Home Cell Cycle DNA/RNA Synthesis inhibitor YK-4-279 For research use only.

YK-4-279

YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).

YK-4-279 Chemical Structure

YK-4-279 Chemical Structure

CAS No. 1037184-44-3

Purity & Quality Control

YK-4-279 Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 Function assay Inhibition of transcriptional activity of full-length EWS-FLI1 (unknown origin) expressed in COS7 cells by NR0B1-luciferase reporter gene assay, IC50=0.35μM 25432018
TC71 Growth inhibition assay 3 days Growth inhibition of human TC71 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.92μM 25432018
TC32 Growth inhibition assay 3 days Growth inhibition of human TC32 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.94μM 25432018
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
Targets
RHA [1]
In vitro
In vitro YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also specifically inhibits ESFT cell growth and induces apoptosis. [1] YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion. [2]
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 29212266
Western blot PARP / Cleaved PARP / Caspase 3 / Cleaved Caspase 3 p-HH3(Ser10) / Histone H3 / p-Aurora A (T288) / Aurora A / Aurora B / Cyclin B / p53 / p21 29212266
In Vivo
In vivo In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. [1] In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors. [3]
Animal Research Animal Models Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts
Dosages 1.5 mg/dose
Administration i.p.

Chemical Information & Solubility

Molecular Weight 366.20 Formula

C17H13Cl2NO4
CAS No. 1037184-44-3 SDF Download YK-4-279 SDF
Smiles COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 73 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I would like to know whether YK-4-279 is the racemate version, or whether it is the + R-enantiomer or the – S-enantiomer of the compound?

Answer:
For our S7679 YK-4-279, it is a recemate.

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