BRD4 Inhibitor-18

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BRD4 Inhibitor-18 

BRD4 Inhibitor-18 是一种高效的 BRD4 抑制剂，IC50 为 110 nM。BRD4 Inhibitor-18 具有疏水乙酰环戊基侧链。BRD4 Inhibitor-18 能显著抑制 BRD4 水平较高的 MV-4-11 细胞的增殖，具有促进细胞凋亡 (apoptosis) 和抑制 G0/G1 周期的活性。

BRD4 Inhibitor-18

BRD4 Inhibitor-18 Chemical Structure

CAS No. : 2451219-73-9

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生物活性

BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity[1].

IC50 & Target

BRD4

110 nM (IC50)

体外研究
(In Vitro)

BRD4 Inhibitor-18 (compound 13f) (0-10 μM; 72 hours) can suppress the proliferation of HL-60 and MV-41 cells[1].
BRD4 Inhibitor-18 (0.5 and 5 μM; 12 hours) significantly arrests MV-4-11 cells in G1 phase in a dose-dependent manner[1].
BRD4 Inhibitor-18 (0.5 and 5 μM; 12 hours) effectively induces apoptosis of MV-4-11 cells in a dose-dependent manner[1].
BRD4 Inhibitor-18 (0.5 and 5 μM; 4 hours) inhibits the expression of c-Myc protein in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: HL-60 and MV-4-11[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Suppressed the proliferation of HL-60 and MV-41 cells with IC50s of 5.52 μM and 0.42 μM.

Cell Cycle Analysis

Cell Line: MV-4-11 cells[1]
Concentration: 0.5 and 5 μM
Incubation Time: 12 hours
Result: Significantly arrested MV-4-11 cells in G1 phase, with the G0/G1 cell proportions of 50.87% and 70.66% at 0.5 and 5 μM.

Apoptosis Analysis

Cell Line: MV-4-11 cells[1]
Concentration: 0.5 and 5 μM
Incubation Time: 12 hours
Result: Effectively induced apoptosis of MV-4-11 cells, with apoptosis rates of 12.39% and 73.24% at at 0.5 and 5 μM.

Western Blot Analysis

Cell Line: MV-4-11 cells[1]
Concentration: 0.5 and 5 μM
Incubation Time: 4 hours
Result: Inhibited the expression of c-Myc protein in a dose-dependent manner.

分子量

496.02

Formula

C26H26ClN3O3S
CAS 号

2451219-73-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Li Q, Li J, Cai Y, et al. Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. Bioorg Med Chem. 2020;28(15):115601.

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