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Toyocamycin

MCE China：Toyocamycin

Brand：MedChemExpress (MCE)

Cat. No.HY-103248

CAS：606-58-6

Synonyms：Vengicide

Purity：99.78%

Storage：Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

In Vivo：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].

IC50 & Target：CDK9/cyclinT1 79 nM (IC50) CDK7/Mat1/cyclinH1 2.8 μM (IC50) CDK2/cyclinA 0.67 μM (IC50) Cdk4/cyclin D3 15 μM (IC50) cdk6/cyclin D3 >10 μM (IC50)

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References：

[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]