NSC-228155 _EGFR Activator - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC 228155Cat. No.: HY-101084CAS No.: 113104-25-9分式: CHNOS分量: 290.25作靶點(diǎn): EGFR; Histone Acetyltransferase; Epigenetic Reader Domain作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK;Epigenetics儲存式: Powder -20C 3 years4C 2 years

2、In solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 16 mg/mL (55.12 mM; Need ultrasonic)H2O : 90% corn oilSolubility: 1.6 mg/mL (5.51 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 NSC 228155 為 EGFR 激活劑，可與 EGFR 的胞外區(qū)域結(jié)合，誘導(dǎo) EGFR 的磷酸化 1。NSC 228155種有效的 KIX-KI

3、D 相互作抑制劑，能夠抑制 CREB 的激酶誘導(dǎo)結(jié)構(gòu)域 (KID) 和 KIX (KID 相互作結(jié)構(gòu)域，來 CBP) 的相互作，IC50 值為 0.36 M 2。IC50 & Target EGFR KIX-KID0.36 M (IC50)體外研究 NSC 228155 (100 M) enhances EGFR tyrosine phosphorylation via action of SOD1 1.NSC 228155 (Compound 1) inhibits CREB- and VP16-CREB-mediated gene transcription in living HEK 2

4、93Tcells with IC50s of 2.09 and 6.14 M, respectively 2.NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells 2.REFERENCES1. Sakanyan V, et al. Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerizationof C

5、u/Zn SOD1. Sci Rep. 2016 Feb 17;6:21088.2. Xie F, et al. Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription.Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-589