KYA1797K | CAS#1956356-56-1

MedKoo Cat#: 525451 | Name: KYA1797K

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

KYA1797K is a novel highly potent and selective inhibitor of both Wnt/ß-catenin and Ras pathways.

Chemical Structure

KYA1797K

CAS#1956356-56-1

Theoretical Analysis

MedKoo Cat#: 525451

Name: KYA1797K

CAS#: 1956356-56-1

Chemical Formula: C17H11KN2O6S2

Exact Mass: 441.9696

Molecular Weight: 442.50

Elemental Analysis: C, 46.14; H, 2.51; K, 8.84; N, 6.33; O, 21.69; S, 14.49

Price and Availability

Size	Price	Availability
25mg	USD 285.00	2 Weeks
50mg	USD 450.00	2 Weeks
100g	USD 750.00	2 Weeks

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Related CAS #

851304-36-4 (free acid) 1956356-56-1

Synonym

KYA1797K

IUPAC/Chemical Name

(5Z)-5-[[5-(4-Nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid potassium salt

InChi Key

PHUNRLYHXGMOLG-WQRRWHLMSA-M

InChi Code

InChI=1S/C17H12N2O6S2.K/c20-15(21)7-8-18-16(22)14(27-17(18)26)9-12-5-6-13(25-12)10-1-3-11(4-2-10)19(23)24;/h1-6,9H,7-8H2,(H,20,21);/q;+1/p-1/b14-9-;

SMILES Code

O=C([O-])CCN(C/1=O)C(SC1=C/C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2)=S.[K+]

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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

In vitro activity:

In cultured proximal tubular cells, KYA1797K shows a better effect on inhibiting cellular senescence and could better suppress mitochondrial dysfunction and ameliorate the fibrotic changes, at the same dose as that in ICG-001. Reference: Kidney Dis (Basel). 2022 Sep 27;8(5):408-423. https://pubmed.ncbi.nlm.nih.gov/36466073/

In vivo activity:

Furthermore, KYA1797K effectively inhibited Kras-driven tumorigenesis in the KrasLA2 mouse model by suppressing the Ras-ERK pathway. Reference: Sci Rep. 2019 Jan 24;9(1):648. https://pubmed.ncbi.nlm.nih.gov/30679620/

Preparing Stock Solutions

The following data is based on the product molecular weight 442.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhu M, Ling X, Zhou S, Meng P, Chen Q, Chen S, Shen K, Xie C, Kong Y, Wang M, Zhou L. KYA1797K, a Novel Small Molecule Destabilizing β-Catenin, Is Superior to ICG-001 in Protecting against Kidney Aging. Kidney Dis (Basel). 2022 Sep 27;8(5):408-423. doi: 10.1159/000526139. PMID: 36466073; PMCID: PMC9710484. 2. Ruan Z, Liang M, Lai M, Shang L, Deng X, Su X. KYA1797K down-regulates PD-L1 in colon cancer stem cells to block immune evasion by suppressing the β-catenin/STT3 signaling pathway. Int Immunopharmacol. 2020 Jan;78:106003. doi: 10.1016/j.intimp.2019.106003. Epub 2019 Dec 5. PMID: 31812723. 3. Park J, Cho YH, Shin WJ, Lee SK, Lee J, Kim T, Cha PH, Yang JS, Cho J, Min DS, Han G, Lee HY, Choi KY. A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer. Sci Rep. 2019 Jan 24;9(1):648. doi: 10.1038/s41598-018-37059-8. PMID: 30679620; PMCID: PMC6345925. 4. 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. PMID: 27294323.

In vitro protocol:

In vivo protocol:

1. Park J, Cho YH, Shin WJ, Lee SK, Lee J, Kim T, Cha PH, Yang JS, Cho J, Min DS, Han G, Lee HY, Choi KY. A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer. Sci Rep. 2019 Jan 24;9(1):648. doi: 10.1038/s41598-018-37059-8. PMID: 30679620; PMCID: PMC6345925. 2. 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. PMID: 27294323.

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. 2: 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.