KY1220

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KY1220  纯度: ≥98.0%

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。

KY1220

KY1220 Chemical Structure

CAS No. : 292168-79-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1380 In-stock
2 mg ￥800 In-stock
5 mg ￥1500 In-stock
10 mg ￥2500 In-stock
25 mg ￥5500 In-stock
50 mg ￥9400 In-stock
100 mg ￥16000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

KY1220 相关产品

•相关化合物库:

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  • Wnt/Hedgehog/Notch Compound Library
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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.

IC50 & Target

IC50: 2.1 μM (HEK293 reporter cells)[1]
体外研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

314.32

Formula

C14H10N4O3S
CAS 号

292168-79-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (318.15 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1815 mL 15.9074 mL 31.8147 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

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

HCT15 or SW480 cells are treated with 25 μM KY1220 or KYA1797K or with control (DMSO) for 72 h. Cell proliferation is measured using the MTT assay. The absorbance of the formazan product is determined at 590 nm every 24 h[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

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

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