Potent and specific inhibitor of human p38 (SAPK2a; IC50=60nM). Exhibits over 2000-fold greater selectivity for p38 over ERK (MAPK), 500-fold over cAMP-dependent protein kinase (PKA), 50-fold over protein kinase C (PKC), and >1000-fold over EGFR. Acts as a potent inhibitor of angiogenesis and as an inhibitor of TNF-α production.
Product Details
| Alternative Name: | 5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinyl)imidazole |
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| Formula: | C18H19FN6 |
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| MW: | 338.4 |
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| CAS: | 165806-53-1 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | White to pale amber solid. |
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| Solubility: | Soluble in DMSO (100mg/ml). |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. Packaged under inert gas. Hygroscopic. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Nrf2 is essential for the expression of lipocalin-prostaglandin D synthase induced by prostaglandin D2: K.H. Kim, et al.; Free Radic. Biol. Med.
65, 1134 (2013),
Application(s): PCR, WB, ChIP Assay,
Abstract;
Full Text
Inhibition of melanogenesis by the pyridinyl imidazole class of compounds: possible involvement of the Wnt/β-catenin signaling pathway: B. Bellei, et al.; PloS One
7, e330201 (2012),
Application(s): WB, PCR, Flow, IF,
Abstract;
Full Text
Crosstalk between Nodal/activin and MAPK p38 signaling is essential for anterior-posterior axis specification: M. Clements, et al.; Curr. Biol.
21, 1289 (2011),
Application(s): p38 in regulating the threshold of Nodal signaling and propose a new mechanism by which A-P axis development can be reinforced during early embryogenesis,
Abstract;
Full Text
TLR agonists extend the functional lifespan of professional phagocytic granulocytes in the bony fish gilthead seabream and direct precursor differentiation towards the production of granulocytes: M.P. Sepulcre, et al.; Mol. Immunol.
48, 846 (2011),
Application(s): IF, Flow, WB,
Abstract;
Cellular stress causes reversible, PRKAA1/2-, and proteasome-dependent ID2 protein loss in trophoblast stem cells: W. Zhong, et al.; Reproduction
140, 921 (2010),
Application(s): IC, WB,
Abstract;
Full Text
Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models: J.R. Jackson, et al.; J. Pharmacol. Exp. Ther.
284, 687 (1998),
Abstract;
Structural basis of inhibitor selectivity in MAP kinases: Z. Wang, et al.; Structure
6, 1117 (1998),
Abstract;
