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  3. TMBIM6 antagonist-1

TMBIM6 antagonist-1 

目录号: HY-137175
产品使用指南

TMBIM6 antagonist-1 是一个有潜力的 TMBIM6 拮抗剂,抑制 TMBIM6 与 mTORC2 结合,降低 mTORC2 活性,调节TMBIM6 释放 Ca2+

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TMBIM6 antagonist-1 Chemical Structure

TMBIM6 antagonist-1 Chemical Structure

CAS No. : 123134-61-2

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Description

TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+[1].

In Vitro

TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibits cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC50 values of 1.7 ± 0.1 μM for HT1080, 2.6 ± 0.4 μM for MCF cells, 2.6 ± 0.5 μM for MDA-MB-231 cells, and 2.4 ± 0.4 μM for SKBR3 cells, respectively[1].
TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreases cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, not TMBIM6 KO HT1080 cells[1].

Cell Viability Assay[1]

Cell Line: HT1080, MCF7, MDA-MB-2341 and SKBR3 cells.
Concentration: 0.5-10 μM.
Incubation Time: 3 days.
Result: Inhibited cell viability.

Western Blot Analysis[1]

Cell Line: WT and TMBIM6 KO HT1080 cells.
Concentration: 0, 2, 5 μM.
Incubation Time:
Result: Downregulated the protein levels of AKT-pS473.
In Vivo

TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaires cell-driven tumor growth[1].

Animal Model: Six- to eight-week BklNbt:BALB/c/nu/nu old mice (HT1080 and MDA-MB-231 cells)[1].
Dosage: 1 mg/kg.
Administration: IP 5 days per week during 25 days.
Result: Impaired cell-driven tumor growth.
Molecular Weight

268.27

Formula

C₁₅H₁₂N₂O₃

CAS No.

123134-61-2

SMILES

O=C(C1=CC=CC=C1N)/C=C/C2=CC=CC([N+]([O-])=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7276 mL 18.6379 mL 37.2759 mL
5 mM 0.7455 mL 3.7276 mL 7.4552 mL
10 mM 0.3728 mL 1.8638 mL 3.7276 mL
*

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References
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Keywords:

TMBIM6 antagonist-1mTORMammalian target of RapamycinCa2+TMBIM6HT1080MCF7MDA-MB-2341SKBR3Inhibitorinhibitorinhibit

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产品名称:
TMBIM6 antagonist-1
目录号:
HY-137175
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