Chemical Structure : 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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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.
| 分子量 | 406.54 | |
| 分子式 | C24H26N2O2S | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Liang J, et al. Cell Rep. 2026 Jul 24;45(8):117719.
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