XRP44X 是Ras诱导的转录激活的抑制剂,IC50为 10 nM,通过 FGF-2 抑制 Ras-ERK-1/2 通路激活。它抑制Elk3。它还对微管有影响。
产品描述
XRP44X is a potent inhibitor of Ras-Net (Elk-3) pathway.
体外活性
XRP44X is an indirect inhibitor of Net phosphorylation that acts upstream from Erk-1/2 activation. XRP44X inhibits luciferase activity with the IC50 of~10 nM[1].
XRP44X (10 nM) inhibits cell growth of HUVEC, NIH3T3, HCT-116, and NIH3T3–Ki-Ras cells[1].
XRP44X (100 nM) inhibits phosphorylation of Mek-1/2 and Raf-1[1].
体内活性
XRP44X may have therapeutic potential for refractory asthma[1].
XRP44X, an inhibitor of Ras/Erk activation of the transcription factor Elk3, inhibits tumor growth and metastasis in mice. XRP44X inhibits tumor growth and metastasis in nude mice. XRP44X decreases the growth of tumours and the formation of metastases in nude mice[2].
Cas No.
729605-21-4
分子式
C21H21ClN4O
分子量
380.87
别名
XRP 44 X;XRP-44X;XRP 44X;XRP-44-X
储存和溶解度
DMSO:36.67 mg/ml (96.27 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years