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> SB 202190 [152121-30-7]

SB 202190 [152121-30-7]

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SB 202190 est un inhibiteur séléctive de p38 MAP kinase avec des IC50s de 50 nM et 100 nM pour p38α et p38β2, respectivement. SB 202190 se lie à la poche ATP de la kinase p38 humaine recombinante active avec un Kd de 38 nM. SB 202190 a une activité anticancéreuse et a sauvé les déficits de mémoire.

SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits. SB202190 induces autophagy.

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SB 202190 Estructura química

SB 202190 Estructura química

No. CAS : 152121-30-7

This product is a controlled substance and not for sale in your territory.

Based on 98 publication(s) in Google Scholar

Other Forms of SB 202190:

  • SB 202190 hydrochloride Obtener un presupuesto

    SB 202190 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Mar;120(3):3898-3910.  [Abstract]

    Cells pretreated with SP600125 show a decreased proapoptotic Bax expression and increase antiapoptotic Bcl-2 formation when JNK pathway is blocked. Inhibition of p38 by SB202190 significantly enhanced Bcl-2 expression. Pretreatment with BAY 11-7082 to inhibit NF‐κB markedly enhance Baxm and decrease Bcl-2 expression compared with the ACR-treated group.

    SB 202190 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2019 Apr 1;51(4):365-374.  [Abstract]

    MAPKs inhibitors suppress LPS-induced COX-2 expression and AKT1 phosphorylation. RAW264.7 cells are pretreated for 1 h with U0126, SB202190, SP600125 alone, or all the three inhibitors, respectively, and then exposed to 40 ng/ml LPS for 30 min or 12 h. The phosphorylated protein kinases and COX-2 expression are detected by western blot analysis using their corresponding antibodies.

    SB 202190 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    SB 202190 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    SB 202190 purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2017 Jan;39(1):71-80.  [Abstract]

    Inhibition of p38 expression enhances the promoting effect of miR-214 on the adipocyte differentiation of bone marrow-derived mesenchymal stem cells (BMSCs) following the overexpression of miR-214. p-p38 protein expression decreases following treatment with p38 inhibitor, as shown by (A) western blot analysis, and (B) statistical analysis of p-p38 protein expression.

    SB 202190 purchased from MedChemExpress. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    SB 202190 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458.  [Abstract]

    Representative immunoblot analysis of p53, p16, p21, and retinoblastoma protein (Rb) in NP cells.

    SB 202190 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2015 Nov 19;2(12):1944-56.  [Abstract]

    SW620 xenograft tumors are treated with SB202190 and OSI027 individually or in combination. The effect on signaling by p38 (P-MK2 and P-Hsp27) and mTOR (P-S6K1 and P-AKT) is analyzed by immunoblot. SB202190 achieves on-target inhibition by diminishes phosphorylation of MK2 and Hsp27. OSI-027 blocks signaling by both mTORC1 and mTORC2 by decreases phosphorylation of S6K1 and AKT. When SB202190 and OSI-027 are used in combination, all three kinases, p38, mTORC1 and mTORC2 are potently inhibited.

    Ver todos los productos específicos de isoformas p38 MAPK:

    Ver todas las isoformas
    p38 MAPK p38α p38β MAPK13 p38δ p38γ
    Descripciòn

    SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1][2]. SB202190 induces autophagy[3].

    IC50 & Target[1]

    p38α

    50 nM (IC50)

    p38β2

    100 nM (IC50)

    In Vitro

    SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner[1].
    SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480)[2].
    In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling[2].

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

    SB 202190 Related Antibodies
    In Vivo

    SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth[2].

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

    Animal Model: 4-week-old female BALB/c nude mice (bearing SW480 and RKO xenograft tumors)[2]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection; daily for 10-12 days
    Result: Inhibition of tumor cell survival and tumor growth.
    Peso molecular

    331.34

    Fòrmula

    C20H14FN3O
    No. CAS

    152121-30-7
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    FC1=CC=C(C2=C(C3=CC=NC=C3)NC(C4=CC=C(O)C=C4)=N2)C=C1
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (301.80 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 3.0180 mL 15.0902 mL 30.1805 mL
    5 mM 0.6036 mL 3.0180 mL 6.0361 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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: ≥ 2.08 mg/mL (6.28 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.28 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    Pureza y Documentación

    Purity: 99.89%

    COA (251 KB) HNMR (195 KB) LCMS (120 KB) Elemental Analysis Report (110 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    • [1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.  [Content Brief]

      [2]. Nemoto S, et al. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20.  [Content Brief]

      [3]. Grossi V, et al. Bay 43-9006 inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81.  [Content Brief]

      [4]. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798.  [Content Brief]

      [5]. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56.  [Content Brief]

    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 3.0180 mL 15.0902 mL 30.1805 mL 75.4512 mL
    5 mM 0.6036 mL 3.0180 mL 6.0361 mL 15.0902 mL
    10 mM 0.3018 mL 1.5090 mL 3.0180 mL 7.5451 mL
    15 mM 0.2012 mL 1.0060 mL 2.0120 mL 5.0301 mL
    20 mM 0.1509 mL 0.7545 mL 1.5090 mL 3.7726 mL
    25 mM 0.1207 mL 0.6036 mL 1.2072 mL 3.0180 mL
    30 mM 0.1006 mL 0.5030 mL 1.0060 mL 2.5150 mL
    40 mM 0.0755 mL 0.3773 mL 0.7545 mL 1.8863 mL
    50 mM 0.0604 mL 0.3018 mL 0.6036 mL 1.5090 mL
    60 mM 0.0503 mL 0.2515 mL 0.5030 mL 1.2575 mL
    80 mM 0.0377 mL 0.1886 mL 0.3773 mL 0.9431 mL
    100 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.7545 mL
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    SB 202190 Related Classifications

    Help & FAQs

    Keywords:

    SB 202190152121-30-7SB202190SB-202190Organoidp38 MAPKAutophagyApoptosisATPpocketanti-cancerspatiallearningmemorydeficitscolorectalInhibitorinhibitorinhibit

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