BMS453

生物活性体外研究 BMS453 试剂级价格

BMS453

CAS号:166977-43-1
英文名:BMS453
中文名:BMS453
CBNumber:CB51387459
分子式:C27H24O2
分子量:380.48
MOL File:166977-43-1.mol

BMS453化学性质

沸点 :560.9±50.0 °C(Predicted)
密度 :1.167±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: soluble10mg/mL, clear
形态 :powder
酸度系数(pKa) :4.27±0.10(Predicted)
颜色 :white to beige

BMS453性质、用途与生产工艺

生物活性 BMS453 (BMS-189453) 是一种合成类维生素 A，是一种 RARβ 激动剂和 RARα/RARγ 拮抗剂。BMS453 主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。

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 ³ 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.