Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H23N3O2S |
Molecular Weight | 369.481 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=O)NC1=CC=C(NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C)C=C1
InChI
InChIKey=WOWJIWFCOPZFGV-UHFFFAOYSA-N
InChI=1S/C20H23N3O2S/c1-13(24)21-16-9-11-17(12-10-16)22-19(26)23-18(25)14-5-7-15(8-6-14)20(2,3)4/h5-12H,1-4H3,(H,21,24)(H2,22,23,25,26)
Molecular Formula | C20H23N3O2S |
Molecular Weight | 369.481 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18455128
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18455128
Tenovin-1 was discovered and characterized as a bioactive small-molecule activator of p53 that. It was shown, tenovin-1 inhibited the activities of human SirT1 and SirT2, two members of the NAD+-dependent class III histone deacetylases that also belong to the sirtuin family. At 10 µM, it elevates p53 expression in MCF-7 cells within two hours of treatment and longer-term exposure significantly decreases the growth of BL2 Burkitt’s lymphoma and ARN8 melanoma cells. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P04637|||Q16810|||Q3LRW5|||Q9NZD0 Gene ID: 7157.0 Gene Symbol: TP53 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/18455128 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18455128
Treatment of BL2 Burkitt's lymphoma cells expressing wild-type p53 with 10 μM tenovin-1 for 48 hr leads to more than 75% cell death. p53 levels in BL2 cells are increased by tenovin-1 (10 uM) and a 2 hr treatment with tenovin-1 (1, 2, 5 and 10 uM) followed by 4 days of incubation in the absence of compound is sufficient to decrease growth and kill the majority of these cells in culture.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:08:55 GMT 2023
by
admin
on
Sat Dec 16 10:08:55 GMT 2023
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Record UNII |
BIQ6AID2B7
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Record Status |
Validated (UNII)
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Record Version |
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
BINDING
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