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

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 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.

For research use only. We do not sell to patients.

TC8026

TC8026 Chemical Structure

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Description

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 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].

In Vivo

TC8026 (Compound 30z) (10-40 mg/kg; i.p.; once daily; 7 consecutive days) is well-tolerated in male C57BL/6 mice, with no observable liver or kidney toxicity[1].
Compound 30z (120-180 mg/kg; i.p.; single dose) exhibits no acute toxicity in male C57BL/6 mice, with no observable liver or kidney injury[1].
Compound 30z (40 mg/kg; i.p.; once daily) significantly inhibits subcutaneous U251 glioblastoma xenograft growth in female athymic nude mice with good in vivo tolerability[1].

MedChemExpress (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.
Molecular Weight

289.72

Formula

C14H12ClN3O2
SMILES

O=C(N1CC#CC(NCC)=O)C2=C(N=C1Cl)C=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TC8026 Related Classifications

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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.

Keywords:

TC8026TC 8026TC-8026PDIApoptosisProtein Disulfide IsomerasesU251 glioblastoma xenograftb' domainglioblastomaC57BL/6 miceendoplasmic reticulum stressapoptosisProtein disulfide isomerasefemale athymic nude miceInhibitorinhibitorinhibit

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