2. Anti-infection Cell Cycle/DNA Damage Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  3. Antibiotic Bacterial Deubiquitinase NOD-like Receptor (NLR) DNA/RNA Synthesis Pyroptosis HMG-CoA Reductase (HMGCR)
  4. Thiolutin

Thiolutin  (Synonyms: Acetopyrrothin)

Cat. No.: HY-N6712 Purity: 99.29%
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Thiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC)[1][2][3][4][5].

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

Thiolutin

Thiolutin Chemical Structure

CAS No. : 87-11-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

Other Forms of Thiolutin:

Thiolutin Related Antibodies

Top Publications Citing Use of Products

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USP1 USP2 USP7 USP8 USP10 USP30 UCHL1

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NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Thiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC)[1][2][3][4][5].

In Vitro

Thiolutin (0.5-2 μM, 24 h) significantly inhibits the expression of BRCC36 and HMGCR proteins in a dose-dependent manner in HepG2 and Hep3B cells[1].

Thiolutin (0-24 h) attenuates the interaction between HMGCR and BRCC36 in HepG2 cells and reduces the half-life of the HMGCR protein while increasing its ubiquitination level in both HepG2 and Hep3B cells[1].

Thiolutin (0.1-10 μM, 48 h) inhibits the proliferation of HepG2 and Hep3B cells dose-dependently[1].

Thiolutin (0.25-0.5 μM, 14 days) elevates RSL3 (HY-100218A)-induced cell death and RSL3-triggered lipid peroxidation in HepG2 cells[1].

Thiolutin (25-250 nM) inhibits the LDH release induced by LPS (HY-D1056) and Nigericin (HY-127019)[1].

Thiolutin (0.5 μM, 14 days) reduces the colony-forming ability of HepG2 cancer cells in the presence of Lovastatin (HY-N0504) (5 μM)[1].

Thiolutin (50 μM, 0-120 min) induces global transcriptional stress in Neurospora[2].

Thiolutin (50 μM, 1-4 h) inhibits protein degradation by the proteasome in N.crassa and HeLa cells[2].

Thiolutin (0.001-100 μM) inhibits AMSH with an IC50 of 4 μM, which is higher than its inhibition of Rpn11 (IC50 = 0.53 μM), and this effect is reversible by Zn(cyclen)²⁺[2].

Thiolutin (10-50 nM, 30 min) attenuates pyroptosis and NLRP3 inflammasome activation in J774 A.1 murine monocyte-macrophage cells[3].

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

Thiolutin Related Antibodies

Cell Viability Assay[3]

Cell Line: J774 A.1 murine monocyte-macrophage cells
Concentration: 10, 25, 50 nM
Incubation Time: 30 min
Result: Increased progressively with higher concentrations.

ELISA Assay[3]

Cell Line: J774 A.1 murine monocyte-macrophage cells
Concentration: 10, 25, 50 nM
Incubation Time: 30 min
Result: Suppressed the levels of IL-1β and IL-18.

Western Blot Analysis[3]

Cell Line: J774 A.1 murine monocyte-macrophage cells
Concentration: 10, 25, 50 nM
Incubation Time: 30 min
Result: Suppressed the levels of IL-1β and caspase-1.
In Vivo

Thiolutin (0.75 mg/kg, i.p., every 3 days for 18 days) significantly decreases the volume and weight of the tumor in the BALB/c or C57 mice subcutaneously injected with 0.1 mL of PBS containing SMMC7721, HepG2, or Heap1-6 cells[1].

Thiolutin (0.5-5 mg/kg, i.p., every 2 days for 4 weeks) alleviates kidney injury, attenuates renal inflammation and modulates the NLRP3 inflammasome pathway in IgAN mice without hepatotoxic effects[3].

Thiolutin (1 mg/kg, i.p., once daily for 4 weeks ) improves cardiac function, mitigates cardiac remodeling urged by Doxorubicin (DOX) and restrains the NLRP3 inflammasome activation in DOX‑challenged mice[4].

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

Animal Model: BALB/c or C57 mice (5 weeks) were subcutaneously injected with 0.1 mL of PBS containing SMMC7721, HepG2, or Heap1-6 cells[1]
Dosage: 0.75 mg/kg
Administration: i.p. every 3 days for 18 days
Result: Decreased the volume and weight of the tumor.
Animal Model: IgAN model mice (8 weeks male BALB/c)[3]
Dosage: 0.5, 2.5, 5 mg/kg
Administration: i.p. every 2 days for 4 weeks
Result: Decreased Serum BUN S-cr levels, Serum IgA levels and ACR in urine, which were markedly elevated in the IgAN-positive group.
Diminished the glomerular hypercellularity and matrix expansion.
Ameliorated mesangial proliferation and extracellular matrix expansion.
Reduced the level of IFN-γ, TNF-α and IL-6.
Showed no necrosis or injury in both the liver and heart sections of mice.
Downregulated the mRNA expression levels of NLRP3, IL-1β, IL-18, and caspase-1
Animal Model: DOX‑challenged Male C57BL/6 mice(8-10 weeks)[4]
Dosage: 1 mg/kg
Administration: i.p. once daily for 4 weeks
Result: Ameliorated the changes of LVEF and LVFS as well as LVESD and LVEDD.
Increased the survival rate to 80%.
Decreased the levels of cTnT, CRP, and BNP.
Ameliorated the larger heart size.
Ameliorated DOX-induced pathological changes in cardiomyocytes, including misalignment, inflammatory cell infiltration, widened intercellular gaps, and abnormal morphology/size.
Decreased the protein levels of NLRP3, C-caspase-1/Pro-c-caspase, and GSDMD-N/GSDMD.
Molecular Weight

228.29

Formula

C8H8N2O2S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(NC1=C2C(N(C)C1=O)=CSS2)=O
Structure Classification
Initial Source

Streptomyces
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (27.38 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 4.3804 mL 21.9020 mL 43.8039 mL
5 mM 0.8761 mL 4.3804 mL 8.7608 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 1.25 mg/mL (5.48 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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.
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: 99.29%

SDS (479 KB)

COA (256 KB) RP-HPLC (624 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3804 mL 21.9020 mL 43.8039 mL 109.5098 mL
5 mM 0.8761 mL 4.3804 mL 8.7608 mL 21.9020 mL
10 mM 0.4380 mL 2.1902 mL 4.3804 mL 10.9510 mL
15 mM 0.2920 mL 1.4601 mL 2.9203 mL 7.3007 mL
20 mM 0.2190 mL 1.0951 mL 2.1902 mL 5.4755 mL
25 mM 0.1752 mL 0.8761 mL 1.7522 mL 4.3804 mL
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Thiolutin Related Classifications

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  • 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:

Thiolutin87-11-6AcetopyrrothinAntibioticBacterialDeubiquitinaseNOD-like Receptor (NLR)DNA/RNA SynthesisPyroptosisHMG-CoA Reductase (HMGCR)DUBsNLRP3 InflammasomeIgA nephropathyInflammationHepG2 cellsliver cancerDoxorubicin CardiotoxicityInhibitorinhibitorinhibit

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