Product Name :
KY1220
Description:
KY1220 is a small molecule that simultaneously degrades β-catenin and Ras by inhibition of the Wnt/β-catenin pathway.
CAS:
292168-79-7
Molecular Weight:
314.32
Formula:
C14H10N4O3S
Chemical Name:
(Z)-5-((1-(4-Nitrophenyl)-1H-pyrrol-2-yl)methylene)-2-thioxoimidazolidin-4-one
Smiles :
[O-][N+](=O)C1=CC=C(C=C1)N1C=CC=C1/C=C1\NC(=S)NC\1=O
InChiKey:
FMLUAKSJMUPACD-WQLSENKSSA-N
InChi :
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-
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
KY1220 is a small molecule that simultaneously degrades β-catenin and Ras by inhibition of the Wnt/β-catenin pathway.|Product information|CAS Number: 292168-79-7|Molecular Weight: 314.32|Formula: C14H10N4O3S|Synonym:|KY-1220|KY 1220|Chemical Name: (Z)-5-((1-(4-Nitrophenyl)-1H-pyrrol-2-yl)methylene)-2-thioxoimidazolidin-4-one|Smiles: [O-][N+](=O)C1=CC=C(C=C1)N1C=CC=C1/C=C1\NC(=S)NC\1=O|InChiKey: FMLUAKSJMUPACD-WQLSENKSSA-N|InChi: 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-|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|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.{{Palbociclib} site|{Palbociclib} Cell Cycle/DNA Damage|{Palbociclib} Protocol|{Palbociclib} In Vivo|{Palbociclib} supplier|{Palbociclib} Epigenetics} 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.{{Isatuximab (anti-CD38)} medchemexpress|{Isatuximab (anti-CD38)} Immunology/Inflammation|{Isatuximab (anti-CD38)} Immunology/Inflammation|{Isatuximab (anti-CD38)} Technical Information|{Isatuximab (anti-CD38)} Purity|{Isatuximab (anti-CD38)} manufacturer} The proliferation and transformation of the HCT15, SW480, D-WT and D-MT CRC cells are efficiently inhibited after treatment with KY1220.PMID:23903683 |References:|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.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.|
