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BI-D1870

CAS No. : 501437-28-1

產品活性：BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.

研究領域：MAPK/ERK Pathway  |  Autophagy

作用靶點：Ribosomal S6 Kinase (RSK)  |  Autophagy

In Vitro: BI-D1870 inhibits a mutant of RSK2 lacking the C-terminal kinase catalytic domain (RSK2^1-389:S381E) with an IC₅₀ of approx. 30 nM. BI-D1870 inhibits RSK1 and RSK2 with IC₅₀ values of 10 nM and 20 nM respectively, when the kinase assays are performed with 100 μM ATP. When the assays are performed at a 10-fold lower ATP concentration, the IC₅₀ of BI-D1870 is reduced to 5 nM for RSK1 and 10 nM for RSK2.
BI-D1870 inhibits PLK1 with an IC₅₀ of 100 nM, whilst the IC₅₀ values for Aurora B, DYRK1a, CDK2-A, Lck, CK1 and GSK3β are 10- to 100-fold higher than that of the RSK isoforms. BI-D1870 (10 μM) inhibits the PMA-induced phosphorylation of GSK3α and GSK3β in HEK-293 cells. In HEK-293 cells, BI-D1870 inhibits the EGF-induced phosphorylation of LKB1 at Ser431 with an IC₅₀ of approx. 1 μM.
BI-D1870 does not affect the activation of ERK1/ERK2 and MSK1, nor does it inhibit the phosphorylation of CREB.
BI-D1870 is a potent RSK family kinase inhibitor (K_ds: 10-100 nM), and also interact with BRD4(1) and PLK family, with K_ds of 3.5 μM and appr 10 nM.
BI-D1870 (10 μM) strongly induces p70S6K activation in serum-starved LN-229 cells, and alao stimulates the phosphorylation of rpS6 and p70S6K in LN-18 cells. BI-D1870 (1 μM) potently inhibits rpS6 phosphorylation, and inhibits PMA-induced rpS6 phosphorylation at concentrations higher than 1 μM.
BI-D1870 (1-5 μM) induces a dose- and time-dependent inhibition of cell proliferation in all cell types. BI-D1870 (1-3 μM) induces apoptosis in SCC4 cells and HSC-3 cells. BI-D1870 (0-5) modulates cell survival signaling pathways including Akt and p38 MAPK dose-dependently.

In Vivo: BI-D1870 (0.5 mg/kg)-injected experimental autoimmune encephalomyelitis (EAE) mice exhibits a delayed neural deficit without obvious weight loss. Histopathological analyses shows inflammatory cell infiltration and demyelination in the spinal cord in control mice, but not in BI-D1870-treated mice. BI-D1870 protects against the infiltration of TH1 or TH17 cells into the CNS.

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