BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
体外研究
BMS453 (1 μM; 11 hours; 184 and HMEC cells) treatment inhibits the proliferation of normal breast cell growth without significantly inducing apoptosis.
BMS453 (1 μM; 5 days; 184 and HMEC cells) treatment inhibits normal breast cell proliferation by causing G1 arrest.
BMS453 (1 μM; 24-72 hours; 184 cells) treatment induces Rb hypophosphorylation and decrease CDK2 kinase activity. BMS453 increases total p21 protein levels and CDK2-bound p21 protein, but does not change CDK4-bound p21.
BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
Cell Proliferation Assay
Cell Line:
Normal human mammary epithelial cells (184 and HMEC)
Concentration:
1 μM
Incubation Time:
11 hours
Result:
Inhibited H-thymidine uptake in normal breast cells (184 and HMEC) by 40 %.
Cell Cycle Analysis
Cell Line:
Normal human mammary epithelial cells (184 and HMEC)
Concentration:
1 μM
Incubation Time:
5 days
Result:
Increased the proportion of cells in G0/G1 phase and decreased the proportion of cells in S phase.
Western Blot Analysis
Cell Line:
184 cells
Concentration:
1 μM
Incubation Time:
24 hours, 48 hours, 72 hours
Result:
Induced Rb hypophosphorylation and decrease CDK2 kinase activity.
分子式
C27H24O2
分子量
380.48
CAS号
166977-43-1
运输条件
Room temperature in continental US; may vary elsewhere.