BI-D1870 |
| Katalog-Nr.GC13468 |
BI-D1870 ist ein ATP-kompetitiver, zellgÄngiger und ins Gehirn eindringender Inhibitor von RSK-Isoformen mit IC50-Werten von 31 nM/24 nM/18 nM/15 nM fÜr RSK1/RSK2/RSK3/RSK4.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| Cell experiment [1]: | |
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Cell lines |
HEK-293 cells |
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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 |
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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]: | |
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Animal models |
experimental autoimmune encephalomyelitis (EAE) mice |
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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. |
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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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| Cas No. | 501437-28-1 | 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 |
| Löslichkeit | ≥ 19.55mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5548 mL | 12.774 mL | 25.548 mL |
| 5 mM | 0.511 mL | 2.5548 mL | 5.1096 mL |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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