Reaction Details |
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Target | MAP kinase-activated protein kinase 2 [41-364] |
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Ligand | BDBM30225 |
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Substrate/Competitor | Biotinylated GST-LSP1 |
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Meas. Tech. | Dissociation-Enhanced Lanthanide Fluorescent Immunoassay (DELFIA) |
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pH | 7.6±n/a |
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Temperature | 298.15±n/a K |
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IC50 | 820±260 nM |
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Citation | Wu, JP; Wang, J; Abeywardane, A; Andersen, D; Emmanuel, M; Gautschi, E; Goldberg, DR; Kashem, MA; Lukas, S; Mao, W; Martin, L; Morwick, T; Moss, N; Pargellis, C; Patel, UR; Patnaude, L; Peet, GW; Skow, D; Snow, RJ; Ward, Y; Werneburg, B; White, A The discovery of carboline analogs as potent MAPKAP-K2 inhibitors. Bioorg Med Chem Lett17:4664-9 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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MAP kinase-activated protein kinase 2 [41-364] |
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Name: | MAP kinase-activated protein kinase 2 [41-364] |
Synonyms: | MAPK-Activated Protein Kinase 2 (MK2) | MAPK2_HUMAN | MAPKAP kinase 2 | MAPKAPK-2 | MAPKAPK2 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 37477.48 |
Organism: | Homo sapiens (Human) |
Description: | MK2 was activated with p38alpha MAPK and re-purified by GSH affinity chromatography. |
Residue: | 324 |
Sequence: | QQFPQFHVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPK
ARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTE
REASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSL
TTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIR
MGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSR
VLKEDKERWEDVKEEMTSALATMR
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BDBM30225 |
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Biotinylated GST-LSP1 |
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Name: | Biotinylated GST-LSP1 |
Synonyms: | lymphocyte-specific protein 1 |
Type: | Other Protein Type |
Mol. Mass.: | 17410.08 |
Organism: | n/a |
Description: | The GST-LSP1 179-339 substrate of MK2 was biotinylated with a 70-fold molar excess of PEO-iodoacetyl biotin (Pierce), followed by quenching with excess DTT and purification by Sephadex G-25 gel filtration. |
Residue: | 161 |
Sequence: | LVLEGTIEQSSPPLSPTTKLIDRTESLNRSIEKSNSVKKSQPDLPISKIDQWLEQYTQAI
ETAGRTPKLARQASIELPSMAVASTKSRWETGEVQAQSAAKTPSCKDIVAGDMSKKSLWE
QKGGSKTSSTIKSTPSGKRYKFVATGHGKYEKVLVEGGPAP
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