TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
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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] |
Dose | Mice: 7.5 mg/kg[2] (i.v.) |
Administration | i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.73mL 0.35mL 0.17mL |
8.65mL 1.73mL 0.86mL |
17.30mL 3.46mL 1.73mL |
CAS号 | 1858276-04-6 |
分子式 | C25H28ClN5O5S2 |
分子量 | 578.103 |
别名 | TAK-981 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 16 mg/mL(27.68 mM),配合低频超声,并水浴加热至45℃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 |