Subasumstat (TAK-981)

Catalog No.S8829 Batch:S882902

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Technical Data

Formula

C25H28ClN5O5S2
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
* <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.
Targets
SUMOylation enzymatic cascade [1]
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]
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)

Cell Assay:

[1]
  • Cell lines

    mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs)

  • Concentrations

    --

  • Incubation Time

    --

  • Method

    --
Animal Study:

[2]
  • Animal Models

    immune-competent BALB/c mice

  • Dosages

    7.5 mg/kg

  • Administration

    IV

Selleck's Subasumstat (TAK-981) has been cited by 11 publications

TOPORS E3 ligase mediates resistance to hypomethylating agent cytotoxicity in acute myeloid leukemia cells [ Nat Commun, 2024, 15(1):7360] PubMed: 39198401
Dual inhibition of SUMOylation and MEK conquers MYC-expressing KRAS-mutant cancers by accumulating DNA damage [ J Biomed Sci, 2024, 31(1):68] PubMed: 38992694
SUMOylated Golgin45 associates with PML-NB to transcriptionally regulate lipid metabolism genes during heat shock stress [ Commun Biol, 2024, 7(1):532] PubMed: 38710927
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

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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.

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