934358-00-6
中文名稱
Casein Kinase II Inhibitor III
英文名稱
Casein Kinase II Inhibitor III
CAS
934358-00-6
分子式
C9H4Br4O2
分子量
463.74
MOL 文件
934358-00-6.mol
934358-00-6 結(jié)構(gòu)式
基本信息
中文別名
化合物TBCA 英文別名
TBCATetrabromocinnamic acid
SVJQCVOKYJWUBC-OWOJBTEDSA-N
Casein Kinase II Inhibitor III
Casein Kinase II Inhibitor III, TBCA
(E)-3-(2,3,4,5-Tetrabromophenyl)acrylic Acid
InSolution? Casein Kinase II Inhibitor III, TBCA
(2E)-3-(2,3,4,5-Tetrabromophenyl)-2-propenoic acid
2-Propenoic acid, 3-(2,3,4,5-tetrabromophenyl)-, (2E)-
Casein Kinase II Inhibitor III, TBCA - CAS 934358-00-6 - Calbiochem
物理化學(xué)性質(zhì)
熔點189.2-191.2 °C
沸點490.8±45.0 °C(Predicted)
密度2.443±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL，澄清
酸度系數(shù)(pKa)3.83±0.16(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
TBCA 是一種高選擇性的酪蛋白激酶II CK2 抑制劑，IC50 為 110 nM，Ki 為 77 nM。TBCA 對 CK1、DYRK1A 和 其它 27 個激酶表現(xiàn)出選擇性。靶點
|
CK2 110 nM (IC 50 ) |
CK2 77 nM (Ki) |
體外研究
TBCA (0-100 μM; 24 hours) shows a drastic effect on Jurkat cells viability.
TBCA also inhibits CK2 double mutant (Val66 Ile174) with an IC
50
of 0.68 μM.
TBCA dose-dependently inhibits platelet aggregation and secretion induced by various agonists including 2-MeSADP, AYPGKF, SFLLRN, and CRP. TBCA also inhibits phosphorylation of PDK1, Akt, and GSK3β induced by AYPGKF.
Cell Viability Assay
| Cell Line: | Jurkat cells |
| Concentration: | 0-100 μM |
| Incubation Time: | 24 hours |
| Result: | The viability of Jurkat cells was reduced. |