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BI-D1870 P90 RSK inhibitor,ATP-competitive and cell-permeable

Catalog No.B2227
Size Price Stock Qty
10mM (in 1mL DMSO)
$160.00
In stock
5mg
$120.00
In stock
10mg
$190.00
In stock
50mg
$470.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BI-D1870

Biological Activity

Description BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 values of 31 nM/24 nM/18 nM/15 nM, respectively.
Targets RSK4 RSK3 RSK2 RSK1    
IC50 15 nM 18 nM 24 nM 31 nM    

Protocol

Cell experiment [1]:

Cell lines

HEK-293 cells

Preparation method

The solubility of this compound in DMSO is >19.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-10 μM; 15, 30, 60, 120 and 240 min

Applications

In HEK-293 cells, BI-D1870 greatly inhibited the PMA-induced phosphorylation of GSK3α and GSK3β. BI-D1870 also inhibited PMA-induced phosphorylation of GSK3 isoforms and another RSK substrate, the protein kinase LKB1 with an IC50 of approx. 1 μM.

Animal experiment [2]:

Animal models

experimental autoimmune encephalomyelitis (EAE) mice

Dosage form

0.5 mg/kg; intraperitoneal injection; every other day for 11 days

Application

In EAE mice immunized with MOG peptide, BI-D1870 protected mice from EAE by reducing the infiltration of TH1 and TH17 cells into the CNS and decreasing mRNA levels of Ccr6 in TH17 cells.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

[2]. Takada I1, Yogiashi Y2, Makishima M3. et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221(2):188-92.

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Chemical Properties

Cas No. 501437-28-1 SDF Download SDF
Chemical Name 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
Canonical SMILES CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
Formula C19H23F2N5O2 M.Wt 391.42
Solubility >19.6mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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.