Chemical Structure : DHODH inhibitor HL6
CAS No.:
DHODH inhibitor HL6
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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406.54
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Formula
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C24H26N2O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-2-((2-(cyclobutylmethoxy)-[1,1'-biphenyl]-3-yl)amino)-4,5,6,7-tetrahydrobenzo[d]thiazol-4-ol
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References
1. Liang J, et al. Cell Rep. 2026 Jul 24;45(8):117719.
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