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[CAS NO. 869185-85-3] Adezmapimod hydrochloride

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Catalog:	HY-10256A
Brand:	MCE
CAS:	869185-85-3

Overview

MDL	-
Molecular Weight	413.90
Molecular Formula	C21H17ClFN3OS
SMILES	O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C.[H]Cl

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

340 Publications Citing Use of MCE

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Summary

Adezmapimod (SB 203580) hydrochloride 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 hydrochloride inhibits LCK, GSK3β and PKBα with IC ₅₀ s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator ^[1] .

IC50 & Target

p38

50 nM (IC ₅₀ )

p38β2

500 nM (IC ₅₀ )

In Vitro

Adezmapimod hydrochloride (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] .
Adezmapimod hydrochloride blocks PKB phosphorylation (IC ₅₀ 3-5 μM). Adezmapimod hydrochloride 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 hydrochloride (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

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 241.60 mM ; Need ultrasonic)

H ₂ O : 8.43 mg/mL ( 20.37 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4160 mL	12.0802 mL	24.1604 mL
5 mM	0.4832 mL	2.4160 mL	4.8321 mL
10 mM	0.2416 mL	1.2080 mL	2.4160 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 (6.04 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

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

References

[1] Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
[2] Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitoge
[3] Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18.

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