产品
编 号：F308118
分子式：C14H10N4O3S
分子量：314.32
分子式：C14H10N4O3S
分子量：314.32
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 292168-79-7
产品详情
生物活性：
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
体外研究：
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.
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
体外研究：
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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