1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. PDI Apoptosis
  3. TC8026

TC8026 是一种靶向蛋白质二硫键异构酶 (PDI) 的变构-共价抑制剂,对人源 PDI IC50 为 7 μM。TC8026 可诱导内质网应激介导的细胞凋亡 (apoptosis)。TC8026 是经高通量筛选得到的 PDI 活性苗头化合物,可用于胶质母细胞瘤的研究。

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TC8026

TC8026 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC8026 is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI), with an IC50 of 7 μM against human PDI. TC8026 induces endoplasmic reticulum stress-mediated cell apoptosis (apoptosis). TC8026 is a hit compound with PDI inhibitory activity identified via high-throughput screening, and it can be used for the research of glioblastoma[1].

体内研究
(In Vivo)

TC8026 (Compound 30z) (10-40 mg/kg; i.p.; 每日 1 次; 7 d) 在雄性 C57BL/6 小鼠中耐受性良好,未观察到明显的肝毒性或肾毒性[1]
TC8026 (120-180 mg/kg; i.p.; 单剂量) 在雄性 C57BL/6 小鼠中无急性毒性,未观察到肝或肾损伤[1]
TC8026 (40 mg/kg; i.p.; 每日 1 次) 可显著抑制雌性无胸腺裸鼠体内皮下 U251 胶质母细胞瘤异种移植物的生长,且具有良好的体内耐受性[1]

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

Animal Model: C57BL/6 (male, 8 weeks old)[1]
Dosage: 10-40 mg/kg
Administration: i.p.; once daily; 7 consecutive days
Result: Exhibited normal body weight gain comparable to vehicle controls.
Maintained serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and blood urea nitrogen (BUN) levels within normal ranges with no significant differences from vehicle controls.
Animal Model: C57BL/6 (male, 8 weeks old)[1]
Dosage: 120-180 mg/kg
Administration: i.p.; single dose
Result: Showed no mortality or adverse clinical signs over the 7-day monitoring period.
Had body weight changes comparable to vehicle controls.
Maintained serum ALT, AST, and BUN levels within normal ranges with no significant differences from vehicle controls.
Animal Model: athymic nude (nu/nu) (female, 6 weeks old; subcutaneous glioblastoma xenograft model)[1]
Dosage: 40 mg/kg
Administration: i.p.; once daily
Result: Significantly suppressed subcutaneous U251 glioblastoma tumor growth compared to vehicle controls, as measured by reduced tumor volume over time and lower terminal tumor weights.
Had body weight changes comparable to vehicle controls, indicating good tolerability.
分子量

289.72

Formula

C14H12ClN3O2

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
  • 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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产品名称:
TC8026
目录号:
HY-181573
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