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Protein kinase inhibitor
BML-EI286-0001 1 mg 116.00 USD
BML-EI286-0005 5 mg 472.00 USD
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Replaces Prod. #: ALX-270-179

Cell permeable, specific inhibitor of p38 (SAPK2a). Inhibits p38 MAPK stimulation of MAPKAPK2 (IC50=70nM). Can inhibit the key cell cycle event of retinoblastoma protein phosphorylation in interleukin-2-stimulated T cells. Studies on the proximal regulator of this event, the PI(3)K (phosphoinositide 3-kinase)/Akt (protein kinase B; PKB) pathway, showed that SB203580 blocks the phosphorylation and activation of Akt by inhibiting the Akt kinase, phosphoinositide-dependent protein kinase 1 (PDK1).

The concentrations of SB203580 required to block Akt phosphorylation (IC50= 3-5µM) are only approximately 10-fold higher than those required to inhibit p38 MAP kinase (IC50=0.3-0.5µM). These data define a new activity for this drug and suggest that extreme caution should be used when interpreting data when SB203580 has been used at concentrations above 1-2µM. Non-specific effects include inhibition of COX-1 and -2. Enhances clonal growth of skin epithelial progenitor cells and stimulates neural stem cell proliferation.

Product Details

Alternative Name:4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole
Purity:≥97% (HPLC)
Appearance:White to off-white powder.
Solubility:Soluble in DMSO (50mg/ml).
Shipping:Ambient Temperature
Long Term Storage:-20°C
Technical Info/Product Notes:Replacement for ADI-HPK-110
Regulatory Status:RUO - Research Use Only
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Product Literature References

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S1P/S1P2 Signaling Axis Regulates Both NLRP3 Upregulation and NLRP3 Inflammasome Activation in Macrophages Primed with Lipopolysaccharide: C.H. Lee & J.W. Choi; Antioxidants 10, 1706 (2021), Abstract;
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Mitigation of ER-stress and inflammation by chemokine (CC motif) ligand 21 during early pregnancy: H. Bae, et al.; Dev. Comp. Immunol. 94, 73 (2019), Abstract;
Nemo-like kinase drives Foxp3 stability and is critical for maintenance of immune tolerance by regulatory T cells: V. Fleskens, et al.; Cell Rep. 26, 3600 (2019), Abstract; Full Text
Quercetin augments apoptosis of canine osteosarcoma cells by disrupting mitochondria membrane potential and regulating PKB and MAPK signal transduction: S. Ryu, et al.; J. Cell. Biochem. 120, 17449 (2019), Abstract;
Carbon monoxide releasing molecule-2 attenuates Pseudomonas aeruginosa-induced ROS-dependent ICAM-1 expression in human pulmonary alveolar epithelial cells: C.W. Lee, et al.; Redox Biol. 18, 93 (2018), Abstract; Full Text
Chrysin attenuates progression of ovarian cancer cells by regulating signaling cascades and mitochondrial dysfunction: W. Lim, et al.; J. Cell. Physiol. 233, 3129 (2018), Abstract;
PRMT1 mediates RANKL-induced osteoclastogenesis and contributes to bone loss in ovariectomized mice: J.H. Choi, et al.; Exp. Mol. Med. 50, 111 (2018), Abstract; Full Text
Sideroxylin (Callistemon lanceolatus) suppressed cell proliferation and increased apoptosis in ovarian cancer cells accompanied by mitochondrialdysfunction, the generation of reactive oxygen species, and an increase of lipid peroxidation: S. Park, et al.; J. Cell. Physiol. 233, 8597 (2018), Application(s): Treatment of ovarian cancer cells (ES2 and OV90), Abstract;
Acinar-to-Ductal Metaplasia Induced by Transforming Growth Factor Beta Facilitates KRASG12D-driven Pancreatic Tumorigenesis: N. Chuvin, et al.; Cell. Mol. Gastroenterol. Hepatol. 4, 263 (2017), Abstract; Full Text
Balance between IL-3 and type Iinterferons and their interrelationship with FasL dictates lifespan and effector functions of human basophils: B.R. Hagmann, et al.; Clin. Exp. Allergy 47, 71 (2017), Abstract;
Differential expression and functional roles of chemokine (C-C motif) ligand 23 and its receptor chemokine (C-C motif) receptor type 1 in the uterine endometrium during early pregnancy in pigs: W. Jeong, et al.; Dev. Comp. Immunol. 76, 316 (2017), Abstract;
Activation of autophagy by FOXO3 regulates redox homeostasis during osteogenic differentiation: M.C. Gómez-Puerto, et al.; Autophagy 12, 1804 (2016), Abstract; Full Text
Calcitonin gene-related peptide is a key factor in the homing of transplanted human MSCs to sites of spinal cord injury: Y. Zhang, et al.; Sci. Rep. 6, 27724 (2016), Application(s): Migration assay in Boyden chamber, Abstract; Full Text
Curcumin suppresses NTHi-induced CXCL5 expression via inhibition of positive IKKβ pathway and up-regulation of negative MKP-1 pathway: A.S. Konduru, et al.; Sci. Rep. 6, 31695 (2016), Application(s): Cell culture, effect on nuclear translocation of p65, Abstract; Full Text
Delphinidin suppresses proliferation and migration of human ovarian clear cell carcinoma cells through blocking AKT and ERK1/2 MAPK signaling pathways: W. Lim, et al. ; Mol. Cell. Endocrinol. 422, 172 (2016), Application(s): Cell culture, Abstract;
Follicle-stimulating hormone enhances alveolar bone resorption via upregulation of cyclooxygenase-2: C. Zhu, et al.; Am. J. Transl. Res. 8, 3861 (2016), Application(s): Treatment of cultured PDLCs, Abstract; Full Text
Simvastatin induces differentiation of rabbit articular chondrocytes via the ERK-1/2 and p38 kinase pathways: Y. Han, et al.; Exp. Cell Res. 346, 198 (2016), Application(s): Isolation and monolayer culture of rabbit articular chondrocytes, Abstract;
TNF-α increases the expression and activity of vitamin D receptor in keratinocytes: role of c-Jun N-terminal kinase: E. Ziv, et al.; Dermatoendocrinol. 8, e1137399 (2016), Application(s): Cell culture, Abstract; Full Text
Amphiregulin may be a new biomarker of classically activated macrophages: C. Meng, et al.; Biochem. Biophys. Res. Commun. 466, 393 (2015), Application(s): Cell Culture, Abstract;
Areca nut exposure increases secretion of tumor‐promoting cytokines in gingival fibroblasts that trigger DNA damage in oral keratinocytes: R.P. Illeperuma, et al.; Int. J. Cancer 137, 2545 (2015), Application(s): Cell Culture, Abstract; Full Text
Dibenzoylmethane Exerts Metabolic Activity through Regulation of AMP-Activated Protein Kinase (AMPK)-Mediated Glucose Uptake and Adipogenesis Pathways: N. Kim, et al.; PLoS One 10, e0120104 (2015), Application(s): Cell Culture, Abstract; Full Text
Glycated albumin triggers fibrosis and apoptosis via an NADPH oxidase/Nox4-MAPK pathway-dependent mechanism in renal proximal tubular cells: W. Qi, et al.; Mol. Cell. Endocrinol. 405, 74 (2015), Application(s): Cell Culture, Abstract;
Involvement of JNK and Caspase Activation in Hoiamide A-Induced Neurotoxicity in Neocortical Neurons: Z. Cao, et al.; Mar. Drugs 13, 903 (2015), Application(s): Cell Culture, Abstract; Full Text
Phloretin ameliorates chemokines and ICAM-1 expression via blocking of the NF-κB pathway in the TNF-α-induced HaCaT human keratinocytes: W.C. Huang, et al.; Int. Immunopharmacol. 27, 32 (2015), Application(s): Cell Culture, Western Blot, Abstract;
Stimulatory Effects of Interleukin-1 Beta on Development of Porcine Uterine Epithelial Cell are Mediated by Activation of the ERK1/2 MAPK Cell Signaling Cascade: W. Jeong, et al.; Mol. Cell. Endocrinol. 419, 255 (2015), Application(s): Cell culture , Abstract;
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The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mit: F.V. Lali, et al.; J. Biol. Chem. 275, 7395 (2000), Abstract; Full Text
Effect of SB 203580 on the activity of c-Raf in vitro and in vivo: C.A. Hall-Jackson, et al.; Oncogene 18, 2047 (1999), Abstract;
Low density lipoprotein phosphorylates the focal adhesion-associated kinase p125(FAK) in human platelets independent of integrin alphaIIb beta3: C.M. Hackeng, et al.; J. Biol. Chem. 274, 384 (1999), Abstract; Full Text
Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor, SB203580: A. Kalmes, et al.; FEBS Lett. 444, 71 (1999), Abstract;
SB 203580, an inhibitor of p38 mitogen-activated protein kinase, enhances constitutive apoptosis of cytokine-deprived human eosinophils: H. Kankaanranta, et al.; J. Pharmacol. Exp. Ther. 290, 621 (1999), Abstract;
Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution: P.A. Eyers, et al.; Chem. Biol. 5, 321 (1998), Abstract;
Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. SB 203580 also inhibits thromboxane synthase: A.G. Börsch-Haubold, et al.; J. Biol. Chem. 273, 28766 (1998), Abstract; Full Text
The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs): A. Clerk & P.H. Sugden; FEBS Lett. 426, 93 (1998), Abstract;
A p38 MAP kinase inhibitor SB203580 inhibits CD28-dependent T cell proliferation and IL-2 production: S.G. Ward, et al.; Biochem. Soc. Trans. 25, 304S (1997), Abstract;
p38 mitogen activated protein kinase regulates endothelial VCAM-1 expression at the post-transcriptional level: A. Pietersma, et al.; BBRC 230, 44 (1997), Abstract;
Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site: P.R. Young, et al.; J. Biol. Chem. 272, 12116 (1997), Abstract;
Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase: T.F. Gallagher, et al.; Bioorg. Med. Chem. 5, 49 (1997), Abstract;
Characterization of the structure and function of a new mitogen-activated protein kinase (p38beta): Y. Jiang, et al.; J. Biol. Chem. 271, 17920 (1996), Abstract; Full Text
The primary structure of p38 gamma: a new member of p38 group of MAP kinases: Z. Li, et al.; BBRC 228, 334 (1996), Abstract;
SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1: A. Cuenda, et al.; FEBS Lett. 364, 229 (1995), Abstract;
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis: J.C. Lee, et al.; Nature 372, 739 (1994), Abstract;

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