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KY1220

Catalog No. T15677   CAS 292168-79-7

KY1220 destabilizes both β-catenin and Ras by targeting the Wnt/β-catenin pathway. It has an IC50 of 2.1 μM in HEK293 reporter cells.

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KY1220 Chemical Structure
KY1220, CAS 292168-79-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
2 mg In stock $ 64.00
5 mg In stock $ 122.00
10 mg In stock $ 198.00
25 mg In stock $ 455.00
50 mg In stock $ 672.00
100 mg In stock $ 956.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
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Purity: 99.66%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KY1220 destabilizes both β-catenin and Ras by targeting the Wnt/β-catenin pathway. It has an IC50 of 2.1 μM in HEK293 reporter cells.
Targets&IC50 Wnt/β-catenin:2.1 μM
In vitro KY1220 accelerates the degradation rates of both β-catenin and Ras in SW480 cell lines. KY1220 dose-dependently reduces Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells. 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. In HEK293 cells, both β-catenin and pan-Ras 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 the progression of CRCs, is also destabilized by KY1220 via polyubiquitin-dependent proteasomal degradation. The proliferation and transformation of the HCT15, SW480, D-WT, and D-MT CRC cells are efficiently inhibited after treatment with KY1220.
Molecular Weight 314.32
Formula C14H10N4O3S
CAS No. 292168-79-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (318.15 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Cytoskeletal Signaling Pathway Compound Library Anti-Aging Compound Library Apoptosis Compound Library Osteogenesis Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Reprogramming Compound Library Bioactive Compound Library Anti-Obesity Compound Library Neural Regeneration Compound Library

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Keywords

KY1220 292168-79-7 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Beta catenin inhibit Wnt Inhibitor β-catenin KY 1220 KY-1220 inhibitor

 

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