OSS-128167 proves to be a selective compounds toward SIRT6, its IC50 values toward SIRT1 and SIRT2 being approximately 20 times higher. It is cell permeable and active in cultured cells.
OSS-128167 increases H3K9 acetylation and GLUT-1 expression. OSS_128167 effectively blunts phorbol myristate acetate (PMA)-induced TNF-α secretion in cultured BxPC-3 cells. OSS_128167 increases glucose uptake in cells. OSS_128167 (200 μM) induces chemosensitization in primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines.
In vivo, OSS_128167 (50 mg/kg; intraperitoneal injection; every 4 days; for 12 days; male HBV transgenic mice) treatment markedly suppresses the level of HBV DNA and 3.5-Kb RNA in HBV transgenic mice.
Heliyon. 2024 Feb 1;158835.
Inhibition of SIRT6 aggravates p53-mediated ferroptosis in acute lung injury in mice
OSS_128167 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | BxPC3 cells |
| Preparation method | 4 × 10^5 BxPC3 cells are plated in six-well plates and allowed to adhere for 24 h. There after, cells are stimulated with 100 μM OSS-128167 or the respective amounts of vehicle DMSO for the indicated time amounts. Finally, cells are used for protein lysate generation, and total H3 and acetylated H3K9 levels are detected by immunoblotting. |
| Concentrations | 100 μM |
| Incubation time | 0, 2, 6, 18, 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 366.32 |
| Formula | C19H14N2O6 |
| CAS Number | 887686-02-4 |
| Solubility (25°C) | DMSO 80 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.
[2] Parenti MD, et al. J Med Chem. Discovery of novel and selective SIRT6 inhibitors.
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