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Merck

506121

p38 MAP Kinase Inhibitor III

The p38 MAP Kinase Inhibitor III, also referenced under CAS 581098-48-8, controls the biological activity of p38 MAP Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

p38 MAP Kinase Inhibitor III, ML3403, (RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-(1-phenylethyl)amine]

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About This Item

Empirical Formula (Hill Notation):
C23H21FN4S
CAS Number:
581098-48-8
Molecular Weight:
404.50
MDL number:
MFCD24369000
UNSPSC Code:
12352200
NACRES:
NA.54

Key Documents

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Product Name

p38 MAP Kinase Inhibitor III, The p38 MAP Kinase Inhibitor III, also referenced under CAS 581098-48-8, controls the biological activity of p38 MAP Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

Fc1ccc(cc1)c2[nH]c(nc2c3cc(ncc3)NC(C)c4ccccc4)SC

InChI

1S/C23H21FN4S/c1-15(16-6-4-3-5-7-16)26-20-14-18(12-13-25-20)22-21(27-23(28-22)29-2)17-8-10-19(24)11-9-17/h3-15H,1-2H3,(H,25,26)(H,27,28)

InChI key

VXPWQNBKEIVYIS-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
p38 MAP kinase
Product competes with ATP.
Reversible: yes
Target IC50: 0.38 µM for p38 MAP kinase α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

General description

A cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC50 = 0.38 µM for p38α). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC50 = 0.16 and 0.039 µM for TNF-α and IL-1β release, respectively, in human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mouse). When compared with SB 203580 (Cat. No. 559389 and 559398), it exhibits reduced inhibitory activity against cytochrome P450-2D6 isoform and, therefore, is better suited for in vivo use. A 10 mM (1 mg/247 µl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.
A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 380 nM for p38α). Shown to effectively suppress LPS-induced cytokine release in vitro (IC50 = 160 nM for TNF-α release and 39 nM for IL-1β release, human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mice). Exhibits reduced inhibitory activity against cytochrome P450-2D6 compared to SB 203580 (Cat. No 559389) and is better suited for use in animal models.

Other Notes

Laufer, S.A., et al. 2003. J. Med. Chem.46, 3230.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Dai-Xu Li et al.
General physiology and biophysics, 39(6), 545-555 (2020-11-24)
Cardiovascular disease (CVD) states are associated with endothelial dysfunction (ED) and increased production of ROS in endothelial cells. The present study aimed to explore the protective effects of antioxidant protein peroxiredoxin 6 (PRDX6) on angiotensin II (AngII)‑induced human umbilical vein

Global Trade Item Number

SKUGTIN
506121-1MGCN04055977199468

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