IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT.
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免费溶解
产品名称 | DUB ↓ ↑ | UCH ↓ ↑ | USP/UBP ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PR-619 |
+
Plpro, EC50: 14.2 μM |
+++
UCH-L3, EC50: 2.95 μM UCH-L5, EC50: 12.8 μM |
+++
USP5, EC50: 4.90 μM USP28, EC50: 6.24 μM |
99%+ | |||||||||||||||
Degrasyn | ✔ | Bcr-Abl | 98+% | ||||||||||||||||
VLX1570 |
+
DUB, IC50: ~10 μM |
99%+ | |||||||||||||||||
ML-323 |
++++
USP1-UAF1, IC50: 76 nM |
99%+ | |||||||||||||||||
LDN-57444 |
++++
UCH-L3, IC50: 25 μM UCH-L1, IC50: 0.4 μM |
99%+ | |||||||||||||||||
TCID |
++++
UCH-L3, IC50: 0.6 μM |
98% | |||||||||||||||||
b-AP15 |
+++
UCHL5, IC50: 2.1 μM |
98% | |||||||||||||||||
P 22077 |
++
USP47, EC50: 8.74 μM USP7, IC50: 8.6 μM |
99%+ | |||||||||||||||||
P005091 |
++
USP47, IC50: 4.3 μM USP7, EC50: 4.2 μM |
99+% | |||||||||||||||||
IU1 |
++
USP14, IC50: 4.7 μM |
98% | |||||||||||||||||
NSC632839 |
+
USP2, EC50: 45 μM USP7, EC50: 37 μM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Usp14, a proteasome-associated deubiquitinating enzyme, can impede the degradation of ubiquitin-protein conjugates, both in vivo and in vitro. IU1 inhibits the catalytic activity of proteasome-associated Usp14 in vitro, with an IC50 of 4-5 μM. IU1 specifically binds to the activated form of Usp14 and may inhibit it by preventing its docking on the proteasome. However, direct tests of this scenario yielded negative results. Usp14 inhibition is rapidly established upon IU1 addition and rapidly reversed upon its removal. IU1 also promotes the degradation of Sic1, a CDK inhibitor from S. cerevisiae [1]. |
体外研究 | Usp14, a proteasome-associated deubiquitinating enzyme, can impede the degradation of ubiquitin-protein conjugates, both in vivo and in vitro. IU1 inhibits the catalytic activity of proteasome-associated Usp14 in vitro, with an IC50 of 4-5 μM. IU1 specifically binds to the activated form of Usp14 and may inhibit it by preventing its docking on the proteasome. However, direct tests of this scenario yielded negative results. Usp14 inhibition is rapidly established upon IU1 addition and rapidly reversed upon its removal. IU1 also promotes the degradation of Sic1, a CDK inhibitor from S. cerevisiae [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.33mL 0.67mL 0.33mL |
16.65mL 3.33mL 1.66mL |
33.29mL 6.66mL 3.33mL |
CAS号 | 314245-33-5 |
分子式 | C18H21FN2O |
分子量 | 300.371 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 40 mg/mL(133.17 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |