YK-4-279

Research use only, not for human use.

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

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.

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.

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).

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

Others

Other Targets

RNA helicase A

Cancer

——

1037184-44-3

366.2

C17H13Cl2NO4

>98% (HPLC)

DMSO : 25 mg/mL. 68.27 mM;

COC1=CC=C(C=C1)C(=O)CC1(O)C(=O)NC2=C(Cl)C=CC(Cl)=C12

4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indole-2-one

(-20℃)

With Ice Pack

≥ 2 years