| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Serine/threonine-protein kinase B-raf [410-766,V600E] |
|---|
| Ligand | BDBM16673 |
|---|
| Substrate/Competitor | Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) |
|---|
| Meas. Tech. | RAF Kinase Assay |
|---|
| pH | 8.2±n/a |
|---|
| Temperature | 305.15±n/a K |
|---|
| IC50 | 38±9 nM |
|---|
| Citation |  Wilhelm, SM; Carter, C; Tang, L; Wilkie, D; McNabola, A; Rong, H; Chen, C; Zhang, X; Vincent, P; McHugh, M; Cao, Y; Shujath, J; Gawlak, S; Eveleigh, D; Rowley, B; Liu, L; Adnane, L; Lynch, M; Auclair, D; Taylor, I; Gedrich, R; Voznesensky, A; Riedl, B; Post, LE; Bollag, G; Trail, PA BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res64:7099-109 (2004) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Serine/threonine-protein kinase B-raf [410-766,V600E] |
|---|
| Name: | Serine/threonine-protein kinase B-raf [410-766,V600E] |
|---|
| Synonyms: | B-Raf Protein Kinase Mutant (V599E) | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF | BRAF1 | BRAF_HUMAN | RAFB1 | p94 | v-Raf murine sarcoma viral oncogene homolog B1 |
|---|
| Type: | COOH-terminal kinase domain |
|---|
| Mol. Mass.: | 40318.46 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Recombinant baculoviruses expressing V599E B-RAF (residues 409-765) was purified as a fusion protein. |
|---|
| Residue: | 357 |
|---|
| Sequence: | LTNVKALQKSPGPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFG
TVYKGKWHGDVAVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVT
QWCEGSSLYHHLHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLT
VKIGDFGLATEKSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYEL
MTGQLPYSNINNRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQ
ILASIELLARSLPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
|
|
|
|---|
| BDBM16673 |
|---|
| Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) |
|---|
| Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
|---|
| Synonyms: | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2 |
|---|
| Type: | Other Protein Type |
|---|
| Mol. Mass.: | 43439.03 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates. |
|---|
| Residue: | 393 |
|---|
| Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
|
|
|
|---|
Search and Browse
