2OH-BNPP1-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE2OH-BNPP1Cat. No.: HY-102081CAS No.: 833481-73-5分式: CHNO分量: 297.35作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (336.30 mM)* means soluble, but saturation

2、unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3630 mL 16.8152 mL 33.6304 mL5 mM 0.6726 mL 3.3630 mL 6.7261 mL10 mM 0.3363 mL 1.6815 mL 3.3630 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 2OH-BNPP1種 BUB1 kinase 抑制劑，可于癌癥研究。IC50 & Target BUB1 kinase 1體外研究2OH-BNPP1

3、 (0.1-50 M) abrogates TGF signaling in a dose dependent manner. 2OH-BNPP1 dose-dependently impairs the TGF-induced phosphorylation of proteins that mediate canonical and non-canonical1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemETGF signaling in multiple cancer cell lines and normal cell lines 1.

4、體內(nèi)研究 2OH-BNPP1 (50 mg/kg) blocks TGF signaling in vivo, and significantly decreases abundance ofphosphorylated SMAD2 in tumor-bearing mice 1.PROTOCOLKinase Assay 1 In vitro kinase assays are performed using 200 ng of protein (BUB1-WT, or a kinase inactive mutant BUB1-KD), and 2 g of substrate (TGFBR

5、I-WT, TGFBRI-KD, SMAD3 or H2A) in 1X kinase buffer (50 mM Tris-HCl,150 mM NaCl, 10 mM MgCl2, 1% (v/v) Glycerol, 0.1% (v/v) Triton X 100, DTT, PMSF, Na3VO4 (1 mM each),2 mM NaF and -glycerol phosphate) in 20 L volume containing 10 Ci 32p-ATP and 300 M cold ATP.Reactions are run at 30C for 0.5-1 hour

6、and quenched using Laemmli buffer and resolved using a 4-12%Bis-Tris gel. Quantitative autoradiography is performed using a Typhoon FLA 9000 scanner.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Cell line-derived xenografts are established by i

7、mplanting 2.5106 A549 cells subcutaneously into each flankAdministration 1 of 4-6 week old male SCID mice. When tumors reach a volume between 40 to 60 mm3, mice are injectedwith a single intraperetoneal dose of SB431542 (10 mg/kg body weight), a dose previously reported to inhibitTGF signaling in mo

8、use models, or 2OH-BNPP1 (50 mg/kg), or vehicle (DMSO). Tumors are excised 4hours after treatment and fixed in formalin. Paraffin-embedded sections are stained using an antibody forphosphorylated SMAD2, and micrographs are taken with an Olympus microscope fitted with an Olympus DP-70 high resolution

9、 digital camera. The proportion of nuclei that stains positive for phosphorylated SMAD2 arecounted in three random fields per tumor per treatment condition vehicle (n=4), SB431542 (n=2), and 2OH-BNPP1 (n=5). A two -ided Students t-test is performed to assess statistical significance. Slides are adju

10、stedfor brightness and contrast with Adobe Photoshop CS2, but the micrographs undergo no furthermanipulations.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Virol. 2018 Aug 29;92(18). pii: e00254-18.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nyati S, et al. The kinase activity of the Ser/Thr kinase BUB1 promotes TGF- signaling. Sci Signal. 2015 Jan 6;8(358):ra1.McePdfHeightCaution: Product has not been fu