TPh A(Synonyms: Triphenyl Compound A)

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TPh A (Synonyms: Triphenyl Compound A) 纯度: 99.76%

TPh A (Triphenyl Compound A) 是核蛋白 pirin 的有效抑制剂,其 Ki 值为0.6 uM。TPh A 破坏 Bcl3-pirin 复合物的形成。TPh A 可作为相关的小分子工具调控细胞内的 Pirin。

TPh A(Synonyms: Triphenyl Compound A)

TPh A Chemical Structure

CAS No. : 21306-65-0

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生物活性

TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells[1].

体外研究
(In Vitro)

The Pirin is a nuclear protein with the nuclear factor I/CCAAT box transcription factor (NFI/CTF). Pirin proteins are highly conserved between mammals, plants, fungi, and prokaryotic organisms and are considered to belong to the cupin superfamily.
TPh A (20 μM; 5 hours) reduces the amount of pirin-bound Bcl3 and inhibits the interaction between pirin and Bcl3 in HEK293T cells in a glutathione S-transferase (GST) pulldown assay (HEK293T cells are transfected with vectors that encoded bcl3-Myc and pirin-His6 for 43 h of transfection)[1].
TPh A (0-100 μM; 48 hours) does not exert any potent cytotoxic activity against many human cancer cell lines, it against MCF7, MDA-MB231, HeLa, DU145, HepG2, A549, HT1080, WM266-4, and SK-MEL-28 cells with IC50 values >50 μM, and exhibits IC50 values of 27 μM, 20 μM and 26 μM for PC3 HL60 and HT29 cells, respectively[1].
TPhA (0-50 μM; 48 hours) inhibits cell migration in WM266-4 cells, SK-MEL-28 cell in a concentration-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF7, MDA-MB231, HeLa, DU145, HepG2, A549, HT1080, WM266-4, and SK-MEL-28 cells
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Did not exert any potent cytotoxic activity against many human cancer cell lines.

分子量

399.53

Formula

C21H21NO3S2

CAS 号

21306-65-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (625.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5029 mL 12.5147 mL 25.0294 mL
5 mM 0.5006 mL 2.5029 mL 5.0059 mL
10 mM 0.2503 mL 1.2515 mL 2.5029 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Isao Miyazaki, et al. A Small-Molecule Inhibitor Shows That Pirin Regulates Migration of Melanoma Cells. Nat Chem Biol. 2010 Sep;6(9):667-73.

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