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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-Thiolutin
Thiolutin

Chemical Structure : Thiolutin

CAS No.: 87-11-6

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Thiolutin (Acetopyrrothin)

货号: PC-49453Not For Human Use, Lab Use Only.

Thiolutin (Acetopyrrothin) is a small molecule inhibitor of the catalytic activity of E3 ubiquitin ligase HOIP, a catalytic subunit of linear ubiquitin chain assembly complex (LUBAC).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Thiolutin (Acetopyrrothin) is a small molecule inhibitor of the catalytic activity of E3 ubiquitin ligase HOIP, a catalytic subunit of linear ubiquitin chain assembly complex (LUBAC).
Thiolutin inhibits JAB1/MPN/Mov34 (JAMM) domain-containing metalloprotease, blocks NLRP3 inflammasome activation by canonical, noncanonical, alternative, and transcription-independent pathways at nanomolar concentrations.
Thiolutin alleviated NLRP3-related diseases in mouse models of lipopolysaccharide-induced sepsis, monosodium urate-induced peritonitis, experimental autoimmune encephalomyelitis, CAPS, and methionine-choline-deficient diet-induced nonalcoholic fatty liver disease.
Thiolutin improved the survival of recipients in murine myeloid leukemia and suppressed propagation in the patient-derived xenograft model of myeloid leukemia.

物理化学性质&存储条件

分子量 228.29
分子式 C8H8N2O2S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-methyl-5-oxo-4,5-dihydro-[1,2]dithiolo[4,3-b]pyrrol-6-yl)acetamide

参考文献

1. Koji Jimbo, et al. Leukemia. 2022 Nov 9. doi: 10.1038/s41375-022-01750-7.

2. Guang-Ming Ren, et al. Sci Immunol. 2021 Apr 30;6(58):eabe2933.

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