Salinosporamide A (NPI-0052, Marizomib) is a novel marine derived proteasome inhibitor which inhibits CT-L, C-L, and T-L proteasome activities in human erythrocyte-derived 20S proteasomes with EC50 of 3.5 nM, 430 nM, 28 nM.
| Molecular Weight | 313.78 |
| Formula | C15H20ClNO4 |
| CAS Number | 437742-34-2 |
| Solubility (25°C) | DMSO >100 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] Hadi Gholami, et al. Total Synthesis of (-)-Salinosporamide A via a Late Stage C-H Insertion
[3] Lo B Marx, et al. A Total Synthesis of Salinosporamide A
[5] Masakatsu Shibasaki, et al. Total synthesis of lactacystin and salinosporamide A
| Related Proteasome Products |
|---|
| NIC-0102
NIC-0102 is an orally potent proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammasome activation.NIC-0102 showed potent anti-inflammatory effects in vivo in a DSS-induced ulcerative colitis model. In addition, NIC-0102 inhibited the production of pro-IL-1β. |
| Ac-WLA-AMC
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate. |
| Ac-Nle-Pro-Nle-Asp-AMC
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. |
| PR-39
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. |
| PSI
PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. |
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