PhiKan 083 hydrochloride

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PhiKan 083 hydrochloride  纯度: ≥99.0%

PhiKan 083 hydrochloride 是一种咔唑衍生物，可以稳定 p53 的突变体 Y220C，Kd 值为 167 μM，在 Ln229 细胞中，相对亲和力 (Kd) 为 150 μM；PhiKan 083 可用于癌症研究。

PhiKan 083 hydrochloride

PhiKan 083 hydrochloride Chemical Structure

CAS No. : 1050480-30-2

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1 mg ￥1000 In-stock
5 mg ￥1200 In-stock
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生物活性

PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], and a relative binding affinity (Kd) of 150 μM in Ln229 cells[3].

IC50 & Target

Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]
体外研究
(In Vitro)

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3].
PhiKan 083 slows down its thermal denaturation rate[2].
PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells[3].
PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W)[3].

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: Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells
Concentration: 125 μM
Incubation Time: 48 hours
Result: Caused ∼70 ± 5% reduction in cell viability of variants of Ln229 cells.

分子量

274.79

Formula

C16H19ClN2
CAS 号

1050480-30-2
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (227.45 mM; ultrasonic and warming and heat to 60°C)

H2O : 2 mg/mL (7.28 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6391 mL 18.1957 mL 36.3914 mL
5 mM 0.7278 mL 3.6391 mL 7.2783 mL
10 mM 0.3639 mL 1.8196 mL 3.6391 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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Boeckler FM, et al. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5.

    [2]. Rauf SM, et al. Effect of Y220C mutation on p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013 Jan;32(1):68-74.

    [3]. Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511.

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