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RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. RA190 treatment inhibits proteasome function, causing rapid accumulation of polyubiquitinated proteins. RA190 has therapeutic activity in a xenograft model, and with sorafenib exhibited synergetic killing of HCC cells in vitro. In vivo, RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancer xenografts, and oral RA190 treatment retards HPV16+ syngeneic mouse tumor growth, without impacting spontaneous HPV-specific CD8+ T cell responses.
| Molecular Weight | 596.76 |
| Formula | C28H23Cl5N2O2 |
| CAS Number | 1617495-03-0 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Proteasome Products |
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Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. |
| 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. |
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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. |
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