KY-1220

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KY-1220 是一种小分子去稳定剂，通过抑制 Wnt/β-catenin 通路来抑制 β-catenin 和 Ras (IC50=2.1 uM)。

KY-1220 is a small molecule destabilizer of both β-catenin and Ras via inhibition of the Wnt/β-catenin pathway (IC50=2.1 uM); dose-dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells; reduces β-catenin and pan-Ras protein levels via polyubiquitin-dependent proteasomal degradation, consequently inhibits the activities of both ERK and Akt in various CRC cell lines; efficiently inhibits proliferation and transformation in HCT15, SW480, D-WT and D-MT CRC cells.

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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KY1220

Wnt/Notch/Hedgehog

Beta-catenin

Beta-catenin

Cancer

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292168-79-7

314.319

C14H10N4O3S

>98% (HPLC)

DMSO : ≥ 100 mg/mL 318.15 mM

O=C(/C(N1)=C/C2=CC=CN2C3=CC=C([N+]([O-])=O)C=C3)NC1=S

(Z)-5-((1-(4-nitrophenyl)-1H-pyrrol-2-yl)methylene)-2-thioxoimidazolidin-4-one

(-20℃)

With Ice Pack

≥ 2 years