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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-Usp22i-S02
Usp22i-S02

Chemical Structure : Usp22i-S02

CAS No.: 309735-96-4

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Usp22i-S02

货号: PC-49546Not For Human Use, Lab Use Only.

Usp22i-S02 (Usp22 inhibitor S02) is a specific small-molecule inhibitor of the Foxp3-specific deubiquitinase USP22, down-regulates Foxp3 expression in Treg cells in a Usp22- but not Usp21-dependent manner.

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5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Usp22i-S02 (Usp22 inhibitor S02) is a specific small-molecule inhibitor of the Foxp3-specific deubiquitinase USP22, down-regulates Foxp3 expression in Treg cells in a Usp22- but not Usp21-dependent manner.
Usp22i-S02 stably binds not only to the hydrophobic residues but also to the charged and polar residues on the surface of the binding pocket of Usp22 protein, implying its potent efficacy in suppressing Usp22 catalytic functions.
Usp22i-S02 halts Usp22-mediated Foxp3 deubiquitination, Usp22i-S02 (10 ug/mL) down-regulates FoxP3 in a Usp22- but not Usp21-dependent manner in Usp22-null iTreg cells.
Usp22i-S02 has minimal effect on Foxp3 levels in murine Treg cells already lacking Usp22 both in vivo and in vitro.
Usp22i-S02 administration (20 mg/kg for 5 days) enhances antitumor immunity with low toxicity in mice, increases CD8+ T cell tumor infiltration, results in a Treg-specific phenotype in naïve mice with little effects on other immune cell types and tissue toxicity.
Usp22i-S02 (20 mg/kg for 3 days) showed marked tumor rejection in LLC1 tumor implantated mice.

物理化学性质&存储条件

分子量 338.414
分子式 C22H18N4
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

11-(phenylamino)-7,8,9,10-tetrahydrobenzo[4,5]imidazo[1,2-b]isoquinoline-6-carbonitrile

参考文献

1. Elena Montauti, et al. Sci Adv. 2022 Nov 25;8(47):eabo4116.

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