[CAS NO. 152121-47-6] Adezmapimod (SB203580)

Name: Adezmapimod (SB203580)
Brand: Arctom Scientific
SKU: SLK-S1076

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PRODUCTS SPECIFICATIONS [152121-47-6]

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Catalog

SLK-S1076

Brand

Selleck

CAS

152121-47-6

DESCRIPTION [152121-47-6]

Overview

MDL	MFCD00922198
Molecular Weight	377.43
Molecular Formula	C21H16FN3OS
SMILES	FC1=CC=C(C2=C(N=C(N2)C3=CC=C(S(C)=O)C=C3)C=4C=CN=CC4)C=C1

For research use only.

Storage

3 years -20°C(in the dark) powder
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

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Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

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Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6495 mL	13.2475 mL	26.4950 mL
5 mM	0.5299 mL	2.6495 mL	5.2990 mL
10 mM	0.2649 mL	1.3247 mL	2.6495 mL
50 mM	0.0530 mL	0.2649 mL	0.5299 mL

Description

Adezmapimod (SB203580, RWJ 64809, PB 203580) is a inhibitor with of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with of 3-5 μM. SB203580 induces and .

Features

First reported p38 inhibitor.

Targets

p38 MAPK ^[1] (THP-1 cells)	PKB ^[1] (THP-1 cells)
0.3 μM-0.5 μM	3 μM-5 μM

In vitro

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.

In vivo

SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).

References

[1] Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.
[2] Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.
[3] Zhang H, et al. Apoptosis, 2011
[4] Barancik M, et al. J Cardiovasc Pharmacol, 2000, 35(3), 474-83.
[5] Jin N, et al. Int Immunopharmacol, 2011, 11(9):1319-26.

Synonyms

Pyridine, 4-[4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]-

Pyridine, 4-[5-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-4-yl]-

4-[4-(4-Fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]pyridine

SB 203580

PB 203580

RWJ 64809

BIRB 203580

4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine