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RA190

Chemical Structure : RA190

CAS No.: 1617495-03-0

RA190 (RA-190, RA 190)

Catalog No.: PC-42242Not For Human Use, Lab Use Only.

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).

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Biological Activity

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).
RA190 is a bis-benzylidine piperidone that covalently binds to Cys 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function.
RA190 inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins.
RA190 profoundly reduced growth of MM and ovarian cancer xenografts.

Physicochemical Properties

M.Wt 596.7594
Formula C28H23Cl5N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 10 mM

Chemical Name/SMILES

4-Piperidinone, 1-[(2S)-2-amino-1-oxo-3-phenylpropyl]-3,5-bis[(3,4-dichlorophenyl)methylene]-, hydrochloride (1:1)

References

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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