[CAS NO. 152121-47-6] Adezmapimod

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PRODUCTS SPECIFICATIONS [152121-47-6]

Catalog

HY-10256

Brand

MCE

CAS

152121-47-6

DESCRIPTION [152121-47-6]

Overview

MDL	MFCD00922198
Molecular Weight	377.43
Molecular Formula	C21H16FN3OS
SMILES	O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C

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

340 Publications Citing Use of MCE

Summary

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC ₅₀ s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 , respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC ₅₀ s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator ^[1] .

IC50 & Target

p38

50 nM (IC ₅₀ )

p38β2

500 nM (IC ₅₀ )

In Vitro

Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC ₅₀ of 3-5 μM ^[1] .
SB203580 blocks PKB phosphorylation (IC ₅₀ 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells ^[1] .

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

Cell Proliferation Assay ^[1]

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC ₅₀ of 3-5 μM.

Western Blot Analysis ^[1]

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

In Vivo

Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel ^[1] .

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

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors ^[1]
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

Appearance

Solid

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 : 20 mg/mL ( 52.99 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 0.5% CMC-Na /saline water

Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution
3.

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

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic
4.

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

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic
5.

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

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

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