產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 25mg 50mg 100mg 250mg
CAS	152121-47-6
別名	N/A
化學(xué)名	4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine
分子式	C21H16FN3OS
分子量	377.44
溶解度	≥ 18.872mg/mL in DMSO, ≥ 3.28 mg/mL in EtOH with ultrasonic
儲存條件	Desiccate at 4°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

SB203580, also called 4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl) 1Himidazole [6], is a specific pyridinyl imidazole inhibitor of p38-MAPK (Mitogen-activated Protein Kinase) signaling pathway [1] [3]. It was competitive with ATP with a selectivity probably determined by nonconserved regions within or near the ATP binding pocket and a Ki of 21 nM [3]. It inhibits c-Raf with an IC50 of 2 mM in vitro [4].

p38 MAPK signaling pathway enables cells to generate a plethora of different effects to interpret a wide range of external signals and respond appropriately. There is a core of three protein kinases acting sequentially in this pathway to ensure the diversity and specificity in cellular outcomes [5].

Exposure to 30 mM SB203580 significantly decreased the resistance of L1210/VCR cells to vincristine accompanied by the LC50 value of vincristine changed from 3.2036±0.521 to 0.5576±0.082 mM. Exposure to 10 mM SB203580 slightly changed the value of the resistance index, accompanied by the LC50 values of SB203580 to sensitive L1210 cells and to resistant cells were 39.26±2.2 mM and 52.06±7.6 mM, respectively [1].

In vivo, administration of SB203580 alone 24 h before the permanent middle cerebral arterial occlusion abolished the isoflurane preconditioning-induced neuroprotection. After isoflurane exposure, administration of SB203580 decreased phosphorylated p38 MAPK. SB203580 inhibited anisomycin pretreatment-induced neuroprotection [6].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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