1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  3. SB 242235

SB 242235 

Cat. No.: HY-18306 Purity: 98.63%
Handling Instructions

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes.

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

SB 242235 Chemical Structure

SB 242235 Chemical Structure

CAS No. : 193746-75-7

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10 mM * 1 mL in DMSO USD 198 In-stock
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10 mg USD 288 In-stock
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50 mg USD 900 In-stock
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100 mg USD 1440 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes[1].

IC50 & Target

IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)[1]

In Vitro

SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β[1].
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate[1].

Western Blot Analysis[1]

Cell Line: Human chondrocytes
Concentration: 0 μM,0.01 μM,0.1 μM,1 μM,10 μM
Incubation Time: 15 minutes
Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 μM.
In Vivo

SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[2].
SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey[3].

Animal Model: Female SKH-1 hairless mice (4–6 weeks)[2]
Dosage: 100 mg/kg
Administration: Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation
Result: Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.
Molecular Weight

353.39

Formula

C₁₉H₂₀FN₅O

CAS No.

193746-75-7

SMILES

COC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCNCC4)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 48 mg/mL (135.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8297 mL 14.1487 mL 28.2973 mL
5 mM 0.5659 mL 2.8297 mL 5.6595 mL
10 mM 0.2830 mL 1.4149 mL 2.8297 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

SB 242235SB242235SB-242235p38 MAPKAutophagyInhibitorinhibitorinhibit

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SB 242235
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