KY1220


Catalog No. size PriceQuantity
M6953-2 2mg solid $107
M6953-10 10mg solid $441

Description

Cas:292168-79-7

Product Information:

KY1220 is a small molecule that simultaneously degrades β-catenin and Ras by inhibition of the Wnt/β-catenin pathway.

 

Chemical Formula: C14H10N4O3S

 

Exact Mass: 314.0474

 

Molecular Weight: 314.32

Elemental Analysis: C, 53.50; H, 3.21; N, 17.83; O, 15.27; S, 10.20

 

Chemical Name:

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

 

InChi Key: 

FMLUAKSJMUPACD-WQLSENKSSA-N

 

InChi Code: 

InChI=1S/C14H10N4O3S/c19-13-12(15-14(22)16-13)8-11-2-1-7-17(11)9-3-5-10(6-4-9)18(20)21/h1-8H,(H2,15,16,19,22)/b12-8-

 

Smiles Code:

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

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

 

References:

 

  1. Cha PH, Choi KY. Simultaneous destabilization of β-catenin and Ras via targeting of the axin-RGS domain as a potential therapeutic strategy for colorectal cancer. BMB Rep. 2016 Sep;49(9):455-6. PubMed PMID: 27470214; PubMed Central PMCID: PMC5227137.

 

  1. Cha PH, Cho YH, Lee SK, Lee J, Jeong WJ, Moon BS, Yun JH, Yang JS, Choi S, Yoon J, Kim HY, Kim MY, Kaduwal S, Lee W, Min do S, Kim H, Han G, Choi KY. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600. doi: 10.1038/nchembio.2103. Epub 2016 Jun 13. PubMed PMID: 27294323.

 

Products are for research use only. Not for human use.

 

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