Product Name: MskSubtide
Product Number: PE-01BIH75
Size: | 200 µg | | Price: | 10.00 |
| 1 mg | | $US | 20.00 |
| 5 mg | | | 48.00 |
Peptide Name: MskSubtide
Product Use: For assaying the phosphotransferase activity of Mitogen & stress-activated protein-serine kinase 1; Ribosomal protein S6 kinase alpha 5 (UniProt ID O75582).
Peptide Production Method: Solid-phase peptide synthesis
Peptide Sequence: RLFRRMSFCFFG
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: βAla-Cys
Peptide Molecular Mass Calculated: 1740.16 Da
Peptide Purity Percent after Synthesis and Purification: >50
Peptide Appearance: White powder
Peptide Form: Solid
Storage Conditions: -20°C
Peptide Recommended Enzyme: Msk
Scientific Background: MSK1 (RPS6KA5) is a protein-serine/threonine kinase of the AGC group and RSK family. It is required for the mitogen (e.g. epidermal growth factor) or stress-induce d(e.g. UV-C irradiation, anisomycin) phosphorylation of the transcription factors CREB1 and ATF1 and for the regulation of the transcription factors RELA, STAT3 and ETV1/ER81, and that contributes to gene activation by histone phosphorylation and functions in the regulation of inflammatory genes. It plays an essential role in the control of RELA transcriptional activity in response to TNF and upon glucocorticoid, associates in the cytoplasm with the glucocorticoid receptor NR3C1 and contributes to RELA inhibition and repression of inflammatory gene expression. In skeletal myoblasts is required for phosphorylation of RELA at S276 during oxidative stress. In erythropoietin-stimulated cells, is necessary for the S727 phosphorylation of STAT3 and regulation of its transcriptional potential.It phosphorylates ETV1/ER81 at S191 and S216, and thereby regulates its ability to stimulate transcription, which may be important during development and breast tumour formation. It directly represses transcription via phosphorylation of S1 of histone H2A. It phosphorylates S10 of histone H3 in response to mitogenics, stress stimuli and EGF, which results in the transcriptional activation of several immediate early genes, including proto-oncogenes c-fos/FOS and c-jun/JUN. It may also phosphorylate S28 of histone H3. It mediates the mitogen- and stress-induced phosphorylation of high mobility group protein 1 (HMGN1/HMG14). In lipopolysaccharide-stimulated primary macrophages, acts downstream of the Toll-like receptor TLR4 to limit the production of pro-inflammatory cytokines. MSK1 functions probably by inducing transcription of the MAP kinase phosphatase DUSP1 and the anti-inflammatory cytokine interleukin 10 (IL10), via CREB1 and ATF1 transcription factors. MSK1 is activated by phosphorylation at S212, S360, S376, T581 and T700. PMA or UV-C induced kinase phosphotransferase activity can be reduced 60% with a S360A mutation, plus a T700A/D can lead to decreased phosphorylation of T581. Kinase phosphotransferase activity can also be lost either with a S376A mutation, leading to decreased phosphorylation of the S60 and T581 residues, or with a T581A mutation leading to decreased phosphorylation of S212, S376, or S381. Aberrant activation of members of the MSK1 family have found to be linked with many human diseases, such as breast and prostate cancers.