product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
3604/1
catalog :
3604/1
quantity :
1 mg
price :
232 USD
more info or order :
citations: 45
Reference
Maddali P, Ambesi A, McKeown Longo P. Induction of pro-inflammatory genes by fibronectin DAMPs in three fibroblast cell lines: Role of TAK1 and MAP kinases. PLoS ONE. 2023;18:e0286390 pubmed publisher
Hughes S, Lin M, Weir A, Huang B, Xiong L, Chua N, et al. Caspase-8-driven apoptotic and pyroptotic crosstalk causes cell death and IL-1β release in X-linked inhibitor of apoptosis (XIAP) deficiency. EMBO J. 2023;42:e110468 pubmed publisher
Carrillo C, Ravi V, Tiwari S, Chernoff E, Belecky Adams T. TAK1 inhibition increases proliferation and differentiation of chick retinal cells. Front Cell Dev Biol. 2022;10:698233 pubmed publisher
Rodrigues M, Petrova T, Tibbs B, Arthur J, Cohen P. TAK1 protein kinase activity is required for TLR signalling and cytokine production in myeloid cells. Biochem J. 2022;479:1891-1907 pubmed publisher
Moser R, Annis J, Nikolova O, Whatcott C, Gurley K, Mendez E, et al. Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res. 2022;82:3375-3393 pubmed publisher
Wang J, Tseng C, Lin F, Chen J, Hsieh E, Lama S, et al. Topical application of TAK1 inhibitor encapsulated by gelatin particle alleviates corneal neovascularization. Theranostics. 2022;12:657-674 pubmed publisher
Chen T, Du W, Junco J, Bridges C, Shen Y, Puppi M, et al. Inhibition of the MAP2K7-JNK pathway with 5Z-7-oxozeaenol induces apoptosis in T-cell acute lymphoblastic leukemia. Oncotarget. 2021;12:1787-1801 pubmed publisher
Cibi D, Sandireddy R, Bogireddi H, Tee N, Ghani S, Singh B, et al. Cardiac Tissue Factor Regulates Inflammation, Hypertrophy, and Heart Failure in Mouse Model of Type 1 Diabetes. Diabetes. 2021;70:2131-2146 pubmed publisher
Wang C, Shen J, Ying J, Xiao D, O Keefe R. 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. 2020;117:30488-30497 pubmed publisher
Jin J, Jung I, Moon S, Jeon S, Jeong S, Sonn S, et al. CD137 Signaling Regulates Acute Colitis via RALDH2-Expressing CD11b-CD103+ DCs. Cell Rep. 2020;30:4124-4136.e5 pubmed publisher
Ariana A, Alturki N, Hajjar S, Stumpo D, Tiedje C, Alnemri E, et al. Tristetraprolin regulates necroptosis during tonic Toll-like receptor 4 (TLR4) signaling in murine macrophages. J Biol Chem. 2020;295:4661-4672 pubmed publisher
Zonneville J, Wong V, Limoge M, NIKIFOROV M, Bakin A. TAK1 signaling regulates p53 through a mechanism involving ribosomal stress. Sci Rep. 2020;10:2517 pubmed publisher
Kehl S, Soos B, Saha B, Choi S, Herren A, Johansen T, et al. TAK1 converts Sequestosome 1/p62 from an autophagy receptor to a signaling platform. EMBO Rep. 2019;20:e46238 pubmed publisher
Lionarons D, Hancock D, Rana S, East P, Moore C, Murillo M, et al. RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance. Cancer Cell. 2019;: pubmed publisher
Fleskens V, Minutti C, Wu X, Wei P, Pals C, McCrae J, et al. Nemo-like Kinase Drives Foxp3 Stability and Is Critical for Maintenance of Immune Tolerance by Regulatory T Cells. Cell Rep. 2019;26:3600-3612.e6 pubmed publisher
Hilt Z, Pariser D, Ture S, Mohan A, Quijada P, Asante A, et al. Platelet-derived β2M regulates monocyte inflammatory responses. JCI Insight. 2019;: pubmed publisher
Iriondo O, Liu Y, Lee G, Elhodaky M, Jimenez C, Li L, et al. TAK1 mediates microenvironment-triggered autocrine signals and promotes triple-negative breast cancer lung metastasis. Nat Commun. 2018;9:1994 pubmed publisher
Jones D, Jenney A, Joughin B, Sorger P, Lauffenburger D. Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition. Sci Signal. 2018;11: pubmed publisher
Annibaldi A, Wicky John S, Vanden Berghe T, Swatek K, Ruan J, Liccardi G, et al. Ubiquitin-Mediated Regulation of RIPK1 Kinase Activity Independent of IKK and MK2. Mol Cell. 2018;69:566-580.e5 pubmed publisher
Lu L, Zhang X, Tong H, Zhang W, Xu P, Qu S. Central Administration of 5Z-7-Oxozeaenol Protects Experimental Autoimmune Encephalomyelitis Mice by Inhibiting Microglia Activation. Front Pharmacol. 2017;8:789 pubmed publisher
Yang Y, Qiu Y, Tang M, Wu Z, Hu W, Chen C. Expression and function of transforming growth factor‑β‑activated protein kinase 1 in gastric cancer. Mol Med Rep. 2017;16:3103-3110 pubmed publisher
Shen H, Li L, Yang S, Wang D, Zhou S, Chen X, et al. 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. 2017;16:2269-2273 pubmed publisher
van Caam A, Madej W, García de Vinuesa A, Goumans M, Ten Dijke P, Blaney Davidson E, et al. TGF?1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity. Arthritis Res Ther. 2017;19:112 pubmed publisher
Jaco I, Annibaldi A, Lalaoui N, Wilson R, Tenev T, Laurien L, et al. MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death. Mol Cell. 2017;66:698-710.e5 pubmed publisher
Jones D, Jenney A, Swantek J, Burke J, Lauffenburger D, Sorger P. Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. Nat Chem Biol. 2017;13:38-45 pubmed publisher
Ismail H, Didangelos A, Vincent T, Saklatvala J. Rapid Activation of Transforming Growth Factor ?-Activated Kinase 1 in Chondrocytes by Phosphorylation and K63 -Linked Polyubiquitination Upon Injury to Animal Articular Cartilage. Arthritis Rheumatol. 2017;69:565-575 pubmed publisher
Thamodaran V, Bruce A. p38 (Mapk14/11) occupies a regulatory node governing entry into primitive endoderm differentiation during preimplantation mouse embryo development. Open Biol. 2016;6: pubmed publisher
Kim M, Caplen N, Chakka S, Hernandez L, House C, Pongas G, et al. Identification of therapeutic targets applicable to clinical strategies in ovarian cancer. BMC Cancer. 2016;16:678 pubmed publisher
Ussher J, van Wilgenburg B, Hannaway R, Ruustal K, Phalora P, Kurioka A, et al. TLR signaling in human antigen-presenting cells regulates MR1-dependent activation of MAIT cells. Eur J Immunol. 2016;46:1600-14 pubmed publisher
Venna V, Benashski S, Chauhan A, McCullough L. Inhibition of glycogen synthase kinase-3β enhances cognitive recovery after stroke: the role of TAK1. Learn Mem. 2015;22:336-43 pubmed publisher
Kuk H, Hutchenreuther J, Murphy Marshman H, Carter D, Leask A. 5Z-7-Oxozeanol Inhibits the Effects of TGFβ1 on Human Gingival Fibroblasts. PLoS ONE. 2015;10:e0123689 pubmed publisher
Huang H, Chiang C, Hung W, Hou M. Targeting of TGF-β-activated protein kinase 1 inhibits chemokine (C-C motif) receptor 7 expression, tumor growth and metastasis in breast cancer. Oncotarget. 2015;6:995-1007 pubmed
Compan V, Martín Sánchez F, Baroja Mazo A, Lopez Castejon G, Gómez A, Verkhratsky A, et al. Apoptosis-associated speck-like protein containing a CARD forms specks but does not activate caspase-1 in the absence of NLRP3 during macrophage swelling. J Immunol. 2015;194:1261-73 pubmed publisher
Graham S, Wicher K, Jedrusik A, Guo G, Herath W, Robson P, et al. BMP signalling regulates the pre-implantation development of extra-embryonic cell lineages in the mouse embryo. Nat Commun. 2014;5:5667 pubmed publisher
Zhang Z, Li S, Zhang H, Wu Q, Gong J, Liang T, et al. Stabilization of ATF5 by TAK1-Nemo-like kinase critically regulates the interleukin-1β-stimulated C/EBP signaling pathway. Mol Cell Biol. 2015;35:778-88 pubmed publisher
Biesemann N, Mendler L, Wietelmann A, Hermann S, Schäfers M, Kruger M, et al. Myostatin regulates energy homeostasis in the heart and prevents heart failure. Circ Res. 2014;115:296-310 pubmed publisher
van Beuningen H, de Vries van Melle M, Vitters E, Schreurs W, van den Berg W, van Osch G, et al. Inhibition of TAK1 and/or JAK can rescue impaired chondrogenic differentiation of human mesenchymal stem cells in osteoarthritis-like conditions. Tissue Eng Part A. 2014;20:2243-52 pubmed publisher
Ansell S, Hodge L, Secreto F, Manske M, Braggio E, Price Troska T, et al. Activation of TAK1 by MYD88 L265P drives malignant B-cell Growth in non-Hodgkin lymphoma. Blood Cancer J. 2014;4:e183 pubmed publisher
Olsen K, Epa A, Kulkarni A, Kottmann R, McCarthy C, Johnson G, et al. Inhibition of transglutaminase 2, a novel target for pulmonary fibrosis, by two small electrophilic molecules. Am J Respir Cell Mol Biol. 2014;50:737-47 pubmed publisher
Choi H, Kim J, Do K, Park S, Moon Y. Prolonged NF-?B activation by a macrophage inhibitory cytokine 1-linked signal in enteropathogenic Escherichia coli-infected epithelial cells. Infect Immun. 2013;81:1860-9 pubmed publisher
Gatheral T, Reed D, Moreno L, Gough P, Votta B, Sehon C, et al. A key role for the endothelium in NOD1 mediated vascular inflammation: comparison to TLR4 responses. PLoS ONE. 2012;7:e42386 pubmed publisher
White B, Tarabishy S, Venna V, Manwani B, Benashski S, McCullough L, et al. Protection from cerebral ischemia by inhibition of TGFβ-activated kinase. Exp Neurol. 2012;237:238-45 pubmed publisher
Matta H, Gopalakrishnan R, Graham C, Tolani B, Khanna A, Yi H, et al. Kaposi's sarcoma associated herpesvirus encoded viral FLICE inhibitory protein K13 activates NF-κB pathway independent of TRAF6, TAK1 and LUBAC. PLoS ONE. 2012;7:e36601 pubmed publisher
Ahmed N, Zeng M, Sinha I, Polin L, Wei W, Rathinam C, et al. The E3 ligase Itch and deubiquitinase Cyld act together to regulate Tak1 and inflammation. Nat Immunol. 2011;12:1176-83 pubmed publisher
Morimoto R, Shindou H, Oda Y, Shimizu T. Phosphorylation of lysophosphatidylcholine acyltransferase 2 at Ser34 enhances platelet-activating factor production in endotoxin-stimulated macrophages. J Biol Chem. 2010;285:29857-62 pubmed publisher
product information
master code :
3604
SKU :
3604/1
product name :
(5Z)-7-Oxozeaenol
unit size :
1 mg
description :
Potent and selective TAK1 MAPKKK inhibitor
target :
Other Kinase Inhibitors
category :
Small Molecules
purity :
98%
observed molecular weight :
362.37
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
(5 Z )-7-Oxozeaenol is a resorcyclic lactone of fungal origin that acts as a potent and selective transforming growth factor- -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- B (IC50 = 83 nM) and JNK/p38. Inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF- -induced apoptosis in vitro .
top caption :
Potent and selective TAK1 MAPKKK inhibitor
extended description :
Potent and selective TAK1 MAPKKK inhibitor
chemical name text :
(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
formula :
C19H22O7
formula text :
C19H22O7
cas num :
253863-19-3
USD :
232 USD
product details :
Potent and selective TAK1 MAPKKK inhibitor
storage :
Desiccate at -20░C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK