401011 Sigma-AldrichHypothemycin - CAS 76958-67-3 - Calbiochem
A cell-permeable cis-enone resorlic acid lactone (RAL) and (5Z)-7-Oxozeaenol analog that inhibits several kinases via an initial affinity binding to the ATP pocket.
More>> A cell-permeable cis-enone resorlic acid lactone (RAL) and (5Z)-7-Oxozeaenol analog that inhibits several kinases via an initial affinity binding to the ATP pocket. Less<<Synonyms: NSC 354462
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Overview
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Key Specifications Table
CAS # | Empirical Formula |
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76958-67-3 | C₁₉H₂₂O₈ |
Description | |
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Overview | A cell-permeable cis-enone resorlic acid lactone (RAL) and (5Z)-7-Oxozeaenol (Cat. No. 499610) analog that inhibits several kinases via an initial affinity binding to the ATP pocket, followed by a covalent adduct formation with a conserved ATP site cysteine residue of the targeted enzymes, including, but not limited to, Flt1/VEGFR-1, Flt3, cKit(D816V), MAPK1, MAPK2, MEK1, MKK6, PKCμ, PKD2, PRAK, and Tak1 (≥90% inhibition at 2 µM). Hypothemycin is also reported to inhibit two non-RAL targets (99% and 82% inhibition of TrkA and TrkB, respectively, at 2 µM), while one of the 46 putative cis-enone RALs targets, namely GSK-3α, is shown not to be affected. Hypothemycin inhibits multiple kinases involved in MAP kinase pathways and is therefore particularly effective in inhibiting BRAF(V600E)-dependent tumor growth. (5Z)-Zeaenol (Cat. No. 499609) may serve as a negative control. |
Catalogue Number | 401011 |
Brand Family | Calbiochem® |
Synonyms | NSC 354462 |
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References | Schirmer, A., et al. 2006. Proc. Natl. Acad. Sci. USA 103, 4234. Solit, D.B., et al. 2006. Nature 439, 358. Tanaka, H., et al. 1999. Jpn. J. Cancer Res. 90, 1139. |
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CAS number | 76958-67-3 |
Form | Lyophilized solid |
Hill Formula | C₁₉H₂₂O₈ |
Chemical formula | C₁₉H₂₂O₈ |
Structure formula Image | |
Quality Level | MQ100 |
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Purity | ≥97% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Catalog Number | GTIN |
401011 | 0 |
Documentation
Hypothemycin - CAS 76958-67-3 - Calbiochem SDS
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Hypothemycin - CAS 76958-67-3 - Calbiochem Certificates of Analysis
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401011 |
References
Reference overview |
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Schirmer, A., et al. 2006. Proc. Natl. Acad. Sci. USA 103, 4234. Solit, D.B., et al. 2006. Nature 439, 358. Tanaka, H., et al. 1999. Jpn. J. Cancer Res. 90, 1139. |