Subasumstat

SKU: orb1298942

Description

TAK-981 (Subasumstat) is a first-in-class, selective inhibitor of the SUMOylation cascade with demonstrated immune-activating and antitumor properties. It is utilized in oncology research to investigate SUMOylation's role in cancer immunity, showing activity in both cellular assays and in vivo tumor models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1858276-04-6
• MW: 578.1
• Purity: 98.22% (May vary between batches)
• Formula: C₂₅H₂₈ClN₅O₅S₂
• SMILES: Cc1sc(cc1[C@@H]1NCCc2ccc(Cl)cc12)C(=O)c1cncnc1N[C@H]1C[C@H](O)[C@@H](COS(N)(=O)=O)C1
• Target: E1/E2/E3 Enzyme
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.46 mM);DMSO:122.5 mg/mL (211.9 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, E3 ligating enzyme, E3 Enzyme, E2Enzyme, E2 conjugating enzyme, E2 Enzyme, E3Enzyme, E1 Enzyme, E1 activating enzyme, E1Enzyme, E1/E2/E3 Enzyme, Ubiquitin ligase, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme, SUMOylation, Subasumstat, TAK981, TAK-981, TAK 981

Compound Identifiers

PubChem CID

118628567