产品信息
抗原名称
E1_E2_E3 Enzyme
商品描述
PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 uM, with no or little activity at E2.
分子量
371.3
纯度
>98%
可溶性
DMSO 74 mg/mL (199.29 mM)
外观
Powder
In vitro(体外研究)
PYR-41 increases total sumoylation in cells in addition to blocking ubiquitylation. PYR-41 attenuates cytokine-mediated nuclear factor-κB activation. PYR-41 also prevents the downstream ubiquitylation and proteasomal degradation of IκBα. Furthermore, PYR-41 inhibits degradation of p53 and activates the transcriptional activity of this tumor suppressor. PYR-41 (50 μM) promotes accumulation of ubiquitinated proteins. PYR-41 causes a concentration-dependent (10-50 μM) decline in DUB activity in Z138 cells after 4 h. PYR-41 potently inhibits USP5 DUB activity, even at the lowest concentration (10 μM). PYR-41 potently (10-50 μM) inhibits the activity of various DUBs, determined to represent USP9x, USP5, USP14, UCH37 and UCH-L3. Co-treatment of Z138 cells with DTT and PYR-41 completely abolishes the accumulation of ubiquitinated proteins.
背景
别名
PYR41; PYR-41
分子式
C17H13N3O7
CAS号
418805-02-4
制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
参考图片
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