BMS-189453

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-189453 (BMS189453, BMS453) 是一种合成类维生素A，可作为 RARβ 的激动剂以及 RARα 和 RARγ 的拮抗剂。

BMS-189453 (BMS189453, BMS453) is a synthetic retinoid that acts as an agonist of RARβ and an antagonist of RARα and RARγ; binds to RAR receptors and transrepresses AP-1, inhibits the growth of normal breast cells (HMEC and 184) and T47D breast cancer cells; increases p21, decrease CDK2 kinase activity, which in turn leads to hypophosphorylation of Rb and G1 arrest. Rheumatoid Arthritis Discontinued.

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 μMIncubation Time:11 hours Result:Inhibited 3H-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 μMIncubation 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.

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BMS189453 | BMS453

Nuclear Receptor/Transcription Factor

RAR/RXR

RAR/RXR

Inflammation/Immunology

Rheumatoid Arthritis

166977-43-1

380.5

C27H24O2

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (43.81 mM)

O=C(O)C1=CC=C(/C=C/C2=CC=C3C(C)(C)CC=C(C4=CC=CC=C4)C3=C2)C=C1

Benzoic acid, 4-[(1E)-2-[5,6-dihydro-5,5-dimethyl-8-(phenylethynyl)-2-naphthalenyl]ethenyl]- (9CI)

(-20℃)

With Ice Pack

≥ 2 years