1. Cell Cycle/DNA Damage
    Anti-infection
    Apoptosis
  2. IRE1
    Fungal
    Antibiotic
    Apoptosis
    CDK
  3. Toyocamycin

Toyocamycin  (Synonyms: Vengicide)

Cat. No.: HY-103248 Purity: 99.90%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Toyocamycin Chemical Structure

Toyocamycin Chemical Structure

CAS No. : 606-58-6

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10 mM * 1 mL in DMSO USD 55 In-stock
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Based on 1 publication(s) in Google Scholar

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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[1][2][3].

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)

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].

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

Western Blot Analysis[1]

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[3]

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[3]

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%.
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].

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

Animal Model: SCID mice injected with human multiple myeloma (MM) cells[1]
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).
Molecular Weight

291.26

Formula

C12H13N5O4

CAS No.
SMILES

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

Structure Classification
Source

Streptomyces diastatochromogenes

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (343.34 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4334 mL 17.1668 mL 34.3336 mL
5 mM 0.6867 mL 3.4334 mL 6.8667 mL
10 mM 0.3433 mL 1.7167 mL 3.4334 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.90%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Toyocamycin
Cat. No.:
HY-103248
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