MW 267.28 Da, Purity >99%. Inhibitor of MKK1 (MEK1). Achieve your results faster with highly validated, pure and trusted compounds.
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- Translational psychiatry 12:5222022ERK/mTOR signaling may underlying the antidepressant actions of rapastinel in mice.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMengxin Shen,Dan Lv,Xinya Liu,Chuang WangPubMed 36550125
- Frontiers in immunology 12:7558622021Co-Exposure of Cardiomyocytes to IFN-γ and TNF-α Induces Mitochondrial Dysfunction and Nitro-Oxidative Stress: Implications for the Pathogenesis of Chronic Chagas Disease Cardiomyopathy.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJoão Paulo Silva Nunes,Pauline Andrieux,Pauline Brochet,Rafael Ribeiro Almeida,Eduardo Kitano,André Kenji Honda,Leo Kei Iwai,Débora Andrade-Silva,David Goudenège,Karla Deysiree Alcântara Silva,Raquel de Souza Vieira,Débora Levy,Sergio Paulo Bydlowski,Frédéric Gallardo,Magali Torres,Edimar Alcides Bocchi,Miguel Mano,Ronaldo Honorato Barros Santos,Fernando Bacal,Pablo Pomerantzeff,Francisco Rafael Martins Laurindo,Priscila Camillo Teixeira,Helder I Nakaya,Jorge Kalil,Vincent Procaccio,Christophe Chevillard,Edecio Cunha-NetoPubMed 34867992
- Journal of neuroinflammation 18:1502021Red nucleus IL-33 facilitates the early development of mononeuropathic pain in male rats by inducing TNF-α through activating ERK, p38 MAPK, and JAK2/STAT3.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHao-Nan Li,Qing-Qing Yang,Wen-Tao Wang,Xue Tian,Fan Feng,Shu-Ting Zhang,Yu-Tong Xia,Jia-Xue Wang,Yuan-Wu Zou,Jun-Yang Wang,Xiao-Yan ZengPubMed 34225736
- Glia 69:1478-14932021Expression and secretion of apoE isoforms in astrocytes and microglia during inflammation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMaria Fe Lanfranco,Jordy Sepulveda,Gregory Kopetsky,G William RebeckPubMed 33556209
- International journal of molecular medicine 47:256-2662020TGF‑β1‑induced autophagy activates hepatic stellate cells via the ERK and JNK signaling pathways.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJing Zhang,Na Jiang,Jian Ping,Lieming XuPubMed 33236148
- Cell reports 29:4144-4158.e72019Discrimination of Dormant and Active Hematopoietic Stem Cells by G Marker Reveals Dormancy Regulation by Cytoplasmic Calcium.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTsuyoshi Fukushima,Yosuke Tanaka,Fiona K Hamey,Chih-Hsiang Chang,Toshihiko Oki,Shuhei Asada,Yasutaka Hayashi,Takeshi Fujino,Taishi Yonezawa,Reina Takeda,Kimihito Cojin Kawabata,Tomofusa Fukuyama,Terumasa Umemoto,Keiyo Takubo,Hitoshi Takizawa,Susumu Goyama,Yasushi Ishihama,Hiroaki Honda,Berthold Göttgens,Toshio KitamuraPubMed 31851939
- Biochimica et biophysica acta. Molecular cell rese 1866:1398-14112019Regulation of MAP kinase-mediated endothelial dysfunction in hyperglycemia via arginase I and eNOS dysregulation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSafoura Mazrouei et. al.PubMed 31150695
- FASEB journal : official publication of the Federa 33:7301-73142019The emerging role of xanthine oxidase inhibition for suppression of breast cancer cell migration and metastasis associated with hypercholesterolemia.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSe-Hyun Oh et. al.PubMed 30860872
- Journal of neuroscience research 96:1847-18612018Red nucleus interleukin-1β evokes tactile allodynia through activation of JAK/STAT3 and JNK signaling pathways.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYi-Jie Guo et. al.PubMed 30216497
Key facts
- CAS number
- 167869-21-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 267.28 Da
- Molecular formula
- C16H13NO3
- PubChem identifier
- 4713
- Nature
- Synthetic
Alternative names
(R)-limonene 6-monooxygenase, (S)-limonene 6-monooxygenase, (S)-limonene 7-monooxygenase, 1,8-cineole 2-exo-monooxygenase, AI838772, AW493413, Albendazole monooxygenase, Albendazole sulfoxidase, Antigen NY-CO-13, BCC7, BCD541, C-mpl ligand, CP2C9_HUMAN, CP33, CP34, CP3A4_HUMAN, CPC12, CPC8, CPC9, CPCJ, CYP2C, CYP2C10, CYP3, CYP3A, CYP3A3, CYP3A4, CYPIIC9, CYPIIIA3, CYPIIIA4, Cellular tumor antigen p53, Component of gems 1, Craf 1 transforming gene, Cyclooxygenase 3, included, Cyclooxygenase-1, Cytochrome P-450MP, Cytochrome P450 2C9, Cytochrome P450 3A3, Cytochrome P450 3A4, Cytochrome P450 HLp, Cytochrome P450 MP-4, Cytochrome P450 MP-8, Cytochrome P450 NF-25, Cytochrome P450 PB-1, Cytochrome P450 family 3 subfamily A polypeptide 4, Cytochrome P450 subfamily IIIA polypeptide 4, Cytochrome P450, family 2, subfamily C, polypeptide 9, Cytochrome P450-PCN1, Dual specificity mitogen-activated protein kinase kinase 1, EC 1.14.99.1, ERK activator kinase 1, ERK-1, ERK-2, ERR a, ERR-alpha, ERR1 protein, ERR1_HUMAN, ERT 2, ERT1, ESRL 1, ESRR A, Estrogen receptor related 1, Estrogen receptor-like 1, Estrogen-related receptor alpha, Estrra, Extracellular signal related kinase 1, Extracellular signal-regulated kinase 1, Extracellular signal-regulated kinase 2, FLJ11090, FLJ92943, Gemin-1, Glucocorticoid inducible P450, HGNC6877, HLP, HS44KDAP, HUMKER1A, Insulin-stimulated MAP2 kinase, LFS1, MAP Kinase, MAP kinase 1, MAP kinase 2, MAP kinase 3, MAP kinase isoform p42, MAP kinase isoform p44, MAP kinase kinase 1, MAP kinase/Erk kinase 1, MAP2K1, MAPK, MAPK 1, MAPK/ERK kinase 1, MAPKK 1, MEK 1, MEKK 1, MGC104252, MGC112732, MGC126680, MGC149605, MGC20180, MGC88320, MGDF, MK01_HUMAN, MK03_HUMAN, MKCSF, MKK 1, MP2K1_HUMAN, MPL ligand, MPLLG, Megakaryocyte colony-stimulating factor, Megakaryocyte growth and development factor, Megakaryocyte stimulating factor, Microsomal monooxygenase, Microtubule-associated protein 2 kinase, Mitogen Activated Protein Kinase Kinase 1, Mitogen-activated protein kinase 1, Mitogen-activated protein kinase 2, Mitogen-activated protein kinase 3, Murine sarcoma 3611 oncogene 1, Mutant tumor protein 53, Myeloproliferative leukemia virus oncogene ligand, NF 25, NR3B1, Nifedipine oxidase, Nuclear receptor subfamily 3 group B member 1, OTTHUMP00000020135, OTTHUMP00000125198, OTTHUMP00000174538, OTTHUMP00000174541, OTTHUMP00000223567, OTTHUMP00000223568, OTTHUMP00000224066, OTTHUMP00000226924, Oncogene RAF1, P38, P41, P450 III steroid inducible, P450 MP, P450 PB 1, P450 PCN1, P450, family III, P450C2C, P450C3, P450IIC19, P450IIC9, P53_HUMAN, PCOX1, PGG/HS, PGH synthase 1, PGH1_HUMAN, PGHS-1, PHS 1, PRKM 2, PRKM 3, PRKM1, PRKMK 1, PTGHS, PTGS1, Partial COX1 proteins, included, Phosphoprotein p53, Prostaglandin G/H synthase 1, Prostaglandin H2 synthase 1, Prostaglandin-endoperoxide synthase 1, Prostaglandin-endoperoxide synthase 1 (prostaglandin G/H synthase and cyclooxygenase), Protein Kinase Mitogen Activated 3, Protein kinase mitogen activated kinase 1 (MAP kinase kinase 1), Quinine 3-monooxygenase, RP24-311F12.2, Raf proto oncogene serine threonine protein kinase, S-mephenytoin 4-hydroxylase, SCAN1, SMA, SMA 1, SMA 2, SMA 3, SMA 4, SMN1, SMN2, SMNT, SMN_HUMAN, Sarcoma 3611 oncogene, Steroid hormone receptor ERR1, Survival motor neuron protein, Survival of motor neuron 1, telomeric, T-BCD541, THCYT1, TRP53, TYDP, TYDP1_HUMAN, Taurochenodeoxycholate 6-alpha-hydroxylase, Thrombopoietin, Thrombopoietin nirs variant 1, Tp53, Transformation related protein 53, Tumor protein 53, Tumor protein p53, Tumor suppressor p53, Tyr-DNA phosphodiesterase 1, Tyrosyl-DNA phosphodiesterase 1, Xenobiotic monooxygenase, cytochrome P-450 S-mephenytoin 4-hydroxylase, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, estrogen receptor related receptor alpha, flavoprotein-linked monooxygenase, hERR1, p42-MAPK, p44-ERK1, p44-MAPK, p53 tumor suppressor, protein kinase mitogen-activated kinase 1, protein kinase, mitogen-activated, 1, protein kinase, mitogen-activated, 2, protein tyrosine kinase ERK2, tumor antigen p55, vRaf1 murine leukemia viral oncogene homologue 1
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MW 267.28 Da, Purity >99%. Inhibitor of MKK1 (MEK1). Achieve your results faster with highly validated, pure and trusted compounds.
Key facts
- CAS number
- 167869-21-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 267.28 Da
- Molecular formula
- C16H13NO3
- PubChem identifier
- 4713
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 25 mM.
Soluble in ethanol to 5 mM.
Soluble in DMSO to 25 mM and in ethanol to 5 mM.
- Biochemical name
- 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
- Biological description
Inhibitor of MKK1 (MEK1).
- Canonical SMILES
- COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
- InChI
- InChI=1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3
- InChIKey
- QFWCYNPOPKQOKV-UHFFFAOYSA-N
- IUPAC name
- 2-(2-amino-3-methoxyphenyl)chromen-4-one
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
MEK1 also known as MAP2K1 is a dual-specificity kinase that plays a role in the MAPK/ERK pathway. It has a molecular weight of around 45 kDa. MEK1 phosphorylates and activates the extracellular signal-regulated kinases ERK1 and ERK2. MEK1 is expressed in various tissues but is especially abundant in brain and heart tissues. Researchers commonly measure MEK1 levels using techniques like MEK1 ELISA while phospho-MEK antibodies help analyze its activity state.
- Biological function summary
MEK1 impacts cell processes such as proliferation differentiation and survival. It does not work alone but forms a complex with other proteins to exert its function. MEK1 activity is tightly controlled by upstream activators and downstream targets. One of the key phosphorylation sites on MEK1 is at serine 298 often marked as MEK1 pS298. This phosphorylation indicates MEK1's activated state which is critical for its biological function.
- Pathways
MEK1 integrates signals within the MAPK/ERK pathway and interacts closely with RAF kinases upstream and ERK kinases downstream. This pathway modulates cellular responses to growth factors. MEK1 undergoes phosphorylation enhancing its activity and subsequently phosphorylates ERK proteins. Many studies isolate MEK1 activity using specific inhibitors such as the MEK1 inhibitor to dissect pathway dynamics. ERK inhibitor PD98059 also helps when studying parallel interactions with MEK1.
- Associated diseases and disorders
MEK1 mutations or dysregulation have links to several types of cancer including melanoma. These often involve changes that lead to continuous MEK1 activation contributing to uncontrolled cell growth. MEK1 involvement in the RASopathies also shows its connection to disorders characterized by heart and facial abnormalities. In cancer MEK1 works closely with the BRAF protein which often harbors mutations leading to disease progression showcasing MEK1 as a target for therapeutic intervention.
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2 product images
Chemical Structure - PD 98059, MEK1 inhibitor (ab120234)
2D chemical structure image of ab120234, PD 98059, MEK1 inhibitor
Immunocytochemistry/ Immunofluorescence - PD 98059, MEK1 inhibitor (ab120234)
Anti-hnRNP K antibody ab18195 staining hnRNP K in HeLa cells treated with PD 98059 (ab120234), by ICC/IF. Changes in localization of hnRNP K (translocation from cytoplasm to nucleous) correlates with increased concentration of hnRNP K, as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120234 ( hnRNP K) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with Anti-hnRNP K antibody ab18195 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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