Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes. Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine kinase activated by environmental stresses and inflammatory cytokines. CAY10571 is an analog of SB203580. It inhibits IL-1 production in the human monocytic cell line THP with an IC value of 0.20 µM and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity with an IC value of 0.03 µM. CAY105571 also inhibits 5-lipoxygenase production in RBL-1 cells with an IC value of 24 µM.
CAY10571 (SB 203580 sulfone) is an analog of p38 MAP kinase inhibitor SB 203580. CAY10571 (SB 203580 sulfone) inhibits the IL-1 production (IC50 of 0.2 μM in monocytes) and binds competitively with CSAID binding proteins (CSBP), inhibits it mediated stress response signaling with an IC50 of 0.03 μM. CAY10571 (SB 203580 sulfone) inhibits 5-LO with an IC50 value of 24 µM. SB 203580 sulfone can be used in the research of inflammatory diseases.
IC50&Target
IL-1
0.2 μM (IC50)
体外研究
CAY10571 (SB 203580 sulfone) inhibits the production of IL-1 in monocytes with an IC50 of 0.2 μM.
CAY10571 (SB 203580 sulfone) inhibits 5-LO with an IC50 value of 24 µM (this assay uses semi purified enzyme from RBL-1 cells).
分子式
C21H16FN3O2S
分子量
393.43
CAS号
152121-46-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 100 mg/mL (254.17 mM; ultrasonic and warming and heat to 60°C)
DMF : 50 mg/mL (127.09 mM; Need ultrasonic and warming)