172286-77-0
中文名稱
Homocarbonyltopsentin
英文名稱
Homocarbonyltopsentin
CAS
172286-77-0
分子式
C21H14N4O3
分子量
370.36
MOL 文件
172286-77-0.mol
172286-77-0 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13723 英文別名
PK4C9Homocarbonyltopsentin
Methanone, [2-[(6-hydroxy-1H-indol-3-yl)carbonyl]-1H-imidazol-4-yl]-1H-indol-3-yl- (9CI)
物理化學(xué)性質(zhì)
熔點(diǎn)>210 °C
沸點(diǎn)801.2±75.0 °C(Predicted)
密度1.539±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 125 mg/mL (337.51 mM)
酸度系數(shù)(pKa)7.50±0.10(Predicted)
形態(tài)Solid
顏色White to yellow
常見(jiàn)問(wèn)題列表
生物活性
Homocarbonyltopsentin (PK4C9) 是結(jié)合 TSL2 的小分子化合物，高羰基形成蛋白，
與 TSL2 的 pentaloop 構(gòu)象結(jié)合并促進(jìn)向三葉草構(gòu)象的轉(zhuǎn)變，增強(qiáng) SMN2 外顯子7 (E7) 剪接，EC50 值為 16 μM。體外研究
Homocarbonyltopsentin (PK4C9) (10-40 μM; 24 hours) shows an up to 5.2-fold decrease in the expression of E7-excluding SMN2 isoforms, and up to three-fold increase in E7-including isoforms in GM03813C cells. Homocarbonyltopsentin (PK4C9) (40 μM; 24 hours) increased 1.5-fold SMN protein expression compared to GM03813C cells treated with DMSO.
RT-PCR
| Cell Line: | GM03813C (SMA) cells; GM03814B fibroblasts cells |
| Concentration: | 10-40 μM |
| Incubation Time: | 24 hours |
| Result: | E7 inclusion reached a maximum of 91% (25% increase, DMSO-treated cells). |
Western Blot Analysis
| Cell Line: | GM03813C (SMA) cells; GM03814B fibroblasts cells |
| Concentration: | 40 μM |
| Incubation Time: | 24 hours |
| Result: | Increased SMN protein in SMA cells. |