-week-oldAdministration 1 female mice by a single subcutaneous injection of tumor cells (2 to 6105 cells in 100 mL of sterile PBS).The growth rates of tumors are determined by daily monitoring of tumor volume with vernier calipers tumorvolume=1/2(lengthwidth2). Once the tu

10、mor size reaches 50 mm3, etoposide (10 mg/kg mouse) andHAMNO (2 mg/kg) are administered intraperitoneally every day for 3 days. Tumor size is monitored daily andthe volume of the tumor is compared among all experimental groups. At least three mice are used per group1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Glanzer JG, et al. RPA inhibition increases replication stress and suppresses tumor growth. Cancer Res. 2014 Sep 15;74(18):5165-72.McePdfHeightCaution: Product has not been