| Customization: | Available |
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| Powder: | Yes |
| Customized: | Non-Customized |
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| Molecular Weight | 578.10 |
|---|---|
| Formula |
C25H28ClN5O5S2 |
| CAS No. | 1858276-04-6 |
| Storage | 3 years-20°C powder 2 years-80°C in solvent |
| Synonyms | N/A |
| Description | Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities. | |
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| Targets |
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| 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.
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| In vivo |
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. |
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