KG-501-Naphthol-AS-E-phosphate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKG-501Cat. No.: HY-103299CAS No.: 18228-17-6Synonyms: Naphthol AS-E phosphate分式: CHClNOP分量: 377.72作靶点: Epigenetic Reader Domain作通路: 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

2、: 6 mg/mL (15.88 mM; Need ultrasonic and warming)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2 mg/mL (5.29 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2 mg/mL (5.29 mM); Suspended solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DM

3、SO 90% corn oilSolubility: 2 mg/mL (5.29 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 KG-501是CREB 的抑制剂，其 IC50 值为 6.89 M。IC50 & Target IC50: 6.89 M (CREB) 1.体外研究 KG-501, which directly targets the KIX domain of CBP, results in a disrupted CREB-CBP complex, inhibitsCREB-target gene induction, and inhibit

4、s IL-1-mediated angiogenic activity in NSCLC 1. KG-501 disruptsphospho (Ser-133) CREB binding to KIX with a Ki of 90 M, using concentrations of CREB that are withinthe linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction ofendogenous CREB target genes (NR4A

5、2, CG, c-fos, and RGS2) by forskolin, indicating that KG-501 likelyexerts a general effect on CREB activity 2. KG-501 can also inhibit NF-B transcription activity because NF-B also uses CBP as a cofactor to regulate gene expression. The migration of HUVECs induced by CM fromA549 cells treated with I

6、L-1 plus 10 M of KG-501 is significantly lower than that induced by CM from A549cells treated with IL-1 alone. At 10 M, KG-501 suppresses the expression of all of the IL-1induced CXCchemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1inducedCXCL5 protein secretio

7、n. Similar effects of KG-501 are also observed in the H1734 cell line 3.REFERENCES1. Lee JW, et al. A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell CycleRegulation, Autophagy Suppression and Endoplasmic Reticulum Stress. PLoS One. 2015 Apr 21

8、;10(4):e0122628.2. Best JL et al. Identification of small-molecule antagonists that inhibit an activator: coactivator interaction. Proc Natl Acad Sci U S A. 2004Dec 21;101(51):17622-73. Sun H, et al. Cyclic AMP-responsive element binding protein- and nuclear factor-kappaB-regulated CXC chemokine gene expression inlung carcinogenesis. Cancer Prev Res (Phila). 2008 Oct;1(5):316-28.McePdfHeightCaution: Product has not been fully validated for medical applicat