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Protein kinase inhibitor
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.
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Product Details
| Alternative Name |
4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole |
|---|---|
| Appearance |
White to off-white powder. |
| CAS |
152121-47-6 |
| Couple Target |
p38, Phosphoinositide-dependent protein kinase |
| Couple Type |
Inhibitor |
| Formula |
C21H16N3FOS |
| MW |
377.4 |
| Purity |
≥97% (HPLC) |
| Solubility |
Soluble in DMSO (50mg/ml). |
| Technical Info / Product Notes |
Replacement for ADI-HPK-110 |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- CREB Is Activated by the SCF/KIT Axis in a Partially ERK-Dependent Manner and Orchestrates Survival and the Induction of Immediate Early Genes in Human Skin Mast Cells: K. Franke, et al.; Int. J. Mol. Sci. 24, 4135 (2023), Abstract
- Picolinafen exposure induces ROS accumulation and calcium depletion, leading to apoptosis in porcine embryonic trophectoderm and uterine luminal epithelial cells: W. Park, et al.; Theriogenology 201, 12 (2023), Abstract
- Fluroxypyr-1-methylheptyl ester causes apoptosis of bovine mammary gland epithelial cells by regulating PI3K and MAPK signaling pathways and endoplasmic reticulum stress: G. Am, et al.; Pestic. Biochem. Physiol. 180, 105003 (2022), Abstract
- TRAIL receptors promote constitutive and inducible IL-8 secretion in non-small cell lung carcinoma: F. Favaro, et al.; Cell Death Dis. 13, 1046 (2022), Abstract
- Aclonifen induces bovine mammary gland epithelial cell death by disrupting calcium homeostasis and inducing ROS production: J. Park, et al.; Pestic. Biochem. Physiol. 181, 105011 (2022), Abstract
- Hesperidin Suppresses the Proliferation of Prostate Cancer Cells by Inducing Oxidative Stress and Disrupting Ca2+ Homeostasis: S.A. Jeong, et al.; Antioxidants 11, 1633 (2022), Abstract
- Exosomal p38 Mitogen-activated Protein Kinase Promotes Tumour Repopulation in TP53-mutated Bile Duct Cancer Cells: M. Osawa, et al.; Anticancer Res. 42, 745 (2022), Abstract
- p38-mediated cell growth and survival drive rapid embryonic wound repair: G. Scepanovic , et al.; Cell Rep. 37, 109874 (2021), Abstract
- 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
- FJU-C28 inhibits the endotoxin-induced pro-inflammatory cytokines expression via suppressing JNK, p38 MAPK and NF-κB signaling pathways: F. Jung, et al.; Pharmacol. Res. Perspect. 9, e00876 (2021), Abstract
- Direct activation of endothelial cells by SARS-CoV-2 nucleocapsid protein is blocked by Simvastatin: Y. Qian, et al.; bioRxiv , (2021), Application(s): Treatment of human primary lung microvascular endothelial cells (HLMECs), Abstract — Full Text
- Exposure to fipronil induces cell cycle arrest, DNA damage, and apoptosis in porcine trophectoderm and endometrial epithelium, leading to implantation defects during early pregnancy: W. Park, et al.; Environ. Pollut. 291, 118234 (2021), Abstract
- Induction of Lysosomal Membrane Permeabilization Is a Major Event of FTY720-Mediated Non-Apoptotic Cell Death in Human Glioma Cells: K. Min, et al.; Cancers (Basel) 12, 3388 (2020), Abstract — Full Text
- Regulation of hippocampal neuronal apoptosis and autophagy in mice with sepsis-associated encephalopathy by immunity-related GTPase M1: R.X. Zhou, et al.; CNS Neurosci. Ther. 26, 177 (2020), Abstract — Full Text
- ArhGAP15, a RacGAP, Acts as a Temporal Signaling Regulator of Mac-1 Affinity in Sterile Inflammation: A. Margraf, et al.; J. Immunol. 205, 1365 (2020), Application(s): Murine neutrophils treatment, 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
- 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
- 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
- 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
- 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
- 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
- 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
- Mechanotransduction-Induced Reversible Phenotypic Switching in Prostate Cancer Cells: Aw Yong, K. M., Sun, Y., et al.; Biophys. J. 112, 1236 (2017), 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
- 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
- Avian leukosis virus subgroup J induces VEGF expression via NF-κB/PI3K-dependent IL-6 production: Gao, Y., Zhang, Y., et al.; Oncotarget 7, 80275 (2016), Application(s): In Vitro, Abstract
- Cilia are required for asymmetric nodal induction in the sea urchin embryo: Tisler, M., Wetzel, F., et al.; BMC Dev. Biol. 16, 28 (2016), Abstract
- Hepatitis B virus X protein activates Notch signaling by its effects on Notch1 and Notch4 in human hepatocellular carcinoma: Gao, J., Xiong, Y., et al.; Int. J. Oncol. 48, 329 (2016), 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
- Activation of autophagy by FOXO3 regulates redox homeostasis during osteogenic differentiation: M.C. Gómez-Puerto, et al.; Autophagy 12, 1804 (2016), Abstract — Full Text
- 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
- 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
- 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
- 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
- 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
- Antiviral potential of ERK/MAPK and PI3K/AKT/mTOR signaling modulation for Middle East respiratory syndrome coronavirus infection as identified by temporal kinome analysis: Kindrachuk, J., Ork, B., et al.; Antimicrob. Agents Chemother. 59, 1088 (2015), Abstract
- Induction of neurite outgrowth in PC12 cells treated with temperature-controlled repeated thermal stimulation: Kudo, T. A., Kanetaka, H., et al.; PLoS One 10, e0124024 (2015), Abstract
- Inhibition of FAAH confers increased stem cell migration via PPARα: Wollank, Y., Ramer, R., et al.; J. Lipid Res. 56, 1947 (2015), Abstract
- Post-transcriptional regulation of satellite cell quiescence by TTP-mediated mRNA decay: Hausburg, M. A., Doles, J. D., et al.; Elife 4, e03390 (2015), Abstract
- 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
- 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
- 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
- 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
- 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
- Sodium transport is modulated by p38 kinase-dependent cross-talk between ENaC and Na,K-ATPase in collecting duct principal cells: Wang, Y. B., Leroy, V., et al.; J. Am. Soc. Nephrol. 25, 250 (2014), Abstract
- Expression profile of cord blood neutrophils and dysregulation of HSPA1A and OLR1 upon challenge by bacterial peptidoglycan: Fong, O. N., Chan, K. Y., et al.; J. Leukoc. Biol. 95, 169 (2014), Abstract
- Expression of the transcription factor Egr-1 in pancreatic acinar cells following stimulation of cholecystokinin or Gαq-coupled designer receptors: Kaufmann, A., Rössler, O. G., et al.; Cell. Physiol. Biochem. 33, 1411 (2014), Abstract
- Valproic acid overcomes transforming growth factor-β-mediated sorafenib resistance in hepatocellular carcinoma: Matsuda, Y., Wakai, T., et al.; Int. J. Clin. Exp. Pathol. 7, 1299 (2014), Abstract
- Small molecule-induced mitochondrial disruption directs prostate cancer inhibition via UPR signaling: Rico-Bautista, E., Zhu, W., et al.; Oncotarget 4, 1212 (2013), Abstract
- Phosphorylation of serine 4,642 in the C-terminus of plectin by MNK2 and PKA modulates its interaction with intermediate filaments: Bouameur, J. E., Schneider, Y., et al.; J. Cell Sci. 126, 4195 (2013), Abstract
- Induction of interleukin-10 is dependent on p38 mitogen-activated protein kinase pathway in macrophages infected with porcine reproductive and respiratory syndrome virus: Hou, J., Wang, L., et al.; Virol. J. 9, 165 (2012), Abstract
- Regulation of Rela/p65 and Endothelial Cell Inflammation by Proline-Rich Tyrosine Kinase 2: K.M. Bijli, et al.; Am. J. Respir. Cell Mol. Biol. 47, 660 (2012), Abstract — Full Text
- IRES-dependent translation of egr2 is induced under inflammatory conditions: Rübsamen, D., Blees, J. S., et al.; RNA 18, 1910 (2012), Abstract
- Astrocyte senescence as a component of Alzheimer’s disease: Bhat, R., Crowe, E. P., et al.; PLoS One 7, e45069 (2012), Abstract
- The ω-3 epoxide of eicosapentaenoic acid inhibits endothelial cell proliferation by p38 MAP kinase activation and cyclin D1/CDK4 down-regulation: Cui, P. H., Petrovic, N., et al.; Br. J. Pharmacol. 162, 1143 (2011), Abstract
- Thapsigargin induces expression of activating transcription factor 3 in human keratinocytes involving Ca2+ ions and c-Jun N-terminal protein kinase: Spohn, D., Rössler, O. G., et al.; Mol. Pharmacol. 78, 865 (2010), Abstract
- DNA-dependent protein kinase catalytic subunit mediates T-cell loss in rheumatoid arthritis: Shao, L., Goronzy, J. J., et al.; EMBO Mol. Med. 2, 415 (2010), Abstract
- Increased monomerization of mutant HSPB1 leads to protein hyperactivity in Charcot-Marie-Tooth neuropathy: Almeida-Souza, L., Goethals, S., et al.; J. Biol. Chem. 285, 12778 (2010), Abstract
- Role of SMAD and non-SMAD signals in the development of Th17 and regulatory T cells: Lu, L., Wang, J., et al.; J. Immunol. 184, 4295 (2010), Abstract
- Inhibition of N-(4-hydroxyphenyl)retinamide-induced autophagy at a lower dose enhances cell death in malignant glioma cells: Tiwari, M., Bajpai, V. K., et al.; Carcinogenesis 29, 600 (2008), Abstract
- CoCl2 induces protective events via the p38-MAPK signalling pathway and ANP in the perfused amphibian heart: Gaitanaki, C., Kalpachidou, T., et al.; J. Exp. Biol. 210, 2267 (2007), Abstract
- Synergistic effect of AS101 and Bryostatin-1 on myeloid leukemia cell differentiation in vitro and in an animal model: Hayun, M., Okun, E., et al.; Leukemia 21, 1504 (2007), Abstract
- Role of receptor for advanced glycation end-products and signalling events in advanced glycation end-product-induced monocyte chemoattractant protein-1 expression in differentiated mouse podocytes: Gu, L., Hagiwara, S., et al.; Nephrol. Dial. Transplant. 21, 299 (2006), Abstract
- 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
- Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor, SB203580: A. Kalmes, et al.; FEBS Lett. 444, 71 (1999), Abstract
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase: T.F. Gallagher, et al.; Bioorg. Med. Chem. 5, 49 (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
- The primary structure of p38 gamma: a new member of p38 group of MAP kinases: Z. Li, et al.; BBRC 228, 334 (1996), 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
- 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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