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SB 242235 MAPK inhibitor

Catalog No.B1161
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1g Please Inquire Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

SB 242235

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Chemical Properties

Cas No. 193746-75-7 SDF Download SDF
Chemical Name 4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine
Canonical SMILES COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F
Formula C19H20FN5O M.Wt 353.39
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

SB 242235 is a selective inhibitor of p38 mitogen activated protein kinase (MAPK) with IC50 values of 0.019μM and 1μM for p38α MAPK and p38β MAPK, respectively [1].

SB 242235 is developed for the treatment of cytokine-mediated diseases such as rheumatoid arthritis (RA). It belongs to the pyridinyl imidazole class and shows potent anti-inflammatory activity without affecting 5-lipoxygenase or cyclooxygenase-1. SB 242235 is found to be a selective p38MAPK inhibitor. It has no significant inhibitory activity against ERK and JNK. In normal rats, administration of SB 242235 significantly inhibits the production of TNFα induced by LPS. When treated with AIA rats, SB 242235 inhibits paw edema with ED50 value of about 30 mg/kg. It also remarkably suppresses the joint damage of the rats. Moreover, SB 242235 exerts a significant inhibition of the cytokine IL-6 at dose of 60 mg/kg [2].

References:
[1] Ward K W, Proksch J W, Salyers K L, et al. SB-242235, a selective inhibitor of p38 mitogenactivated protein kinase. I: Preclinical pharmacokinetics. xenobiotica, 2002, 32(3): 221-233.
[2] Badger A M, Griswold D E, Kapadia R, et al. Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis. Arthritis & Rheumatism, 2000, 43(1): 175-183.