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Submit ReviewCMPD-1 is a non-ATP-competitive, selective inhibitor of p38α-mediated MK2a (mitogen-activated protein kinase-2a) phosphorylation (apparent Ki = 330 nM). Does not inhibit p38α-mediated phosphorylation of MBP and ATF-2. Also tubulin polymerization inhibitor. Cytotoxic in glioblastoma cells at concentrations that do not affect the MK2 pathway.
CMPD-1 is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 349.4 |
Formula | C22H20FNO2 |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 41179-33-3 |
PubChem ID | 11382492 |
InChI Key | ODYAQBDIXCVKAE-UHFFFAOYSA-N |
Smiles | OC1=CC=C(NC(=O)CCCC2=CC=C(C=C2)C2=CC=CC=C2F)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 34.94 | 100 | |
ethanol | 34.94 | 100 |
The following data is based on the product molecular weight 349.4. 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.86 mL | 14.31 mL | 28.62 mL |
5 mM | 0.57 mL | 2.86 mL | 5.72 mL |
10 mM | 0.29 mL | 1.43 mL | 2.86 mL |
50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
References are publications that support the biological activity of the product.
Davidson et al (2004) Discovery and characterisation of a substrate selective p38α inhibitor. Biochemistry 43 11658 PMID: 15362850
Gurgis et al (2015) Cytotoxic activity of the MK2 inhibitor CMPD1 in glioblastoma cells is independent of MK2. Cell Death Discovery 1 15028
If you know of a relevant reference for CMPD-1, please let us know.
Keywords: CMPD-1, CMPD-1 supplier, Non-ATP-competitive, p38α, p38alpha, inhibitors, inhibits, Mitogen-Activated, Protein, Kinase, p38, MAPK, Kinases, Signaling, Signalling, Microtubules, MK2, 2186, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for CMPD-1 include:
Ryals et al (2018) The Inner Ear Heat Shock Transcriptional Signature Identifies Compounds That Protect Against Aminoglycoside Ototoxicity. Front Cell Neurosci 12 445 PMID: 30532693
Breindel et al (2013) EGF receptor activates MET through MAPK to enhance non-small cell lung carcinoma invasion and brain metastasis. Cancer Res 73 5053 PMID: 23794705
Fricke et al (2013) p38 and OGT sequestration into viral inclusion bodies in cells infected with human respiratory syncytial virus suppresses MK2 activities and stress granule assembly. J Virol 87 1333 PMID: 23152511
Do you know of a great paper that uses CMPD-1 from Tocris? Please let us know.
Average Rating: 4 (Based on 1 Review.)
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Zebrafish larvae were placed into 48-well plates and used the DASPEI screen by 42 perturbagens drugs, including this compound
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.