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TAK-981

A potent and selective sumoylation inhibitor
Catalog #: B3411
SKU-Size Size Price Qty
B3411-1 1 mg
$75.00
B3411-5 5 mg
$275.00
More Sizes Get Quote

Product Details

Alternate Name [(1R,2S,4R)-4-[[5-[[4-[(1R)-7-chloro-1,2,3,4-tetrahydro-1-isoquinolinyl]-5-methyl-2-thienyl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]sulfamic acid, methyl ester TAK981 Subasumstat
Appearance Solid
CAS # 1858276-04-6
Molecular Formula C₂₅H₂₈ClN₅O₅S₂
Molecular Weight 578.1
Purity ≥98%
Solubility >50 mg/ml DMSO
SMILES CC1=C(C=C(C(C2=CN=CN=C2N[[email protected]@H]3C[[email protected]](COS(N)(=O)=O)[[email protected]@H](O)C3)=O)S1)[[email protected]@]4([H])C5=CC(Cl)=CC=C5CCN4
InChi 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
InChi Key LXRZVMYMQHNYJB-UNXOBOICSA-N
PubChem CID 118628567
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

TAK-981 is potent and selective inhibitor of SUMO-activating enzyme (SAE; IC50 = <10 nM). SUMOylation is a reversible post-translational modification that regulates protein function by covalent attachment of small ubiquitin-like modifier (SUMO) proteins to a protein substrate. SUMOylation has a key role in restraining Type I interferon (IFN) responses. TAK-981 upregulates the expression of IFN-regulated genes in the blood and tumor tissue in an A20 syngeneic lymphoma mouse model. It also decreases intratumor levels of SUMOlyated proteins and reduces tumor growth in the same model.


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