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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Immune Checkpoints-ZY-MY-111
ZY-MY-111

Chemical Structure : ZY-MY-111

CAS No.:

ZY-MY-111

货号: PC-26971Not For Human Use, Lab Use Only.

ZY-MY-111 is a selective, reversible, small-molecule inhibitor of interleukin-4-induced-1 (IL4I1) with IC50 of 1.86 uM, specifically targets the IL4I1-AHR axis and restores anti-tumor immunity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZY-MY-111 is a selective, reversible, small-molecule inhibitor of interleukin-4-induced-1 (IL4I1, FIG1) with IC50 of 1.86 uM, specifically targets the IL4I1-AHR axis and restores anti-tumor immunity.
ZY-MY-111 displays exceptional selectivity, showing no inhibition of IDO1-mediated tryptophan metabolism at 10 uM.
ZY-MY-111 occupies the enzymatic active site of IL4I1, directly overlapping with the binding regions of endogenous substrates phenylalanine and tryptophan.
ZY-MY-111 dose-dependently suppresses basal AHR activation with IC50 of 2.14 uM in HEK293T-XRE reporter cells.
ZY-MY-111 significantly suppressed L-tryptophan (500 μM)-induced AHR nuclear accumulation, rescued the up-regulation of CYP1A1 expression induced by tryptophan in HT-29 cells.
ZY-MY-111 enhances CD8+ T cell proliferation and antitumor response, exhibits antitumor efficacy through immune reprogramming.
ZY-MY-111 (50 mg/kg, BID, i.p.) significantly suppressed tumor growth in the syngeneic A20 B cell lymphoma mouse model.
ZY-MY-111 (25 mg/kg, BID, i.p.) significantly increased CD8+/CD4+ ratio and infiltration of effector memory T cells in mice bearing CT26 colon carcinoma.

物理化学性质&存储条件

分子量 320.81
分子式 C16H14ClFN2S
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-(3-Chlorophenethyl)-6-fluoro-3,4-dihydroquinazoline-2(1H)-thione

参考文献

1. Li JF, et al. Acta Pharmacol Sin. 2026 Jun 8. doi: 10.1038/s41401-026-01843-4.

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