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Toyocamycin

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Chemical Structure| 606-58-6 同义名 : Vengicide
CAS号 : 606-58-6
货号 : A178051
分子式 : C12H13N5O4
纯度 : 95%
分子量 : 291.263
MDL号 : MFCD00866513
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(360.5 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Toyocamycin is an adenosine analogue produced by Streptomyces diastatochromogenes and can be used as an XBP1 inhibitor.Toyocamycin blocks RNA synthesis and ribosomal function and induces apoptosis.Toyocamycin affects the IRE1α-XBP1 pathway and inhibits XBP1 mRNA. Toyocamycin affects the IRE1α-XBP1 pathway and inhibits the cleavage of XBP1 mRNA with an IC50 value of 80 nM, and also affects the autophosphorylation of IRE1α. 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 ER stress-induced activation of the IRE1α-XBP1 pathway[1][2][3].Toyocamycin inhibits the constitutive activation of XBP1 in MM cell lines at concentrations of 0-0.3 μM for 24 h[1] .Toyocamycin inhibited the enzymatic activity of CDK9 in colon cancer cell lines at a concentration of 250 nM for 48 hours. In contrast, at concentrations ranging from 0.05 nM to 50 μM for 48 and 72 hours, Toyocamycin did not cause immediate cytotoxicity in YB5 and HCT116 cells with cell viability greater than 50%, but resulted in eradication of the cancer cells after 2 weeks following a 10 nM treatment for 24 hours[2] .Toyocamycin induces apoptosis in PC-3 cells via the mitochondrial pathway at concentrations ranging from 0-100 nM for 24 or 48 hours[3] .At 60 nM for 0-48 h, Toyocamycin promotes p38/ERK MAPK activation and regulates ROS-mediated apoptosis by inhibiting p38 on ERK MAPK[3] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.17mL

3.43mL

1.72mL

34.33mL

6.87mL

3.43mL
参考文献

[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.

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

[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.