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RA190

CAS No. : 1617495-03-0

MCE 国际站：RA190

产品活性：RA190是双亚苄基哌啶，通过与泛素受体RPN13的半胱氨酸88共价结合来抑制蛋白酶体功能。

研究领域：Metabolic Enzyme/Protease

作用靶点：Proteasome

In Vitro: RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, even those resistant to bortezomib, are sensitive to RA190 via endoplasmic reticulum stress-related apoptosis. RA190 stabilizes targets of human papillomavirus (HPV) E6 oncoprotein, and preferentially kills HPV-transformed cells.

In Vivo: RA190 distributes to plasma and major organs excepting brain, and inhibits proteasome function in skin and muscle. 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.

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