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A cell-permeable benzoylthiourea compound that acts as a reversible inhibitor of class III HDAC sirtuins against SirT2 (IC50 = ~ 10 µM). Based on studies using the more soluble analog Tenovin-6, Tenovin-1 is expected not to compete with substrate binding and display lower potency against SirT1/3 (IC50 = 21/67 µM using Tenovin-6). Tenovin-1 (10 µM) up-regulates cellular p53 protein, but not mRNA, level in MCF-7 (≥6-fold in 6 h), presumably by blocking mdm2-mediated p53 degradation. Two day Tenovin-1 treatment (10 µM) results in selective killing of cancer cells with functional p53, but not p53-lacking cancer cells or normal human dermal fibroblasts. Despite its low aqueous solubility, administration of Tenovin-1 suspension is shown to effectively reduce BL2 and ARN8 xenographs in mice in vivo (≥50% reduction with 92 mg/kg, daily, i.p.).
Catalogue Number
580566
Brand Family
Calbiochem®
Synonyms
N-(4-tert-Butylbenzoyl)-Nʹ-(4-acetylaminophenyl)-thiourea, SIRT2 Inhibitor V
Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing. In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
Product Usage Statements
Storage and Shipping Information
Ship Code
Ambient Temperature Only
Toxicity
Standard Handling
Storage
+2°C to +8°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
19-April-2011 RFH
Synonyms
N-(4-tert-Butylbenzoyl)-Nʹ-(4-acetylaminophenyl)-thiourea, SIRT2 Inhibitor V
Description
A cell-permeable benzoylthiourea compound that acts as a reversible inhibitor of class III HDAC sirtuins (IC50 against SirT2 ~10 µM). Based on studies using the more soluble analog Tenovin-6, Tenovin-1 is expected not to compete with substrate binding and display lower potency against SirT1/3 (IC50 = 21/67 µM using Tenovin-6). Tenovin-1 (10 µM) up-regulates cellular p53 protein, but not mRNA, level in MCF-7 (≥6-fold in 6 h), presumably by blocking mdm2-mediated p53 degradation. Two day Tenovin-1 treatment (10 µM) results in selective killing of cancer cells with functional p53, but not p53-lacking cancer cells or normal human dermal fibroblasts. Despite its low aqueous solubility, administration of Tenovin-1 suspension is shown to effectively reduce BL2 and ARN8 xenographs in mice in vivo (≥50% reduction with 92 mg/kg daily i.p.).
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
380315-80-0
Chemical formula
C₂₀H₂₃N₃O₂S
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (5 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
