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Submit Review(5Z)-7-Oxozeaenol
说明： Potent and selective TAK1 MAPKKK inhibitor
化学名： (3S,5Z,8S,9S,11E)-3,4,9,10-tetrahydro-8,9,16-trihydroxy-14-methoxy-3-methyl-1H-2-benzoxacyclotetradecin-1,7(8H)-dione
纯度： ≥98% (HPLC)
生物活性 for (5Z)-7-Oxozeaenol
(5Z)-7-Oxozeaenol is a resorcyclic lactone of fungal origin that acts as a potent and selective transforming growth factor-β-activated kinase 1 (TAK1) mitogen-activated protein kinase kinase kinase (MAPKKK) inhibitor (IC50 = 8 nM). Displays > 33-fold and > 62-fold selectivity over MEKK1 and MEKK4 respectively. Inhibits IL-1-induced activation of NF-κB (IC50 = 83 nM) and JNK/p38. Inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF-α-induced apoptosis in vitro.
技术数据 for (5Z)-7-Oxozeaenol
| 分子量 | 362.37 |
| 公式 | C19H22O7 |
| 储存 | Desiccate at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 253863-19-3 |
| PubChem ID | 9799061 |
| InChI Key | NEQZWEXWOFPKOT-ULSULSEOSA-N |
| Smiles | O=C/2[C@@H](O)[C@@H](O)C/C=C/C1=CC(OC)=CC(O)=C1C(O[C@@H](C)C\C=C2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for (5Z)-7-Oxozeaenol
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 9.06 | 25 |
制备储备液 for (5Z)-7-Oxozeaenol
以下数据基于产品分子量 362.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 11.04 mL | 55.19 mL | 110.38 mL |
| 1.25 mM | 2.21 mL | 11.04 mL | 22.08 mL |
| 2.5 mM | 1.1 mL | 5.52 mL | 11.04 mL |
| 12.5 mM | 0.22 mL | 1.1 mL | 2.21 mL |
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产品说明书 for (5Z)-7-Oxozeaenol
参考文献 for (5Z)-7-Oxozeaenol
参考文献是支持产品生物活性的出版物。
Ninomiya-Tsuji et al (2003) A resorcyclic acid lactone, 5Z-7-Oxozeaenol, prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase. J.Biol.Chem. 278 18485 PMID: 12624112
Choo et al (2006) Blockade of transforming growth factor-β-activated kinase 1 activity enhances TRAIL-induced apoptosis through activation of a caspase cascade. Mol.Cancer Ther. 5 2970 PMID: 17172402
Windheim et al (2007) Molecular mechanisms involved in the regulation of cytokine production by muramyl dipeptide. Biochem.J. 404 179 PMID: 17348859
If you know of a relevant reference for (5Z)-7-Oxozeaenol, please let us know.
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关键词: (5Z)-7-Oxozeaenol, (5Z)-7-Oxozeaenol supplier, Potent, selective, TAK1, MAPKKK, inhibitors, inhibits, Kinases, Other, 3604, Tocris Bioscience
40 篇 (5Z)-7-Oxozeaenol 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (5Z)-7-Oxozeaenol 的部分引用包括：
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Tsvetana et al (2022) TAK1 protein kinase activity is required for TLR signalling and cytokine production in myeloid cells. Biochem J 479 1891-1907 PMID: 36062803
Teri L et al (2022) TAK1 inhibition increases proliferation and differentiation of chick retinal cells. Front Cell Dev Biol 10 698233 PMID: 36176271
Guei-Sheung et al (2022) Topical application of TAK1 inhibitor encapsulated by gelatin particle alleviates corneal neovascularization. Theranostics 12 657-674 PMID: 34976206
Iriondo (2018) TAK1 mediates microenvironment-triggered autocrine signals and promotes triple-negative breast cancer lung metastasis. Nat Commun 9 1994 PMID: 29777109
Wim B et al (2014) Inhibition of TAK1 and/or JAK can rescue impaired chondrogenic differentiation of human mesenchymal stem cells in osteoarthritis-like conditions. Tissue Eng Part A 20 2243-52 PMID: 24547725
Michelle et al (2020) TAK1 signaling regulates p53 through a mechanism involving ribosomal stress. Sci Rep 10 2517 PMID: 32054925
Seungwoon et al (2020) CD137 Signaling Regulates Acute Colitis via RALDH2-Expressing CD11b-CD103+ DCs. Cell Rep 30 4124-4136.e5 PMID: 32209473
Deborah J et al (2020) Tristetraprolin regulates necroptosis during tonic Toll-like receptor 4 (TLR4) signaling in murine macrophages. J Biol Chem 295 4661-4672 PMID: 32094226
Jie et al (2020) FoxO1 is a crucial mediator of TGF-β/TAK1 signaling and protects against osteoarthritis by maintaining articular cartilage homeostasis. Proc Natl Acad Sci U S A 117 30488-30497 PMID: 33199631
Bhaskar et al (2019) TAK1 converts Sequestosome 1/p62 from an autophagy receptor to a signaling platform. EMBO Rep 20 e46238 PMID: 31347268
Thamodaran (2016) p38 (Mapk14/11) occupies a regulatory node governing entry into primitive endoderm differentiation during preimplantation mouse embryo development. Open Biol 6 PMID: 27605380
Morimoto et al (2010) Phosphorylation of lysophosphatidylcholine acyltransferase 2 at Ser34 enhances platelet-activating factor production in endotoxin-stimulated macrophages. Proc Natl Acad Sci U S A 285 29857 PMID: 20663880
Zhang et al (2015) Stabilization of ATF5 by TAK1-Nemo-like kinase critically regulates the interleukin-1β-stimulated C/EBP signaling pathway. Nat Commun 35 778 PMID: 25512613
Ahmed et al (2011) The E3 ligase Itch and deubiquitinase Cyld act together to regulate Tak1 and inflammation. Nat Immunol 12 1176 PMID: 22057290
Kate E et al (2023) Caspase-8-driven apoptotic and pyroptotic crosstalk causes cell death and IL-1β release in X-linked inhibitor of apoptosis (XIAP) deficiency. EMBO J 42 e110468 PMID: 36647737
Anthony et al (2023) Induction of pro-inflammatory genes by fibronectin DAMPs in three fibroblast cell lines: Role of TAK1 and MAP kinases. PLoS One 18 e0286390 PMID: 37228128
Annibaldi et al (2018) Ubiquitin-Mediated Regulation of RIPK1 Kinase Activity Independent of IKK and MK2. Mol Cell 69 566 PMID: 29452637
Jones et al (2018) Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition. Sci Signal 11 PMID: 29511118
Choi et al (2013) Prolonged NF-κB activation by a macrophage inhibitory cytokine 1-linked signal in enteropathogenic Escherichia coli-infected epithelial cells. Infect Immun 81 1860 PMID: 23403560
Graham et al (2014) BMP signalling regulates the pre-implantation development of extra-embryonic cell lineages in the mouse embryo. J Biol Chem 5 5667 PMID: 25514175
Hilt et al (2019) Platelet-derived β2M regulates monocyte inflammatory responses. JCI Insight 4 PMID: 30702442
Fleskens et al (2019) Nemo-like Kinase Drives Foxp3 Stability and Is Critical for Maintenance of Immune Tolerance by Regulatory T Cells. Cell Rep 26 3600 PMID: 30917315
Lu et al (2017) Central Administration of 5Z-7-Oxozeaenol Protects Experimental Autoimmune Encephalomyelitis Mice by Inhibiting Microglia Activation. Front Pharmacol 8 789 PMID: 29163172
Olsen et al (2014) Inhibition of transglutaminase 2, a novel target for pulmonary fibrosis, by two small electrophilic molecules. Am J Respir Cell Mol Biol 50 737 PMID: 24175906
Ansell et al (2014) Activation of TAK1 by MYD88 L265P drives malignant B-cell Growth in non-Hodgkin lymphoma. Blood Cancer J 4 e183 PMID: 24531446
Lionarons et al (2019) RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance. Cancer Cell 36 68 PMID: 31257073
Ismail et al (2017) Rapid Activation of Transforming Growth Factor β-Activated Kinase 1 in Chondrocytes by Phosphorylation and K(63) -Linked Polyubiquitination Upon Injury to Animal Articular Cartilage. Arthritis Rheumatol 69 565 PMID: 27768832
Jones et al (2017) Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. Nat Chem Biol 13 38 PMID: 27820799
Jaco et al (2017) MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death. Mol Cell 66 698 PMID: 28506461
Yang et al (2017) Expression and function of transforming growth factor?β?activated protein kinase 1 in gastric cancer. Mol Med Rep 16 3103 PMID: 28714004
van Caam (2017) TGFβ1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity. Arthritis Research & Therapy 19 112 PMID: 28569204
Sharon E et al (2015) Inhibition of glycogen synthase kinase-3β enhances cognitive recovery after stroke: the role of TAK1. Learn Mem 22 336-43 PMID: 26077686
Huang et al (2015) Targeting of TGF-β-activated protein kinase 1 inhibits chemokine (C-C motif) receptor 7 expression, tumor growth and metastasis in breast cancer. Oncotarget 6 995 PMID: 25557171
Kuk et al (2015) 5Z-7-Oxozeanol Inhibits the Effects of TGFβ1 on Human Gingival Fibroblasts. PLoS One 10 e0123689 PMID: 25927238
White et al (2012) Protection from cerebral ischemia by inhibition of TGFβ-activated kinase. Exp Neurol 237 238 PMID: 22683931
Nigel et al (2021) Cardiac Tissue Factor Regulates Inflammation, Hypertrophy, and Heart Failure in Mouse Model of Type 1 Diabetes. Diabetes 70 2131-2146 PMID: 34155039
Ye et al (2021) Inhibition of the MAP2K7-JNK pathway with 5Z-7-oxozeaenol induces apoptosis in T-cell acute lymphoblastic leukemia. Oncotarget 12 1787-1801 PMID: 34504651
Dandan et al (2017) Regulatory role of tumor necrosis factor receptor-associated factor 6 in breast cancer by activating the protein kinase B/glycogen synthase kinase 3β signaling pathway. Mol Med Rep 16 2269-2273 PMID: 28627683
Kim et al (2016) Identification of therapeutic targets applicable to clinical strategies in ovarian cancer. BMC Cancer 16 678 PMID: 27558154
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Works for kinase assay, easy storage.
By
Scott Scarneo on 02/06/2019
分析类型： In Vitro
种属： Human
Works great for kinase assay. This was tested in TAK1 in vitro kinase assay.
Great inhibitor for TAK1 signaling.
By
Anonymous on 12/04/2017
分析类型： In Vitro
种属： Mouse
细胞系/组织： Primary human small airway epithelial cells
Primary human small airway epithelial cells were incubated with TAK1 inhibitor prior to the addition of poly(I:C). The supernatant was collected and analyzed for IL-6.
