Information Subasumstat (TAK-981) Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities. Targets SUMOylation enzymatic cascade In vitro In both mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs), TAK-981 treatment ex vivo induced markers of activation and maturation including CD40, CD80 and CD86, as well as increased secretion of inflammatory cytokines like IP-10, MCP1, MIP-1α, MIP1β, IFNα and IFNβ. In vivo a single sub-cutaneous injection of TAK-981 in naïve Balb/c mice at the brachial lymph nodes induced activation of DCs, measured as significant increases in CD40 and CD86 expression. TAK-981 demonstrates antitumor activity, including complete regression (CR) of some tumors, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumors. Cell Research(from reference) Cell lines:mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs)
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Subasumstat (TAK-981)
CAS number:1858276-04-6 molecular formula:C25H28ClN5O5S2
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| Chinese alias | 苏巴坦 (TAK-981) | ||
| English alias | [(1R,2S,4R)-4-{[5-({4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methyl-2- thienyl}carbonyl)pyrimidin-4-yl]amino}-2-hydroxycyclopentyl]methyl sulfamate | LXRZVMYMQHNYJB-UNXOBOICSA-N | Sumoylation inhibitor TAK-981 | SUBASUMSTAT [WHO-DD] | 185827 | ||
| CAS number | 1858276-04-6 | molecular formula | C25H28ClN5O5S2 |
| molecular weight | 578.10 g/mol | Exact mass | - |
| PSA | 193.000 Ų | logp | 3.500 |
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