KYA1797K

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Chemical Structure| 1956356-56-1 同义名 : -
CAS号 : 1956356-56-1
货号 : A228508
分子式 : C17H11KN2O6S2
纯度 : 99%+
分子量 : 442.507
MDL号 : MFCD30718585
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(11.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.26 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Colorectal cancer (CRC) is one of the most frequent cancers and the second leading cause of cancer-related deaths in Western countries. Both the Wnt/β-catenin and Ras pathways are aberrantly activated in most human colorectal cancers (CRCs) and interact cooperatively in tumor promotion. KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. YA1797K inhibited TOPflash activity to a greater extent with an IC50 of 0.75 μM, and effectively reduced the levels of both β-catenin and pan-Ras as well as the activities of ERK (extracellular-signal-regulated kinase) and Akt in SW480 cells. Using multipathway reporter arrays, KYA1797K significantly (P < 0.01) decreased reporter activities for the Wnt/β-catenin and MAPK/ERK pathways. In the CRC lines SW480, LoVo, DLD1 and HCT15, KYA1797K degraded both β-catenin and Ras in a dose-dependent manner. Consistently, cell proliferation was suppressed by KYA1797K treatment. KYA1797K destabilized β-catenin and Ras in DLD1 cells expressing WT β-catenin or WT K-Ras. Those data indicated that KYA1797K inhibited proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. In vivo, KYA1797K was injected intraperitoneally (i.p.) into mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations. KYA1797K administration (25 mg/kg) reduced both weight and volume of the tumor by 70%. KYA1797K treatment significantly reduced levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling target[2].
作用机制 KYA1797K bound directly to the regulators of G-protein signaling domain of axin[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.60mL

4.52mL

2.26mL
参考文献

[1]Cha PH, Cho YH, Lee SK, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016;12(8):593-600

[2]Cha PH, Cho YH, Lee SK, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016;12(8):593‐600