BI-D1870 |
| カタログ番号GC13468 |
BI-D1870 は、RSK アイソフォームの ATP 競合性、細胞透過性、脳透過性の阻害剤であり、RSK1/RSK2/RSK3/RSK4 の IC50 はそれぞれ 31 nM/24 nM/18 nM/15 nM です。
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Cas No.: 501437-28-1
Sample solution is provided at 25 µL, 10mM.
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BI-D1870 is a cell-permeable inhibitor of the p90 RSK isoforms with IC50 values of 31nM, 24nM, 18nM and 15nM for RSK1, RSK2, RSK3 and RSK4 respectively [1].
BI-D1870 is a derivative of dihydropteridinone and found to be a remarkably specific inhibitor of RSK isoforms. It is an ATP-competitive inhibitor. When the concentrations of ATP are 10μM and 100μM, the IC50 values of BI-D1870 against RSK1 and RSK2 are 5nM, 10nM and 10nM, 20nM, respectively. BI-D1870 also inhibits RSK3 and RSK4 with IC50 values of 18nM and 15nM respectively, when ATP is 100μM. The inhibition activity of BI-D1870 against RSK is more than 500-fold greater than some other AGC kinases suggesting BI-D1870 as a specific inhibitor of RSK. In addition, BI-D1870 is reported to induce the phosphorylation of ERK1/ERK2 and the subsequent phosphorylation of CREB in Rat-2 cells [1].
References:
[1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38.
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