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NSC 687852(b-AP15)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NSC 687852(b-AP15)图片
CAS NO:1009817-63-3
规格:98%
分子量:419.39
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
19S regulatory particle Inhibitor
CAS:1009817-63-3
分子式:C22H17N3O6
分子量:419.39
纯度:98%
存储:Store at -20°C

Background:

IC50: N/A


NSC 687852 is a 19S regulatory particle inhibitor.


The 19S particles bind polyubiquitin-linked polypeptides and present them to the 20S degradative units. USP14 and UCHL5 are cysteine enzymes that become activated after being associated with the proteasome.


In vitro: NSC 687852 blocked deubiquitylating activity of USP14 and UCHL5 selectively without inhibiting proteasome activity. NSC 687852 decreased viability in multiple myeloma (MM) cell lines and patient MM cells, inhibited MM cell proliferation even in the presence of bone marrow stroma cells, and overcomed bortezomib resistance. Anti-MM activity of NSC 687852 was associated with growth arrest through downregulating CDC2, CDC25C, and cyclin B1, as well as induction of caspase-dependent apoptosis and activation of unfolded protein response [1].


In vivo: In vivo studies using distinct human MM xenograft models showed that NSC 687852 was well tolerated, inhibited tumor growth, and prolonged mouse survival. Combination of NSC 687852 with suberoylanilide hydroxamic acid, lenalidomide, or dexamethasone was found to induce synergistic anti-MM activity [1].


Clinical trial: N/A


Reference:
[1] Ze Tian,Padraig D'Arcy,Xin Wang,Arghya Ray,Yu-Tzu Tai,Yiguo Hu,Ruben D Carrasco,Paul Richardson,Stig Linder,Dharminder Chauhan,Kenneth C Anderson.  A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood. 2014 Jan 30; 123(5): 706–716.