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iCRT3

CAS No. : 901751-47-1

MCE 国际站：iCRT3

产品活性：iCRT3 是 Wnt 和 β-连环蛋白应答转录 (β-catenin-responsive transcription) 的抑制剂。

研究领域：Stem Cell/Wnt  |  Apoptosis

作用靶点：Wnt  |  Apoptosis

In Vitro: iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription. iCRT3 significantly decreases TOP Flash activity and reduces the level of NTSR1. The anti-apoptotic effects of Neurotensin (NTS) and Wnt3a can be largely abrogated by iCRT3. Cells maintained long term with iCRT3 show enhanced expression of classic pluripotency genes compare with the DMSO control, whereas expression of differentiation markers and T-cell factor (TCF) target genes is concomitantly reduced. Treatment with iCRT3 at doses of 12.5, 25, 50, and 75 μM decreases TNF-α levels by 14.7%, 18.5%, 44.9% and 61.3%, respectively. With iCRT3 treatment, IκB levels are increased in a dose-dependent manner compare to the vehicle.

In Vivo: The tumor growth rates are markedly retarded by iCRT3 treatment. Consistently, the tumor-suppressive role of iCRT3 is accompanied with a reduction in Ki67 index, a proliferation marker. The IL-6 levels in the 10 mg/kg iCRT3 treatment group are 82.9% lower than those in the vehicle group. IL-1β levels are undetectable in the sham but reach 371 pg/mL in septic mice and are down by 30.2% and 53.2%, respectively, with 5 and 10 mg/kg iCRT3. With iCRT3 treatment at doses of 5 and 10 mg/kg, AST levels in these septic mice are 15.4% and 44.2% lower, respectively, than those in the vehicle-treated mice. After treatment with 10 mg/kg iCRT3, lung morphology is improved with much reduced microscopic deterioration, compare to the vehicle group. The number of apoptotic cells in the lung tissues of the iCRT3-treated mice is significantly reduced by 92.7% in comparison with the vehicle group.

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