Toyocamycin  (Synonyms: Vengicide)

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^[1][2][3].

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^[1].
Toyocamycin (0-0.3 μM; 24 h) inhibits constitutive activation of XBP1 in MM cell lines^[1].
Toyocamycin (250 nM; 48 h) inhibits CDK9 enzymatic activity in colon cancer cell lines^[2].
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^[2].
Toyocamycin (0-100 nM; 24 or 48 h) induces apoptosis via mitochondrial pathway in PC-3 cells^[3].
Toyocamycin (60 nM; 0-48 h) promotes p38/ERK MAPK activation and regulates ROS-mediated apoptosis by inhibition of p38 on ERK MAPK^[3].

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

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)^[1].

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

291.26

Solid

C₁₂H₁₃N₅O₄

606-58-6

O[C@H]1[C@@H](O[C@H](CO)[C@H]1O)N2C3=C(C(N)=NC=N3)C(C#N)=C2

Room temperature in continental US; may vary elsewhere.

• [1]. Toyocamycin, et al. Identification of Toyocamycin, an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing. Blood Cancer J. 2012 Jul;2(7):e79.  [Content Brief]

  [2]. Pandey S, et al. Selective CDK9 Inhibition by Natural Compound Toyocamycin in Cancer Cells. Cancers (Basel). 2022 Jul 8;14(14):3340.   [Content Brief]

  [3]. Park SG, et al. Toyocamycin induces apoptosis via the crosstalk between reactive oxygen species and p38/ERK MAPKs signaling pathway in human prostate cancer PC-3 cells. Pharmacol Rep. 2017 Feb;69(1):90-96.  [Content Brief]