Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM.

Solid

CDK9/cyclinT1
79 nM (IC50)CDK7/Mat1/cyclinH1

Toyocamycin (0-0.3 μM; 4 h) inhibits ER stress-induced XBP1 mRNA splicing, and selectively inhibits the ER stress-induced activation of the IRE1α-XBP1 pathway.
Toyocamycin (0-0.3 μM; 24 h) inhibits constitutive activation of XBP1 in MM cell lines.
Toyocamycin (250 nM; 48 h) inhibits CDK9 enzymatic activity in colon cancer cell lines.
Toyocamycin (0.05 nM-50 μM; 48 h and 72 h) doesn’t trigger immediate cytotoxicity against YB5 and HCT116 cells with cell viability above 50%, but results eradication of cancer cells 2 weeks later at 10 nM for 24 h treatment.
Toyocamycin (0-100 nM; 24 or 48 h) induces apoptosis via mitochondrial pathway in PC-3 cells.
Toyocamycin (60 nM; 0-48 h) promotes p38/ERK MAPK activation and regulates ROS-mediated apoptosis by inhibition of p38 on ERK MAPK.
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Toyocamycin (0.5 mg/kg, 1.0 mg/kg; i.p.; twice a week; 2 weeks) shows anti-tumor activity in a xenograft model with human multiple myeloma (MM) cells, while the anti-tumor effect enhanced by Bortezomib (HY-10227).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
1 fwb

Room temperature or refrigerated transport.

Powder； -20°C； 3 years；In solvent； -80°C； 6 months；

Antibiotics
Other

Streptomyces diastatochromogenes

体外研究:
DMSO : 50 mg/mL(171.67 mM;ultrasonic and warming and heat to 60°C)
配制储存液