Application
一种致癌转录因子EWS-FLI1与RNA解旋酶A(RHA)结合的有效抑制剂。
YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis. IC50 value: Target: RNA Helicase A ES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a family of undifferentiated tumors that occur throughout the body. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 μM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
YK-4-279抑制尤因氏肉瘤家族肿瘤（ESFT）细胞的生长； YK-4-279诱导细胞凋亡。 IC50值：目标：RNA解旋酶ES-FLI1是一种在尤文氏肉瘤中发现的致癌融合蛋白，尤文氏肉瘤是一类未分化的肿瘤，遍布全身。 RNA解旋酶A（RHA）与ES-FLI1的结合可促进其致癌功能。 YK-4-279是ES-FLI1和RHA之间的蛋白质-蛋白质相互作用的抑制剂。 YK-4-279浓度为10μM时，会阻断RHA与ES-FLI1的结合，并诱导Ewing肉瘤细胞株的凋亡，其IC50值为0.5-2μM。 YK-4-279的剂量为1.5毫克/剂，可在用抑制剂治疗两周后减少尤因肉瘤原位异种移植物在小鼠体内的生长。
性质
| Iupac Name | 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1,3-dihydro-2H-indol-2-one |
| Inchi Code | 1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22) |
| Inchi Key | HLXSCTYHLQHQDJ-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport
