Subasumstat (TAK-981)

製品コードS8829 バッチS882903

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₈ClN₅O₅S₂

分子量

578.10

CAS No.

1858276-04-6

Solubility (25°C)*

体外

DMSO

100 mg/mL (172.98 mM)

Ethanol

33 mg/mL (57.08 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (8.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.
in vitro	Ex vivo treatment with Subasumstat (TAK-981) induced markers of activation and maturation—including CD40, CD80, and CD86—as well as increased secretion of inflammatory cytokines such as IP-10, MCP1, MIP-1α, MIP1β, IFNα, and IFNβ in both mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs).^[1]
in vivo	In vivo, a single sub-cutaneous injection of Subasumstat (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] This compound demonstrates antitumor activity, including complete regression (CR) of some tumors, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumors.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs)
	濃度	--
	反応時間	--
	実験の流れ	Subasumstat (TAK-981) is described in this text, and it will appear alongside many other descriptions of this compound.
動物実験	動物モデル	immune-competent BALB/c mice
	投薬量	7.5 mg/kg
	投与方法	IV

参考

https://cancerres.aacrjournals.org/content/79/13_Supplement/3252.short
https://cancerres.aacrjournals.org/content/79/13_Supplement/3079.short

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

SUMOylation inhibition potentiates the glucocorticoid receptor to program growth arrest of acute lymphoblastic leukemia cells [ Oncogene, 2025, none]	PubMed: 39953147
TopBP1 coordinates DNA repair synthesis in mitosis via recruitment of the nuclease scaffold SLX4 [ Commun Biol, 2025, 8(1):1005]	PubMed: 40615546
SUMOylation regulates GSDMD stability and pyroptosis [ Int Immunopharmacol, 2025, 149:114187]	PubMed: 39919454
Phosphorylation-induced SUMOylation promotes Ulk4 condensation at the ciliary tip to transduce Hedgehog signal [ J Cell Sci, 2025, 138(20)jcs263695]	PubMed: 40171800
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
Targeting SUMOylation with an injectable nanocomposite hydrogel to optimize radiofrequency ablation therapy for hepatocellular carcinoma [ J Nanobiotechnology, 2024, 22(1):338]	PubMed: 38890737
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。