Art. -Nr.: HY-18306

SB 242235

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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

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Reinheit: 99.67%
CAS. Nr.: 193746-75-7
Formel: C₁₉H₂₀FN₅O
Molecular Weight:353.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SB 242235 Chemical Structure

CAS. Nr.: 193746-75-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	170 nM Compound: SB-242235	Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA	[PMID: 18602262]

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].

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

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].

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

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.

Chemical Information

CAS. Nr. 193746-75-7
Appearance Solid
Molecular Weight 353.39
Formel C₁₉H₂₀FN₅O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Cell Death Dis

LIF is essential for ISC function and protects against radiation-induced gastrointestinal syndrome. [Abstract]

2020 Jul 27;11(7):588. PMID: 32719388
J Neuroinflammation

CD36 deletion prevents white matter injury by modulating microglia polarization through the Traf5-MAPK signal pathway. [Abstract]

2024 Jun 5;21(1):148. PMID: 38840180

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 48 mg/mL (135.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (7.07 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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. [Content Brief]

[2]. Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. [Content Brief]

[3]. Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.8297 mL	14.1487 mL	28.2973 mL	70.7434 mL
	5 mM	0.5659 mL	2.8297 mL	5.6595 mL	14.1487 mL
	10 mM	0.2830 mL	1.4149 mL	2.8297 mL	7.0743 mL
	15 mM	0.1886 mL	0.9432 mL	1.8865 mL	4.7162 mL
	20 mM	0.1415 mL	0.7074 mL	1.4149 mL	3.5372 mL
	25 mM	0.1132 mL	0.5659 mL	1.1319 mL	2.8297 mL
	30 mM	0.0943 mL	0.4716 mL	0.9432 mL	2.3581 mL
	40 mM	0.0707 mL	0.3537 mL	0.7074 mL	1.7686 mL
	50 mM	0.0566 mL	0.2830 mL	0.5659 mL	1.4149 mL
	60 mM	0.0472 mL	0.2358 mL	0.4716 mL	1.1791 mL
	80 mM	0.0354 mL	0.1769 mL	0.3537 mL	0.8843 mL
	100 mM	0.0283 mL	0.1415 mL	0.2830 mL	0.7074 mL

Keywords

SB 242235

2 Cited Publications

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SB 242235

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Publications Citing Use of MedChemExpress (MCE) SB 242235

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB 242235 Related Classifications

HY-18306 Related Classifications