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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Immune Checkpoints-JNU-0921
JNU-0921

Chemical Structure : JNU-0921

CAS No.: 3079468-41-7

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JNU-0921 (JNU0921)

货号: PC-22968Not For Human Use, Lab Use Only.

JNU-0921 is a specfiic, small molecule CD137 (4-1BB/TNFRSF9) agonist with EC50 of 64 nM in cell-based luciferase assays, activates both human and mouse CD137, directly binds the extracellular domain of CD137, induces CD137 oligomerizationand activates CD137 signaling.

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10 mg ￥2180 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

JNU-0921 is a specfiic, small molecule CD137 (4-1BB/TNFRSF9) agonist with EC50 of 64 nM in cell-based luciferase assays, activates both human and mouse CD137, directly binds the extracellular domain of CD137, induces CD137 oligomerizationand activates CD137 signaling.
JNU-0921 treatment stimulated transcription levels of IFN-γ and Granzyme B (GZMB) in JC-luc cells.
JNU-0921 treatment promoted the proliferation of both CD8+ and CD4+ splenic T cells from WT mice in a similar manner to agonistic anti-CD137 antibody (aCD137), but not enhance proliferation of CD137 knockout (KO) T cells.
JNU-0921 treatment increased the levels of CD25 and CD69 in a CD137-dependent manner, up-regulated the expression of effector cytokines in both CD8+ and CD4+ T cells, including IL-2 and IFN-γ.
JNU-0921 promoted the proliferation of CD8+ T cells and CD4+ T cells in human peripheral blood cells.
JNU-0921 binding to CD137 led to recruitment of TRAF2 and TRAF3 to form signaling complex, activates the NF-κB signaling pathway.
JNU-0921 (50 mg/kg per day, gavage) effectively shrinks tumors and rewires tumor immune microenvironment in MC38 xenograft mouse model.

物理化学性质&存储条件

分子量 316.32
分子式 C19H12N2O3
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

3-(5-(naphthalen-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid

参考文献

1. Lu Liu, et al. Sci Adv. 2024 Aug 23;10(34):eadp8647.

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