Toyocamycin

SKU: orb1219280

Description

Toyocamycin is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). Toyocamycin induces apoptosis.

Key Properties

• CAS Number: 606-58-6
• MW: 291.26
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₃N₅O₄
• SMILES: O[C@H]1[C@@H](O[C@H](CO)[C@H]1O)N2C3=C(C(N)=NC=N3)C(C#N)=C2
• Target: XBP1
• Solubility: DMSO:100 mg/mL (343.34 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: SCID mice injected with human multiple myeloma (MM) cells. Dosage: 0.5 mg/kg, 1.0 mg/kg. Administration: Intraperitoneal injection; twice a week; 2 weeks. Result: Reduced the tumor volume significantly. Showed enhancing anti-tumor activity represented as smaller tumor volumes when compared with Bortezomib (HY-10227).
• In Vitro:
  Western blot analysis. Cell line: HeLa, HEK293. Concentration: 0, 0.03, 0.1, 0.3 μM Incubation time: 4 hours. Result: Suppressed neither tunicamycin-induced ATF6 nor PERK activation. Inhibited IRE1α-induced XBP1 mRNA cleavage without affecting IRE1α phosphorylation on Ser724. Western blot analysis. Cell line: Human prostate cancer PC-3 cells. Concentration: 60 nM. Incubation time: 12, 24, 36, 48 hours. Result: Suppressed the phosphorylation level of AKA, while decreasing the phosphorylation level of ERK and p38. Cell Viability Assay Cell line: PC-3 and RWPE-1 cells. Concentration: 0, 20, 40, 60, 80, 100 nM. Incubation time: 24 or 48 hours. Result: Inhibted cell viability and induced cell apoptosis by 62%.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Vengicide

Quick Database Links

Gene Symbol

XBP1