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YK-4-279

Catalog No. T2275   CAS 1037184-44-3

YK 4-279, an inhibitor of RNA Helicase A (RHA), binds to the oncogenic transciption factor EWS-FLI1.

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YK-4-279 Chemical Structure
YK-4-279, CAS 1037184-44-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 54.00
10 mg In stock $ 79.00
25 mg In stock $ 148.00
50 mg In stock $ 277.00
100 mg In stock $ 491.00
200 mg In stock $ 751.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
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Purity: 99.89%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description YK 4-279, an inhibitor of RNA Helicase A (RHA), binds to the oncogenic transciption factor EWS-FLI1.
In vitro In the fusion-positive LNCaP-luc-M mouse tumor model, YK-4-279 effectively inhibits tumor cell proliferation and migration. In the in vivo Ewing's Sarcoma Family of Tumors (ESFT) xenografts, YK-4-279 (1.5 mg/kg i.p.) successfully suppresses growth.
In vivo In TC32 cells containing EWS-FLI1, YK-4-279 inhibits cell growth by blocking the interaction between EWS-FLI1 and RHA, thereby reducing the level of cyclin D. In ESFT cells, YK-4-279 can suppress cellular proliferation and induce apoptosis. Additionally, in prostate cancer cells positive for fusion, YK-4-279 inhibits the biological activity of ERG and ETV1, leading to decreased cell migration.
Kinase Assay Cytosolic phosphorylation of Akt: Hela cells are serum starved for 1 hr and treated with IGF (100ng/mL) or SC79 (4 μg/mL) for 30 minutes. Cells are lysed in Lysis buffer containing 250 mM Sucrose, 20 mM HEPES, 10 mM KCl, 1.5 mM MgCl2, 1 mM EDTA, 1 mM EGTA supplemented with protease inhibitors. Cells are passed through 25 g needle several times and kept on ice for 20 minutes. Total cell lysate is taken at this point. Cell lysates are centrifuged at 100,000 g for 30 minutes. Supernatant is collected as the cytosolic fraction. Pellet is washed with lysis buffer and represents the membrane fraction. Total cell lysate, cytosolic and membrane fractions are resolved by SDS-PAGE and analyzed for phospho-Akt (S473), Total Akt, Tubulin (cytosolic marker) and Orai1 (membrane marker) by western blotting.
Molecular Weight 366.2
Formula C17H13Cl2NO4
CAS No. 1037184-44-3

Storage

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

Solubility Information

Ethanol: 48 mg/mL (131.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 68 mg/mL (185.7 mM)

TargetMolReferences and Literature

1. Erkizan HV, et al. Nat Med. 2009, 15(7), 750-756. 2. Rahim S, et al. PLoS One. 2011, 6(4), e19343. 3. Rahim S, et al. PLoS One. 2014, 9(12), e114260.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Anti-Aging Compound Library Bioactive Compound Library Toxic Compound Library Anti-Cancer Compound Library Immunology/Inflammation Compound Library Transcription Factor-Targeted Compound Library Cell Cycle Compound Library NO PAINS Compound Library

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Keywords

YK-4-279 1037184-44-3 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis chiral YK 4 279 anti-proliferation Inhibitor YK4279 inhibit breast pancreatic enantiomer prostate mice ESFT inhibitor

 

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