2. Autophagy Apoptosis
  3. Autophagy Apoptosis
  4. ARN5187

ARN5187 是一种亲溶酶体 REV-ERBβ 配体，抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 显示出溶酶体效力和细胞毒性。 ARN5187 诱导细胞凋亡 (apoptosis)。

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ARN5187 Chemical Structure

ARN5187 Chemical Structure

CAS No. : 1287451-26-6

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ARN5187 的其他形式现货产品:

Customer Review

Other Forms of ARN5187:

ARN5187 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis[1][2].

IC50 & Target

REV-ERBβ[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BT-474 IC50
10 μM
Compound: 1, ARN5187
Lysosomotropic activity in human BT474 cells assessed as reduction in lysosomal pH incubated for 24 hrs by lysosomotropy assay
Lysosomotropic activity in human BT474 cells assessed as reduction in lysosomal pH incubated for 24 hrs by lysosomotropy assay
[PMID: 26135471]
BT-474 IC50
23.5 μM
Compound: 40; ARN5187
Cytotoxicity against human BT474 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human BT474 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 29211480]
BT-474 IC50
30.14 μM
Compound: 1, ARN5187
Cytotoxicity against human BT474 cells assessed as reduction in cell number incubated for 72 hrs
Cytotoxicity against human BT474 cells assessed as reduction in cell number incubated for 72 hrs
[PMID: 26135471]
HEK293 IC50
17.5 μM
Compound: 1, ARN5187
Inhibition of REV-ERBbeta (unknown origin) expressed in HEK293 cells incubated for 24 hrs assessed as inhibition of receptor-mediated transcriptional repression by REV-ERB luciferase reporter assay
Inhibition of REV-ERBbeta (unknown origin) expressed in HEK293 cells incubated for 24 hrs assessed as inhibition of receptor-mediated transcriptional repression by REV-ERB luciferase reporter assay
[PMID: 26135471]
HMEC IC50
> 100 μM
Compound: 1, ARN5187
Cytotoxicity against HMEC cells assessed as reduction in cell number incubated for 72 hrs
Cytotoxicity against HMEC cells assessed as reduction in cell number incubated for 72 hrs
[PMID: 26135471]
体外研究
(In Vitro)

ARN5187 (compound 1) (0-100 µM; 48 h) shows cytotoxicity with EC50 of 23.5 µM in BT-474 cells and IC50 of 30.14 µM, >100 µM for BT-474 and HMEC cells, respectively[1][2].
ARN5187 (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells[1].
ARN5187 (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity[1].
ARN5187 (50 µM; 24 h) shows autophagy inhibition[1].
ARN5187 (50 µM; 2, 8, 24 h) effects autophagy formation and maturation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ARN5187 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: BT-474 cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed cytotoxicity with EC50 of 23.5 µM.

RT-PCR[1]

Cell Line: BT-474 cells
Concentration: 25, 50 µM
Incubation Time:
Result: Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: BT-474 cells
Concentration: 50 µM
Incubation Time: 24 h
Result: Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.
分子量

397.53

Formula

C24H32FN3O
CAS 号
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.
纯度 & 产品资料
参考文献

ARN5187 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARN51871287451-26-6ARN 5187ARN-5187AutophagyApoptosisapoptosisBT-474 cellslysosomotropicchloroquineanticancerα-p62HEK-293 cellsInhibitorinhibitorinhibit

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