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| | TENOVIN-1 Basic information |
| Product Name: | TENOVIN-1 | | Synonyms: | CS-571;TENOVIN-1;N-[[[4-(Acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide;N-[(4-acetaMidophenyl)carbaMothioyl]-4-tert-butylbenzaMide;Benzamide, N-[[[4-(acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)-;N-[[[4-(Acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide Tenovin 1;Tenovin 1 N-[[[4-(Acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide;Tenovin-1, >=98% | | CAS: | 380315-80-0 | | MF: | C20H23N3O2S | | MW: | 369.48 | | EINECS: | 200-256-5 | | Product Categories: | Inhibitor;Inhibitors | | Mol File: | 380315-80-0.mol |  |
| | TENOVIN-1 Chemical Properties |
| Melting point | >180°C (Subl.) | | density | 1.238±0.06 g/cm3(Predicted) | | storage temp. | Sealed in dry,Room Temperature | | solubility | Soluble in DMSO (10 mg/ml with warming) | | form | solid | | pka | 9.09±0.70(Predicted) | | color | White | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| RIDADR | 3077 | | HS Code | 29242990 |
| | TENOVIN-1 Usage And Synthesis |
| Description | Tenovin-1 is a small molecule activator of p53 transcriptional activity. 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. Functioning upstream of p53, tenovin-1 acts by inhibiting the deacetylase activity of purified human SIRT1 and SIRT2, members of NAD+-dependent class III histone deacetylases that belong to the sirtuin family. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo. | | Uses | Tenovin 1 is a sirtuin inhibitor. | | Definition | ChEBI: N-[(4-acetamidoanilino)-sulfanylidenemethyl]-4-tert-butylbenzamide is a member of thioureas. | | Biological Activity | p53 activator that protects against MDM2-mediated p53 degradation. Elevates levels of p53 and p21 CIP/WAF1 and induces expression from an endogenous p53-dependent promoter. Exhibits potent antiproliferative activity in vitro . | | References | Lain et al. (2008), Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator; Cancer Cell, 13 454
Sonnemann et al. (2014), p53-dependent and p53-independent anticancer effects of different histone deacetylase inhibitors; Br. J. Cancer 110 656
Nihal et al. (2014), SIRT1 is upregulated in cutaneous T-cell lymphoma, and its inhibition induces growth arrest and apoptosis; Cell Cycle 13 632
Wilking et al. (2014), SIRT1 deacetylase is overexpressed in human melanoma and its small molecule inhibition imparts anti-proliferative response via p53 activation; Arch. Biochem. Biophys. 563 94
Marx et al. (2018), The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death in a p53 null Ewing’s sarcoma cell line; New Drugs 36 396
Bang et al. (2019), Tenovin-1 Induces Senescence and Decreases Wound-Healing Activity in Cultured Rat Primary Astrocytes; Biomol. Ther. (Seoul) 27 283 |
| | TENOVIN-1 Preparation Products And Raw materials |
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