UC2288 是新型的、细胞通透性、口服有效的p21衰减试剂,基于索拉非尼的结构合成。在不依赖 于p53的情况下,它可以下调 p21 mRNA 的表达,降低 p21 蛋白水平,对 p21 蛋白的稳定性影响很小。它对VEGFR2 和 Raf 激酶没有抑制作用,即使在 10 μM。
产品描述
UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.
体外活性
UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1].
体内活性
UC2288 (10 mg/kg; i.p.) attenuates MPTP-induced behavioral impairment, prevents activation of MAPK pathway in the MPTP-treated mice brain. MPTP treatment raises TNF-α, IL-6 and IL-1β levels in MPTP treated mice brain, but UC2288 signicantly decreases MPTP-induced TNF-α, IL-6 levels, but IL-1β is not decreased in brain[2].UC2888 (15 mg/kg; oral) co-treatment with imetelstat significantly suppresses tumor growth and does not effect mice weight[3].
Cas No.
1394011-91-6
分子式
C20H18ClF6N3O2
分子量
481.82
储存和溶解度
DMSO:48 mg/mL (99.62 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years