Subasumstat (TAK-981)

製品コードS8829 バッチS882902

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)
		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.

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	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]

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	--
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

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：

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

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。