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DHODH inhibitor HL6

Chemical Structure : DHODH inhibitor HL6

CAS No.:

DHODH inhibitor HL6

货号: PC-27357Not For Human Use, Lab Use Only.

DHODH inhibitor HL6 is a potent, CoQ-competitive DHODH inhibitor with Ki of 2.39 nMand IC50 of 5.29 nM (recombinant human DHODH), disrupts WDR77 stabilization, thereby attenuating PRMT5/WDR77-dependent AKT signaling in PIK3CA-mutant CRC.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DHODH inhibitor HL6 is a potent, CoQ-competitive DHODH inhibitor with Ki of 2.39 nMand IC50 of 5.29 nM (recombinant human DHODH), disrupts WDR77 stabilization, thereby attenuating PRMT5/WDR77-dependent AKT signaling in PIK3CA-mutant CRC.
HL6 suppresses WDR77-dependent AKT activation and selectively inhibits PIK3CA-mutant CRC growth.
HL6 treatment significantly shortened the half-life of WDR77 compared with DMSO treatment in PIK3CA-mutant CRC cells
HL6 significantly reduced levels of WDR77 and p-AKT compared to vehicle controls in PIK3CA-mutant cells (RKO and LS180), while WDR77 overexpression reversed this effect.
HL6 decreased the O-GlcNAcylation of WDR77, mimics the DHODH-knockdown effects in PIK3CA-mutant CRC cells.
HL6 (10 mg/kg/day, p. o.) suppresses tumor growth of PIK3CA-mutant colorectal cancer in orthotopic and PDX models.

物理化学性质&存储条件

分子量 406.54
分子式 C24H26N2O2S
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

(R)-2-((2-(cyclobutylmethoxy)-[1,1'-biphenyl]-3-yl)amino)-4,5,6,7-tetrahydrobenzo[d]thiazol-4-ol

参考文献

1. Liang J, et al. Cell Rep. 2026 Jul 24;45(8):117719.

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