Cat. No. 2731
Chemical Name: N3-(4-Fluorophenyl)-1H-pyrazolo-[3,
Biological ActivityInhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) (IC50 = 2.2 μM) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases. Blocks phosphorylation of eIF4E in cellular assays (IC50 = 3 μM) and inhibits LPS-induced TNFα expression in macrophages.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Andersson and Sundler (2006) Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 33 52. PMID: 16431125.
Ishida et al (2003) Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ.Res. 93 1218. PMID: 14605021.
Knauf et al (2001) Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol.Cell.Biol. 21 5500. PMID: 11463832.
If you know of a relevant reference for CGP 57380 please let us know.
Citations are publications that use Tocris products. Selected citations for CGP 57380 include:
Royall et al (2015) Murine norovirus 1 (MNV1) replication induces translational control of the host by regulating eIF4E activity during infection. Neurochem Res 290 4748. PMID: 25561727.
Brown et al (2014) Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis. J Biol Chem 88 13149. PMID: 25187540.
Melemedjian et al (2010) IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex. J Neurosci 30 15113. PMID: 21068317.
Do you know of a great paper that uses CGP 57380 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: CGP 57380, supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Tocris Bioscience, Mnk Inhibitor products
Find multiple products by catalog number
New Products in this Area
ATP-competitive inhibitor of DAPK and ZIPKst-Ht31 P
Negative control for st-Ht31 (Cat. No. 6286)st-Ht31
Inhibits PKA/AKAP interactions; cell permeableP21d hydrochloride
Potent and selective Brk inhibitorCVT 313
High affinity PKC activator; also APP modulatorJH 295
Irreversible Nek2 inhibitorOXSI 2
Potent Syk kinase inhibitor; also inhibits assembly of NLRP3 inflammasomesSTK16-IN-1
Serine/threonine protein kinase 16 (STK16) inhibitor; also inhibits PI 3Kδ, PI 3Kγ and mTOR kinases.AZ PFKFB3 26
Potent and selective PFKFB3 inhibitorNCL 00017509
Potent and reversible NIMA related kinase 2 (Nek2) inhibitorXMD 8-87
Potent Ack1/TNK2 inhibitorSKI 178
Non-lipid sphingosine kinase 1 (SphK1) inhibitorML 315 hydrochloride
Inhibitor of Clk and DYRK kinasesEverolimus
mTOR inhibitor;immunosuppressantPKI (5-24)
High affinity PKA inhibitorTDZD 8
Selective non-ATP competitive inhibitor of GSK 3βBI 605906
Selective IKKβ inhibitorGSK 319347A
Potent and selective IKKε inhibitorFRAX 597
Potent group I PAK inhibitorMRT 68921 dihydrochloride
Potent ULK inhibitor; inhibits autophagyAM 2394
Potent glucokinase activator; orally bioavailableeCF 309
Potent mTOR inhibitor
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.