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CAS No.: 1858276-04-6

Subasumstat Catalog No. CSN24144

Synonyms: TAK-981

TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.

规格	价格	促销价格	库存	数量

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TAK-981 is a new small molecule inhibitor of sumoylation. Through intravenous administration, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, preventing SUMO conjugation to lysine residues on target proteins and abrogating many sumoylated protein-mediated cellular processes that play key roles in tumor cells, including proliferation, DNA repair, metastasis and survival. Through preventing sumoylation, TAK-981 is able to increase the production of type 1 IFN and thereby increases type 1 IFN-mediated signaling, activates innate effector cells and enhances the antitumor innate immune responses. This may further increase tumor cell killing. These suggest TAK-981 may have potential immune-activating and antineoplastic activities.
作用机制TAK-981 could covalently bind to SUMO protein and form an adduct with SUMO protein, which prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9.^[1]
动物研究
剂量
Mice: 7.5 mg/kg^[2] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 7.5 mg/kg^[2] (i.v.)
给药途径	i.v.

[1] Sumoylation inhibitor TAK-981

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7298 mL
- 8.6490 mL
- 17.2979 mL
- 5 mM
- 0.3460 mL
- 1.7298 mL
- 3.4596 mL
- 10 mM
- 0.1730 mL
- 0.8649 mL
- 1.7298 mL

技术信息

CAS号

1858276-04-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H28ClN5O5S2

运输

蓝冰

分子量

578.10

别名

TAK-981

溶解度

DMSO	97.0 mg/mL (167.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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