| Name | Subasumstat |
| Description | Subasumstat (TAK-981), a selective inhibitor of the SUMOylation enzymatic cascade, has potential immune-activating and antineoplastic activities. |
| In vitro | Methods: HL-60 cells were treated with TAK-981 (10nM; 100nM) for 24 h, and the levels of SUMO-1 and SUMO-2/3 were detected by Western blot. To characterize the effect of the SUMOylation inhibitor TAK-981 on AML cells, we first monitored its effect on SUMOylation in three AML model cell lines HL-60, U937, and THP-1.
Results: TAK-981 significantly reduced the global SUMOylation level mediated by SUMO-1 and SUMO-2/3 at 10 nM concentration and almost completely abolished it at 100 nM concentration. [1] |
| In vivo | Methods: TAK-981 (15 mg/kg) was injected intravenously into the tumor model mice to detect the anti-tumor activity in vivo.
Results: TAK981 significantly inhibited tumor growth. [2] |
| Storage | The compound is unstable in solution. Please use soon | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.46 mM), Sonication is recommended.
DMSO : 122.5 mg/mL (211.9 mM), Sonication is recommended.
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| Keywords | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | TAK981 | TAK 981 | SUMOylation | Subasumstat | Inhibitor | inhibit | E3Enzyme | E3 ligating enzyme | E3 Enzyme | E2Enzyme | E2 Enzyme | E2 conjugating enzyme | E1Enzyme | E1/E2/E3 Enzyme | E1 Enzyme | E1 activating enzyme |
| Inhibitors Related | NSC697923 | T521 | PYZD-4409 | NAcM-OPT | Nutlin-3 | Yucasin | BC-1293 | EN219 | NSC232003 | Auxinole | Indole-3-carbinol | Idasanutlin |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
