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TAK-981 (Subasumstat) is a first-in-class selective small molecule inhibitor of SUMOylation and an immuno-oncology agent. It targets and covalently binds to the small ubiquitin-like modifier (SUMO) protein, forming an adduct (TAK-981-SUMO adduct). This adduct prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9, thus prevents SUMO conjugation to lysine residues on target proteins and abrogates many sumoylated protein-mediated cellular processes that play key roles in tumor cells, including proliferation, DNA repair, metastasis and survival. In addition, by preventing sumoylation, TAK-981 is able to increase the production of type 1 interferon (IFN), thereby increasing type 1 IFN-mediated signaling, activating innate effector cells and enhancing the antitumor innate immune responses (ref 1).
Catalog NO: CT-TAK981
Synonym: Subasumstat
CAS NO: 1858276-04-6
Mol. Formula: C25H28ClN5O5S2
MW: 578.1 (or refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material. >99% by achiral and chiral HPLCs (Attached). Authenticated Stereo-Structure by 2-D NMRs. Validated potency vs SUMO E1 Ligase, more potent than the benchmark reference ML792 (ref. 2), Bulk Stock!! Prompt.