SB-242235

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

选择性 p38 MAPK 抑制剂；抑制人原代软骨细胞中 p38 MAPK 的 IL-1 beta 诱导，IC50 为 1 uM。

A selective p38 MAPK inhibitor; inhibits IL-1 beta induction of p38 MAPK in primary human chondrocytes with IC50 of 1 uM; inhibits LPS-stimulated serum levels of TNFalpha in normal rats with mean ED50 of 3.99 mg/kg.Rheumatoid Arthritis Discontinued(In Vitro):SB 242235 (0-10　μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β.SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.(In Vivo):SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation.SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2.SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey.

SB 242235 (0-10　μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β.SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. Western Blot AnalysisCell Line:Human chondrocytes Concentration:0 μM,0.01 μM,0.1 μM,1 μM,10μM Incubation Time:15 minutes Result:Dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 μM.

SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation.SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2.SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey. Animal Model:Female SKH-1 hairless mice (4–6 weeks)Dosage:100 mg/kg Administration:Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation Result:Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.

SB 242235 | SB242235

MAPK/ERK Signaling

p38 MAPK

p38MAPK

Inflammation/Immunology

Rheumatoid Arthritis

193746-75-7

353.3934

C19H20FN5O

>98% (HPLC)

DMSO: ≥ 48 mg/mL

O=C(C1=CC=CN=C1)NC2=NC3=C(C=CC(OC)=C3OC)C4=NCCN24

Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-

(-20℃)

With Ice Pack

≥ 2 years