In vitro: Thiomyristoyl(TM) is a highly selective SIRT2 inhibitor. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7. In vitro, it shows great inhibition of cell viability and its cytotoxicity is relatively selective toward cancer cells. TM decreases c-Myc oncoprotein level in cancer cells, the ability of TM to decrease c-Myc abundance in different cell lines correlates with the sensitivity of the cell lines to TM. In vivo: The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM has limited effects on non-cancerous cells and tumor-free mice.
J Clin Invest. 2023 Jun 15;133(12):e158978.
An allosteric inhibitor of sirtuin 2 deacetylase activity exhibits broad-spectrum antiviral activity
Thiomyristoyl purchased from AbMole
Cell Experiment | |
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Cell lines | breast cancer cell lines MCF-7 |
Preparation method | Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control. |
Concentrations | 1, 5, 10, 25, 50 μM |
Incubation time | 6 h |
Animal Experiment | |
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Animal models | Mouse xenograft model |
Formulation | DMSO |
Dosages | 1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT) |
Administration | intraperitoneal (IP) or intra-tumor (IT) injections |
Molecular Weight | 581.85 |
Formula | C34H51N3O3S |
CAS Number | 1429749-41-6 |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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