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Catalog: | HY-10256 |
Brand: | MCE |
CAS: | 152121-47-6 |
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 |
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] .
p38 50 nM (IC 50 ) |
p38β2 500 nM (IC 50 ) |
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. |
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). |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 20 mg/mL ( 52.99 mM ; ultrasonic and warming and heat to 60°C)
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 |
Add each solvent one by one: 0.5% CMC-Na /saline water
Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic
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
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic
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