Cat. No.: HY-103248

Toyocamycin

(Synonyms: Vengicide)

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

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.

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Pureté: 99.27%
CAS No.: 606-58-6
Formule: C₁₂H₁₃N₅O₄
Masse moléculaire:291.26

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months

Toyocamycin Chemical Structure

CAS No.: 606-58-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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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Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	3.3 μg/mL Compound: toyocamycin	Inhibition of phosphatidylinositol 4-kinase in human A431 cell membrane by liquid scintillation counting Inhibition of phosphatidylinositol 4-kinase in human A431 cell membrane by liquid scintillation counting	[PMID: 1666120]
B16	EC₅₀	0.005 μM Compound: toyocamycin	Cytotoxicity that caused a 50% reduction in absorbance at 490 nm in B16 mouse melanoma cells using MTS assay. Cytotoxicity that caused a 50% reduction in absorbance at 490 nm in B16 mouse melanoma cells using MTS assay.	[PMID: 11020285]
BSC-1	IC₅₀	46 μM Compound: a	Tested in vitro for cytotoxicity against the monkey kidney cells (BSC-1 cells). Tested in vitro for cytotoxicity against the monkey kidney cells (BSC-1 cells).	[PMID: 2175356]
HFF	IC₅₀	8 μM Compound: a	Tested in vitro for cytotoxicity against the normal human diploid cells (HFF cells). Tested in vitro for cytotoxicity against the normal human diploid cells (HFF cells).	[PMID: 2175356]
HFF	IC₅₀	0.03 μM Compound: 8b	Cytotoxicity was evaluated against the Human diploid cells (HFF) Cytotoxicity was evaluated against the Human diploid cells (HFF)	[PMID: 2913300]
HFF	IC₅₀	<0.01 μM Compound: I	Cytotoxicity against HFF cells, estimated by visual scoring of cells not affected by virus infection in the plaque reduction assay Cytotoxicity against HFF cells, estimated by visual scoring of cells not affected by virus infection in the plaque reduction assay	[PMID: 8632411]
KB	IC₅₀	17 μM Compound: a	Tested in vitro for cytotoxicity against the human neoplastic cell line (KB cells). Tested in vitro for cytotoxicity against the human neoplastic cell line (KB cells).	[PMID: 2175356]
KB	IC₅₀	0.04 μM Compound: 8b	Cytotoxicity was evaluated in Human neoplastic cell line (KB) Cytotoxicity was evaluated in Human neoplastic cell line (KB)	[PMID: 2913300]
KB	IC₅₀	0.03 μM Compound: I	Cytotoxic activity tested against exponentially growing KB cells, determined by staining method Cytotoxic activity tested against exponentially growing KB cells, determined by staining method	[PMID: 8632411]
L1210	IC₅₀	0.0026 μg/mL Compound: 2	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 2693614]
L1210	IC₅₀	4 x 10^-9 M Compound: 8b	In vitro cytotoxicity was evaluated against the L1210 Murine leukemic cells In vitro cytotoxicity was evaluated against the L1210 Murine leukemic cells	[PMID: 2913300]
Vero C1008	EC₅₀	0.59 μM Compound: Toyocamycin	Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in infection measured after 24 hrs by Plaque assay Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in infection measured after 24 hrs by Plaque assay	[PMID: 37229831]

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.

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).

Chemical Information

CAS No. 606-58-6
Appearance Solid
Masse moléculaire 291.26
Formule C₁₂H₁₃N₅O₄
Color Off-white to yellow
SMILES

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

Vengicide
Structure Classification
- Antibiotics
- Other Antibiotics
Initial Source
- Microorganisms
Streptomyces diastatochromogenes
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (15)

All Bio/Physico-chemical AssayWBRT-PCRFlow Cytometry

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Journal Impact Factor

J Adv Res

Rutin triggers IRE1-mediated GSDMD-dependent pyroptosis in macrophages to suppress systemic Salmonella infection. [Abstract]

2026 Apr 1:S2090-1232(26)00273-0. PMID: 41932494
Adv Sci (Weinh)

Cholesterol-Mediated Metabolic-mechanotransductive Crosstalk Orchestrates Castration Resistance in Prostate Cancer. [Abstract]

2026 Jun 4:e75977. PMID: 42240967
J Immunother Cancer

Dexamethasone activates anti-tumor immunity in multiple myeloma by dismantling the GR-PPP1CB complex to restore STING/IRF3 signaling. [Abstract]

2026 Jun 23;14(6):e015256. PMID: 42336654
J Exp Med

Xbp1 controls the reparative function of intestinal ILC2s during colitis. [Abstract]

2026 Jan 5;223(1):e20250440. PMID: 41165618
Cell Death Discov

Oncoprotein CYB561, acting in IRE1-XBP1-SREBF1 and FAK-ERK pathway, promotes breast cancer lipogenesis and progression. [Abstract]

2026 Apr 13;12(1):227. PMID: 41974658
Chin Med J (Engl)

XBP1-mediated mitochondrial damage activates the mtDNA/STING/NLRP3 pathway to delay diabetic wound healing. [Abstract]

2026 May 26. PMID: 42192237
J Agric Food Chem

XBP1s-Regulated GFPT1 via Facilitating O-GlcNAcylation of FASN S509 Is Involved in Arsenic-Induced MASLD through Promoting Fatty Acid Synthesis in Hepatocytes. [Abstract]

2026 Apr 15;74(14):11814-11831. PMID: 41920731
Liver Int

Mitochondrial amidoxime-reducing component 1 p.Ala165Thr increases protein degradation mediated by the proteasome. [Abstract]

2024 May;44(5):1219-1232. PMID: 38375985
Transl Res

Genetic and pharmacological targeting of XBP1 alleviates hepatic ischemia reperfusion injury by enhancing FoxO1-dependent mitophagy. [Abstract]

2024 Oct:272:162-176. PMID: 38494125
Commun Biol

A compatible gravity-driven organoid perfusion (GDOP) platform for drug screening with sensitivity and toxicity process evaluation. [Abstract]

2026 Apr 2;9(1):718. PMID: 41922471
Biochim Biophys Acta Mol Basis Dis

PDIA4 targets IRE1α/sXBP1 to alleviate NLRP3 inflammasome activation and renal tubular injury in diabetic kidney disease. [Abstract]

2025 Mar;1871(3):167645. PMID: 39743023
Am J Pathol

The oncogenic protein kinase/ATPase RIOK1 is up-regulated via the MYC/E2F transcription factor axis in prostate cancer. [Abstract]

2023 Sep;193(9):1284-1297. PMID: 37301535

Toyocamycin purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2023 Sep;193(9):1284-1297. [Abstract]

Toyocamycin is a potent inhibitor of PCa cell growth. Dose-response curves after treatment of various PCa cell lines with the RIOK1 inhibitor Toyocamycin after 72 hours.

Toyocamycin purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2023 Sep;193(9):1284-1297. [Abstract]

Bar plots showing the fold-changes at selected Toyocamycin (0-40 nmol/L) concentrations at 72 hours after treatment.

Toyocamycin purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2023 Sep;193(9):1284-1297. [Abstract]

To investigate the underlying mechanism of Toyocamycin-related toxicity in PCa cells, short-term experiments (24 hours) in PC3 and 22Rv1 cells at a concentration of 100 nmol/L were performed. To differentiate between Toyocamycin-specific and general cell death related alterations, the clinically used chemotherapeutic drug docetaxel (100 nmol/L) was included in these experiments. RIOK1 protein expression was significantly reduced within 24 hours after biochemical inhibition of RIOK1, which might indicate that RIOK1 auto-activates its own expression, as observed in budding yeast.

Toyocamycin purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2023 Sep;193(9):1284-1297. [Abstract]

The impact of Toyocamycin on rRNA content was measured, given the importance of RIOK1 in the production of rRNA and in the processing of the 18S-E pre-rRNA. Total rRNA content per cell was significantly reduced, by >30%, in both cell lines.

Toyocamycin purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2023 Sep;193(9):1284-1297. [Abstract]

To assess whether Toyocamycin induces apoptosis in PCa cells, the sub-G1 fraction was measured in PC3 and 22Rv1 cells using fluorescence-activated cell sorting analysis after 72 hours of Toyocamycin treatment, and the effect was compared to that with docetaxel treatment. With the two drugs at a concentration of 100 nmol/L, apoptosis was significantly induced at 72 hours after treatment.
Cell Signal

Endoplasmic reticulum stress regulates intestinal motility in acute pancreatitis by regulating the expression and phosphorylation of nNOS through IRE1α/XBP1s-PI3K/Akt signaling axis. [Abstract]

2025 Dec:136:112123. PMID: 40930473
SSRN

2024 Jun 18.
bioRxiv

Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]

2023 Sep 12:2023.09.09.557001. PMID: 37745469

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Toyocamycin

15 Cited Publications

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Toyocamycin

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Publications Citing Use of MedChemExpress (MCE) Toyocamycin

Voir tous les produits spécifiques à Isoform Antibiotic

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Toyocamycin Related Classifications

HY-103248 Related Classifications