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

Toyocamycin  (Synonyms: Vengicide)

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

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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
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10 mg USD 75 In-stock
50 mg USD 260 In-stock
100 mg USD 450 In-stock
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Based on 5 publication(s) in Google Scholar

Toyocamycin Related Antibodies

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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].

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

Toyocamycin Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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

Streptomyces diastatochromogenes
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (343.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

COA (250 KB) HNMR (240 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4334 mL 17.1668 mL 34.3336 mL 85.8340 mL
5 mM 0.6867 mL 3.4334 mL 6.8667 mL 17.1668 mL
10 mM 0.3433 mL 1.7167 mL 3.4334 mL 8.5834 mL
15 mM 0.2289 mL 1.1445 mL 2.2889 mL 5.7223 mL
20 mM 0.1717 mL 0.8583 mL 1.7167 mL 4.2917 mL
25 mM 0.1373 mL 0.6867 mL 1.3733 mL 3.4334 mL
30 mM 0.1144 mL 0.5722 mL 1.1445 mL 2.8611 mL
40 mM 0.0858 mL 0.4292 mL 0.8583 mL 2.1458 mL
50 mM 0.0687 mL 0.3433 mL 0.6867 mL 1.7167 mL
60 mM 0.0572 mL 0.2861 mL 0.5722 mL 1.4306 mL
80 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0729 mL
100 mM 0.0343 mL 0.1717 mL 0.3433 mL 0.8583 mL
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Toyocamycin Related Classifications

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.

Keywords:

Toyocamycin606-58-6VengicideIRE1FungalAntibioticApoptosisCDKInositol requiring enzyme 1Cyclin dependent kinaseadenosine analogRNA synthesisribosome functionmRNA cleavageCDKsCDK9 inhibitortoyocamycindrug screeningepigeneticscancerRNA Pol II phosphorylationmolecular dockingextracellular signal-regulated kinasesreactive oxygen speciesInhibitorinhibitorinhibit

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