TMBIM6 antagonist-1是一种有潜力的 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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| 描述 | TMBIM6 is a Ca2+ channel-like protein that lowers the steady-state [Ca2+]ER. Overexpression of TMBIM6 promotes cancer metastasis by regulating cell mobility and invasiveness and glucose metabolism. TMBIM6 antagonist-1 is a potential TMBIM6 antagonist which prevents TMBIM6 binding to mTORC2, thus decreases mTORC2 activity, and it also regulates TMBIM6-leaky Ca2+. TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibited cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC50 values of 1.7 ± 0.1 μM, 2.6 ± 0.4 μM, 2.6 ± 0.5 μM and 2.4 ± 0.4 μM, respectively. TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreased cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells. In vivo, TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaired cell-driven tumor growth in Six- to eight-week BklNbt:BALB/c/nu/nu old mice[1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.73mL 0.75mL 0.37mL |
18.64mL 3.73mL 1.86mL |
37.28mL 7.46mL 3.73mL |
|
| CAS号 | 123134-61-2 |
| 分子式 | C15H12N2O3 |
| 分子量 | 268.27 |
| SMILES Code | O=C(C1=CC=CC=C1N)/C=C/C2=CC=CC([N+]([O-])=O)=C2 |
| MDL No. | MFCD32858323 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | LRMPAVQDWGDIBD-CMDGGOBGSA-N |
| Pubchem ID | 11425639 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(186.38 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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