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KY1220
CAS No. : 292168-79-7
MCE 国际站：KY1220
产品活性：KY1220作用于 Wnt/β-catenin 靶点，使β-catenin 和 Ras不稳定。在HEK293报告细胞中的IC50 值为2.1 μM。
研究领域：Stem Cell/Wnt
作用靶点：Wnt | β-catenin
In Vitro: KY1220 shows an IC50 of 2.1 μM in HEK293 reporter cells. KY1220 dose dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells. In HEK293 cells, both β-catenin and panRas protein levels are similarly reduced in a dose-dependent manner after treatment with KY1220, whereas the mRNA levels of CTNNB1 (which encodes β-catenin), NRAS, KRAS and HRAS remain unchanged. K-Ras, which has a critical role in progression of CRCs, is also destabilized by KY1220 via polyubiquitin-dependent proteasomal degradation. KY1220 accelerates the degradation rates of both β-catenin and Ras in SW480 cell lines. Ras destabilization by KY1220 consequently inhibits the activities of both ERK and Akt, which are downstream effectors of Ras in SW480 cells harboring a KRAS mutation. The proliferation and transformation of the HCT15, SW480, D-WT and D-MT CRC cells are efficiently inhibited after treatment with KY1220.
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A., Delneste Y., Herbault N., Jeannin P., Bonnefoy J.Y., Beck A. and Aubry J.P. (2002)Cytometry, 48:71-79. MEDLINE Cited by[[10]] Garraud O., Diouf A., Nguer C.M., Tall A., Marrama L. and Perraut R. (2001)Scand. J. Immunol., 54:606-612. MEDLINE Cited by[[11
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