1. Apoptosis
  2. Ferroptosis
  3. FA16

FA16 是一种特异、代谢稳定的铁死亡 (ferroptosis) 诱导剂 (IC50=1.26 μM; HT1080 cells),是 2-(三氟甲基) 苯并咪唑的衍生物。胱氨酸/谷氨酸反转运蛋白 (system Xc-) 介导了细胞内谷氨酸和细胞外胱氨酸的交换,FA16 通过抑制 system Xc- 行使功能。FA16 也能够在 HepG2 异种移植瘤模型中显著抑制肿瘤生长。

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FA16 Chemical Structure

FA16 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc-), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model[1].

体外研究
(In Vitro)

FA16 (1 μM; 5 min) 在大鼠和人肝微粒体中具有满意的代谢稳定性[1]
FA16 (5 μM; 10 h) 诱导 HT1080 细胞中脂质 ROS 积累并抑制谷氨酸释放[1]
FA16 (5 μM; 24 h) 结果线粒体萎缩,膜密度增大,符合铁衰相关的形态特征[1]
FA16 (10 μM; 24 h) 诱导的铁死亡能够被铁脱落抑制剂 Fer-1、Trolox 或 DFO 挽救,而凋亡或坏死抑制剂则对其无效[1]

Parameter Microsomal stability (T1/2 min) Intrinsic clearance (μL/min/ mg protein)
Human 15.6 88.6
Rat 10.4 132.8

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

Cell Viability Assay[1]

Cell Line: Human cancer cell lines: Clear-cell renal cell carcinoma cells (786-O), breast cancer cells (MDA-MB-231), cervical cancer cells (HeLa), hepatocellular carcinoma cells (HepG2), melanoma cells (A375), and prostate cancer cells (DU145); Human normal cell lines: cardiomyocytes (AC16), colon mucosal epithelial cells (NCM460), embryonic kidney cells (293T), and hepatic cells (LO2)
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Inhibited cell growth with IC50s of 0.7 μM (786-O), 4.34 μM (MDA-MB-231), 1.91 μM (HeLa), 1.33 μM (HepG2), 2.31 μM (A375), and 1.64 μM (DU145), respectively.

Immunofluorescence[1]

Cell Line: HT1080 cells
Concentration: 5 μM
Incubation Time: 10 hours
Result: Significantly induced lipid ROS accumulation, as indicated by the great enhancement in green fluorescence intensity.

RT-PCR[1]

Cell Line: HT1080 cells
Concentration: 0.5 μM, 1 μM, and 5 μM
Incubation Time: 6 hours and 18 hours
Result: Increased the system Xc- component SLC7A11, ChaC GSHspecific γ-glutamylcyclotransferase 1 (CHAC1), but little changed GPX4.
体内研究
(In Vivo)

FA16 (15 或 30 mg/kg; 腹腔注射; 隔天给药, 共 21 天) 在 786-O 异种移植物小鼠模型中显著抑制肿瘤生长,安全性好 (不引起体重下降),还诱导肿瘤组织中发生铁死亡[1]

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

Animal Model: BALB/c nude mice bearing HepG2 tumors (s.c.)[1]
Dosage: 15 or 30 mg/kg
Administration: Intraperitoneal injection; every other for 21 days
Result: Significantly inhibited tumor growth with a tumor growth inhibition (TGI) value of 47.6% and 77.1% at 15 and 30 mg/ kg, respectively.
分子量

466.52

Formula

C22H25F3N4O2S

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

FA16 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.

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