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    InvivoChem Cat #: V4586
    CAS #: 1858276-04-6 (freePurity ≥98%

    Description: TAK-981 is a novel, potent and selective small molecule inhibitor of sumoylation with potential immune-activating and antineoplastic activities. Upon intravenous administration, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, forming an adduct with SUMO protein (TAK-981-SUMO adduct). This prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9. This 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. This may further increase tumor cell killing. Sumoylation, a post-translational modification that attaches the SUMO protein to target proteins, plays a key role in regulating their activity, function, subcellular localization and stability. Sumoylation also plays a key role in inhibiting innate immune responses, specifically by inhibiting the pattern recognition receptor (PRR) pathway and preventing type 1 IFN expression. Abnormal sumoylation of target proteins is associated with many cancers. 

    ReferencesSumoylation inhibitor TAK-981.

    Related CAS : 1858276-04-6 (free); 1858279-63-6 (hydrate) 

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    Name: TAK-981
    CAS#: 1858276-04-6 (free)
    Chemical Formula: C25H28ClN5O5S2
    Exact Mass: 577.122
    Molecular Weight: 578.099
    Elemental Analysis: C, 51.94; H, 4.88; Cl, 6.13; N, 12.11; O, 13.84; S, 11.09
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: TAK-981; TAK 981; TAK981
    Chemical Name: [(1R,2S,4R)-4-[(5-[4-[(1R)-7-Chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl)amino]-2-hydroxycyclopentyl]methyl sulfamate
    InChi Code: InChI=1S/C25H28ClN5O5S2/c1-13-18(23-19-7-16(26)3-2-14(19)4-5-29-23)9-22(37-13)24(33)20-10-28-12-30-25(20)31-17-6-15(21(32)8-17)11-36-38(27,34)35/h2-3,7,9-10,12,15,17,21,23,29,32H,4-6,8,11H2,1H3,(H2,27,34,35)(H,28,30,31)/t15-,17-,21+,23+/m1/s1
    SMILES Code: O=S(OC[[email protected]@H]1[[email protected]@H](O)C[[email protected]](NC2=NC=NC=C2C(C3=CC([[email protected]@H]4NCCC5=C4C=C(Cl)C=C5)=C(C)S3)=O)C1)(N)=O

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