YK-4-279

SKU: orb1222912

Description

YK-4-279 is a ETV1 inhibitor, which inhibitor protein-protein interactions between ES-FLI1 and RHA.YK-4-279 effectively antagonizes EWS-FLI1 induced leukemia in a transgenic mouse model. YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1. YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model.(In Vitro):YK-4-279 (3-30 μM; overight) dissociates EWS-FLI1 from RHA in Ewing’s sarcoma family tumor (ESFT) cells.YK-4-279 (3-30 μM; 14 h) nearly eliminates cyclin D1 in TC32 cells.YK-4-279 (3-30 μM; 72 h) potently and specifically inhibits ESFTs.YK-4-279 (50 μM; 6 h) induces substantial apoptosis of ESFT cells.YK-4-279 (0.1-30 μM; 72 h) inhibits the growth of ESFT, prostate, breast and pancreatic cancer cells.(In Vivo):YK-4-279 (1.5 mg; i.p. once) inhibited ESFT tumor growth.

Key Properties

• CAS Number: 1037184-44-3
• MW: 366.2
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₃Cl₂NO₄
• SMILES: COC1=CC=C(C=C1)C(=O)CC1(O)C(=O)NC2=C(Cl)C=CC(Cl)=C12
• Target: RNA helicase A
• Solubility: DMSO : 25 mg/mL. 68.27 mM

Bioactivity

• In Vivo:
  Animal model: Beige mice with orthotopic ESFT and ESFT xenografts. Dosage: 1.5 mg. Administration: Intraperitoneal injection; 1.5 mg once. Result: Effectively redeced tumor volume of CHP100 and ESFT xenografts (TC71 and CHP100).
• In Vitro:
  Cell Viability Assay Cell line: TC32, ES925, GUES1, TC71, A673, A4573, CHP100, PANC1, ASP1, MCF-7, MDA-MB-231, PC-3, HFK and HEC cell lines. Concentration: 3-30 μM. Incubation time: 72 h. Result: Inhibited cell growth with IC50s of 900 nM, 1 μM and 8 μM for TC32, ES925 and GUES1 cells, respectively. Apoptosis Analysis Cell line: TC32, HEK, HEC and HFK cell lines. Concentration: 50 μM. Incubation time: 6 h. Result: Induced apoptosis of ESFT cells and increased caspase-3 activity. Cell Viability Assay Cell line: TC32, TC71, RDES, SKES, MMH-ES-1, STA-ET 7.2, A4573, PC3, MCF7, MDA-MB-231, PANC1 and ASPC1 cell lines Concentration: 0.1-30 μM Incubation time: 72 h. Result: Inhibited cell growth with IC50s of 0.94, 1.83, 1.03, 0.33, 0.94, 0.60, 1.46, 4.95, 22.82, 0.82, 1.514 and 14.28 μM for TC32, TC71, RDES, SKES, MMH-ES-1, STA-ET 7.2, A4573, PC3, MCF7, MDA-MB-231, PANC1 and ASPC1 cells, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YK-4-279 | YK4-279 | YK 4-279 | YK 4279

Quick Database Links

Gene Symbol

RNA helicase A