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IU1 {[allProObj[0].p_purity_real_show]}

货号:A875547

IU1是一种细胞可渗透的、可逆的、选择性的蛋白酶体抑制剂,针对人类USP14,IC50为4.7 μM,对IsoT具有25倍的选择性。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
IU1 化学结构 CAS号:314245-33-5
IU1 化学结构
CAS号:314245-33-5
IU1 3D分子结构
CAS号:314245-33-5
IU1 化学结构 CAS号:314245-33-5
IU1 3D分子结构 CAS号:314245-33-5
规格 价格 会员价 库存 数量
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IU1 纯度/质量文件 产品仅供科研

货号:A875547 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DUB UCH USP/UBP 其他靶点 纯度
PR-619 +

Plpro, EC50: 14.2 μM

+++

UCH-L5, EC50: 12.8 μM

UCH-L3, EC50: 2.95 μM

+++

USP5, EC50: 4.90 μM

USP28, EC50: 6.24 μM

99%+
Degrasyn Bcr-Abl 99+%
VLX1570 +

DUB, IC50: ~10 μM

99%+
ML-323 ++++

USP1-UAF1, IC50: 76 nM

99%+
LDN-57444 ++++

UCH-L1, IC50: 0.4 μM

UCH-L3, IC50: 25 μM

99%+
TCID ++++

UCH-L3, IC50: 0.6 μM

98%
b-AP15 +++

UCHL5, IC50: 2.1 μM

98%
P 22077 ++

USP7, IC50: 8.6 μM

USP47, EC50: 8.74 μM

99%+
P005091 ++

USP7, EC50: 4.2 μM

USP47, IC50: 4.3 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 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
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。

IU1 生物活性

靶点
  • USP/UBP

    USP14, IC50:4.7 μM

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].

IU1 细胞实验

Cell Line
Concentration Treated Time Description References
USP14CAT 5 mM 1 hour To evaluate the inhibitory effect of IU1 on USP14, results showed that IU1 inhibits USP14 activity by preventing substrate binding. Cell Res. 2018 Dec;28(12):1186-1194.
CAD5 cells 50 µM 16 hours To test whether IU1 could facilitate the clearance of polyubiquitinated substrates, results showed that IU1 treatment reduced the load of polyubiquitinated conjugates and PrPSc. Acta Neuropathol. 2016 Mar;131(3):411-25.
GSC83 cells 25 µM 2 days To evaluate the effect of IU1 on GSC83 cells, results showed that IU1 significantly downregulated ALDH1A3 expression and upregulated Tuj1 expression, leading to a reduction in GSC properties Theranostics. 2025 Jan 13;15(6):2293-2314.
GSC83 cells 20 µM 24 hours To evaluate the effect of IU1 on ALKBH5 protein levels, results showed that IU1 significantly reduced ALKBH5 protein levels Theranostics. 2025 Jan 13;15(6):2293-2314.
HeLa cells 0.1, 0.2, 0.5, 1, 2, 5, 10, 20, 50, 100 µM 24 hours IU1 significantly inhibited the proliferation of HeLa cells in a dose-dependent manner. Int J Biol Sci. 2020 Sep 16;16(15):2951-2963.
SiHa cells 0.1, 0.5, 2, 5, 10, 20, 50, 100 µM 24 hours IU1 significantly inhibited the proliferation of SiHa cells in a dose-dependent manner. Int J Biol Sci. 2020 Sep 16;16(15):2951-2963.
KGN cells 50 µM 24 hours Reduced ETO-induced DNA damage, promoted DDR function, and inhibited cell senescence J Transl Med. 2024 Sep 11;22(1):834.
HCCLM3 cells 50 µM 24 or 48 hours To assess the effect of IU1 on cell proliferation, results showed that 50 μM IU1 significantly reduced cell viability Cell Death Dis. 2021 Aug 21;12(9):803.
MDA-MB453 75 µM 48 hours To evaluate the effect of IU1 combined with enzalutamide on breast cancer cell proliferation and apoptosis, results showed that the combination significantly enhanced cell growth inhibition and apoptosis induction. J Exp Clin Cancer Res. 2019 May 24;38(1):220.
MCF-7 75 µM 48 hours To evaluate the effect of IU1 combined with enzalutamide on breast cancer cell proliferation and apoptosis, results showed that the combination significantly enhanced cell growth inhibition and apoptosis induction. J Exp Clin Cancer Res. 2019 May 24;38(1):220.
Huh-7 cells 50 and 100 µM To assess the effect of IU1 on cell migration and invasion, results showed that 50 and 100 μM IU1 significantly inhibited cell migration and invasion Cell Death Dis. 2021 Aug 21;12(9):803.

IU1 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Athymic Nude mice Brain tumor xenograft model Intraperitoneal injection 25 μM Once daily, continuous treatment To evaluate the effect of IU1 on brain tumor xenograft models, results showed that IU1 significantly enhanced the cytotoxic effects of radiotherapy, significantly increasing survival rates Theranostics. 2025 Jan 13;15(6):2293-2314.
BALB/c Nude mice Subcutaneous xenograft and liver metastasis models Intragastric administration 40 mg/kg Every three days until the end of the experiment IU1 administration inhibited tumour growth, reduced the expression of TAZ and Ki-67, decreased liver micrometastases, and improved survival rate. Cell Death Differ. 2023 Jan;30(1):1-15.
Nude mice HCCLM3 cell xenograft model Oral 40 mg/kg Every two days for 14 days To assess the effect of IU1 on tumor growth, results showed that IU1 significantly inhibited tumor growth Cell Death Dis. 2021 Aug 21;12(9):803.
Mice D-galactose-induced POI model Intraperitoneal injection 40 mg/kg Once daily for 6 weeks Improved D-gal-induced ovarian function decline, reduced DNA damage and cell senescence J Transl Med. 2024 Sep 11;22(1):834.
BALB/c Nude mice MCF-7 breast cancer xenograft model Oral 40 mg/kg/d Once daily for 17 days To evaluate the effect of IU1 combined with enzalutamide on tumor growth in a breast cancer xenograft model, results showed that the combination significantly inhibited tumor growth. J Exp Clin Cancer Res. 2019 May 24;38(1):220.
ICR mice Ischemia-reperfusion injury model Intraperitoneal injection 400 μg/kg 3 consecutive days IU1 significantly downregulated the expression of USP14 in neurons and reduced neuronal apoptosis Theranostics. 2019 May 4;9(10):2910-2923

IU1 参考文献

[1]Lee BH, et al. Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature. 2010 Sep 9;467(7312):179-84.

IU1 实验方案

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

IU1 技术信息

CAS号314245-33-5
分子式C18H21FN2O
分子量 300.37
SMILES Code CC1=CC(C(CN2CCCC2)=O)=C(C)N1C3=CC=C(F)C=C3
MDL No. MFCD01917473
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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