BI605906 _IKK 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBI605906Cat. No.: HY-13019CAS No.: 960293-88-3分式: CHFNOS分量: 432.51作靶點: IKK作通路: NF-B儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 29 mg/mL (67.05 mM)* means soluble, but saturation unknown

2、.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3121 mL 11.5604 mL 23.1209 mL5 mM 0.4624 mL 2.3121 mL 4.6242 mL10 mM 0.2312 mL 1.1560 mL 2.3121 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BI605906種新型 IKK 抑制劑，在 0.1 mM ATP 條件下測定時 IC50 值為 380 nM。IC50 & Target IKK380 nM (I

3、C50, at 0.1 mM ATP)體外研究BI605906 is an inhibitor of IKK with improved selectivity. BI605906 inhibits IKK in vitro with an IC50 value1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEof 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that is inhibited of over 100 tested,which include I

4、KK, IKK and TBK1, is the insulin-like growth factor 1 (IGF1) receptor (IC50=7.6 M).BI605906 partially inhibits the IL-1-stimulated activation of IKK/TBK1 1. In primary mouse hepatocytes,Metformin treatment for 3 hours suppresses TNF-induced degradation of the NF-B negative regulator IB,while modulat

5、ing AMPK and MTOR signaling in a dose-dependent manner. The magnitude of the effect on IB is comparable with BI605906. Unlike Metformin, BI605906 (10 M ) does not suppress signalingdownstream of mTOR nor does it activate AMPK. TNF-dependent expression of CINC-1/CXCL1, CXCL2,IL-1, and IL-6 is strongl

6、y inhibited by both Metformin and BI605906 (10 M) 2.PROTOCOLCell Assay 2 Primary hepatocytes are incubated in serum-free medium overnight and then stimulated for 3 h with orwithout 2 mM Metformin and TNF-. In addition, cells are incubated with/without 10 M BI605906 or 100 nMRapamycin, before lysis a

7、nd immunoblotting 2.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 Mol Cell. 2017 Jun 1;66(5):698-710.e5. Sci Rep. 2019 Jan 17;9(1):193. Cell Biochem Funct. 2019 Jan;37(1):4-10.See more customer validations on HYPERLINK / www.MedChemEREFERE

8、NCES1. Clark K, et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104.2. Cameron AR, et al. Anti-Inflammatory Effects of Metformin Irrespective of Diabetes Status. Circ Res. 2016 Aug 19;119(5):652-65.McePdfHeightCaution: Product has not been fully validated for medical applications.F