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Technical Data
| Formula | C25H28ClN5O5S2 |
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| Molecular Weight | 578.10 | CAS No. | 1858276-04-6 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (172.98 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| 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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| 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.[1] |
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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.[1] TAK-981 demonstrates antitumor activity, including complete regression (CR) of some tumors, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumors.[2] |
Protocol (from reference)
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References
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Selleck's Subasumstat (TAK-981) has been cited by 8 publications
| ER Stress-Activated HSF1 Governs Cancer Cell Resistance to USP7 Inhibitor-Based Chemotherapy through the PERK Pathway [ Int J Mol Sci, 2024, 25(5)2768] | PubMed: 38474017 |
| The SUMO-NIP45 pathway processes toxic DNA catenanes to prevent mitotic failure [ Nat Struct Mol Biol, 2023, 10.1038/s41594-023-01045-0] | PubMed: 37474739 |
| Supplementation with α-ketoglutarate improved the efficacy of anti-PD1 melanoma treatment through epigenetic modulation of PD-L1 [ Cell Death Dis, 2023, 14(2):170] | PubMed: 36854755 |
| SUMOylation-mediated PSME3-20S proteasomal degradation of transcription factor CP2c is crucial for cell cycle progression [ Sci Adv, 2023, 9(4):eadd4969] | PubMed: 36706181 |
| Suppression of ACE2 SUMOylation protects against SARS-CoV-2 infection through TOLLIP-mediated selective autophagy [ Nat Commun, 2022, 13-1:5204] | PubMed: 36057605 |
| hnRNP G/RBMX enhances HPV16 E2 mRNA splicing through a novel splicing enhancer and inhibits production of spliced E7 oncogene mRNAs [ Nucleic Acids Res, 2022, 50(7):3867-3891] | PubMed: 35357488 |
| SUMO Modification of PAF1/PD2 Enables PML Interaction and Promotes Radiation Resistance in Pancreatic Ductal Adenocarcinoma [ Mol Cell Biol, 2021, 10.1128/MCB.00135-21] | PubMed: 34570619 |
| Hypoxia stimulates SUMOylation-dependent stabilization of KDM5B [ Research Square, 2021, 10.21203/rs.3.rs-620216/v1] | PubMed: None |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.