2. MAPK/ERK Pathway Autophagy
  3. Ribosomal S6 Kinase (RSK) Autophagy
  4. BI-D1870

BI-D1870 est un inhibiteur des isoformes RSK qui est perméable aux cellules et ATP-compétitif, avec des IC50s de 31 nM/24 nM/18 nM/15 nM pour RSK1/RSK2/RSK3/RSK4, respectivement.

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.

For research use only. We do not sell to patients.

BI-D1870 Chemical Structure

BI-D1870 Chemical Structure

CAS No. : 501437-28-1

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Customer Review

Based on 15 publication(s) in Google Scholar

BI-D1870 Related Antibodies

Top Publications Citing Use of Products

    BI-D1870 purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191.  [Abstract]

    H2.35 cells are serum starved for 72 h and then were pre-treated with either DMSO or BI-D1870 (p90 IN, 10 µM). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or p90 IN (10 µM). At 18 hpi, cell lysates are collected for western blot analysis.

    BI-D1870 purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191.  [Abstract]

    H2.35 cells are serum starved for 72 h and then are pre-treated with either DMSO or 10 µM PD0325901 (ERK IN). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or 10 µM ERK IN. At 18 hpi, cell lysates are collected for western blot analysis.

    BI-D1870 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Mar 1;7(9):10283-96.  [Abstract]

    HeLa cells synchronized at mitotic phase are treated with BI-D1870 at indicated concentrations. Phosphorylation of EBP50 is assayed by Western blotting using p-EBP50 (T156) antibody. Phosphorylation of RSK1 at S380 and ribosomal protein S6 (rpS6) at S235-236 are assayed to examine activation of RSK1 at mitotic phase. GAPDH or α-tubulin is examined as a loading control. The morphology of cells at the moment of harvest for the above experiment is shown in photographs.

    View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

    View All Isoforms
    p70S6K RSK1 RSK2 RSK3 RSK4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3][4][5].

    IC50 & Target

    RSK1

     

    RSK2

     

    RSK3

     

    RSK4

     

    In Vitro

    BI-D1870 inhibits a mutant of RSK2 lacking the C-terminal kinase catalytic domain (RSK21-389: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[1].
    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[1].
    BI-D1870 does not affect the activation of ERK1/ERK2 and MSK1, nor does it inhibit the phosphorylation of CREB[1].
    BI-D1870 is a potent RSK family kinase inhibitor (Kds: 10-100 nM), and also interact with BRD4(1) and PLK family, with Kds of 3.5 μM and appr 10 nM[2].
    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[4].
    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[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    BI-D1870 Related Antibodies
    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[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    391.42

    Formula

    C19H23F2N5O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (12.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5548 mL 12.7740 mL 25.5480 mL
    5 mM 0.5110 mL 2.5548 mL 5.1096 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.72%

    COA (248 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Purified His6-RSK1, His6-RSK2 or GST-RSK21-389:S381E (1-2 units/mL) are assayed for 10 min at 30°C in a 50 μL assay mixture in Buffer A containing 30 μM substrate peptide (KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), 10 mM magnesium acetate and 100 μM of [γ-32P]ATP. Reactions are terminated and analysed. The amount of enzyme that catalysed the phosphorylation of 1 nmol of substrate peptide in 1 min is termed one unit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [5]

    Measurement of cell growth is assessed using the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide] assay in six replicates. The cells (5×103/200 μL) are seeded in 96-well, flat-bottom plates for 24 h and then exposed to various concentrations of test agents for the indicated time intervals. After removing the culture medium, 200 μL of the medium containing MTT at a concentration of 0.5 mg/mL is added, and the cells are incubated at 37°C for 2 h. The medium is removed, and the reduced MTT dye in each well is dissolved in 200 μL DMSO. Absorbance is determined with a multimode microplate reader Synergy HT at 570 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Myelin oligodendrocyte glycoprotein (MOG) peptide 35-55 MEVGWYRSPFSRVVHLYRNGK) (BEX) is used to induce EAE in C57/BL6J mice. Mice are injecteds.c. with 200 g of MOG peptide in 100 μL of PBS emulsified in 100 μL complete Freund’s adjuvant (CFA) that is further supplemented with five mg/mL Mycobacterium tuberculosis. In addition, 500 ng pertussis toxin is injected i.p. on days zero and two. The RSK inhibitor (BI-D1870; 0.5 mg/kg) is injected i.p. into mice two days after immunization with MOG peptide, and injection is repeated every other day for 11 days. Mice that receive only dimethyl sulfoxide (DMSO) solution are used as controls. Paralysis is evaluated according to the following scale: zero, no disease; one, tail limpness; two, hind limb weakness; three, hind limb paralysis; four, fore limb weakness; five, quadriplegia; six, death. For histological analysis, CNS samples are fixed with 4% paraformaldehyde and sliced at 4 μm, and then hematoxylin & eosin (H & E) staining is performed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5548 mL 12.7740 mL 25.5480 mL 63.8700 mL
    5 mM 0.5110 mL 2.5548 mL 5.1096 mL 12.7740 mL
    10 mM 0.2555 mL 1.2774 mL 2.5548 mL 6.3870 mL
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    BI-D1870 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    BI-D1870501437-28-1Ribosomal S6 Kinase (RSK)AutophagyS6KInhibitorinhibitorinhibit

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