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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Proteasome-RA190
RA190

Chemical Structure : RA190

CAS No.: 1617495-03-0

RA190 (RA-190, RA 190)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 596.7594
分子式 C28H23Cl5N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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)

参考文献

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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