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Home - Products - Proteasome/Ubiquitin - Proteasome - RA190

RA190

CAS No. 1617495-03-0

RA190( RA-190 | RA 190 )

Catalog No. M12365 CAS No. 1617495-03-0

RA190 (RA-190)?is a reversible, highly selective, orally active inhibitor of the proteasomal ubiquitin receptor Rpn13.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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10MG 154 Get Quote
25MG 232 Get Quote
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Biological Information

  • Product Name
    RA190
  • Note
    Research use only, not for human use.
  • Brief Description
    RA190 (RA-190)?is a reversible, highly selective, orally active inhibitor of the proteasomal ubiquitin receptor Rpn13.
  • Description
    RA190 (RA-190)?is a reversible, highly selective, orally active inhibitor of the proteasomal ubiquitin receptor Rpn13, exhibits potent anti-proliferative effects against MM lines (IC50<0.1 uM) and HPV-transformed cells (IC50<0.3 uM); inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins; profoundly reduced growth of MM and ovarian cancer xenografts.
  • 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.
  • Synonyms
    RA-190 | RA 190
  • Pathway
    Proteasome/Ubiquitin
  • Target
    Proteasome
  • Recptor
    Proteasome
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1617495-03-0
  • Formula Weight
    596.7594
  • Molecular Formula
    C28H23Cl5N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 10 mM
  • SMILES
    C1C(=CC2=CC(=C(C=C2)Cl)Cl)C(=O)C(=CC3=CC(=C(C=C3)Cl)Cl)CN1C(=O)C(CC4=CC=CC=C4)N.Cl
  • Chemical Name
    4-Piperidinone, 1-[(2S)-2-amino-1-oxo-3-phenylpropyl]-3,5-bis[(3,4-dichlorophenyl)methylene]-, hydrochloride (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Anchoori RK, et al. Cancer Cell. 2013 Dec 9;24(6):791-805. 2. Randles L, et al. J Biol Chem. 2016 Apr 15;291(16):8773-83. 3. Song Y, et al. Leukemia. 2016 Sep;30(9):1877-86.
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