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 (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].

Para uso exclusivo en investigación. No vendemos a pacientes.

Thiolutin

Thiolutin Estructura química

No. CAS : 87-11-6

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Revisión del cliente

Based on 4 publication(s) in Google Scholar

Other Forms of Thiolutin:

Thiolutin Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Antibiotic:

Ver todas las isoformas
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

Ver todos los productos específicos de isoformas Deubiquitinase:

Ver todas las isoformas
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15 USP28 USP25

Ver todos los productos específicos de isoformas NOD-like Receptor (NLR):

Ver todas las isoformas
NLRP3 NLRP1 NOD1 NOD2

Ver todos los productos específicos de isoformas DNA/RNA Synthesis:

Ver todas las isoformas
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Actividad biológica

  • Pureza y Documentación

  • Referencias

  • Revisión del cliente

Descripciòn

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].

IC50 & Target

RNA Polymerase

 

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.
Peso molecular

228.29

Fòrmula

C8H8N2O2S2
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Streptomyces
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
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.

  • Calculadora de molaridad

  • Calculadora de dilución

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 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.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.27%

SDS (479 KB)

COA (257 KB) HNMR (251 KB) LCMS (103 KB)

Instrucciones de manejo (2659 KB)
Referencias

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Thiolutin 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:

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

Productos vistos recientemente:

Consulta en línea

Your information is safe with us. * Required Fields.

Nombre del producto

  

Requested Quantity *

Nombre del solicitante *

 

Saludo

Direcciòn del E-mail *

 

Número de teléfono *

Department

 

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

      

Observaciones

Consulta para venta a granel

Inquiry Information

Nombre del producto:
Thiolutin
Cat. No.:
HY-N6712
Cantidad:
MCE Japan Authorized Agent:

Revisión del cliente

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Nombre del producto

  

Lot #

Nombre del solicitante *

 

Direcciòn del E-mail *

Número de teléfono

 

Department *

Nombre de la Organizaciòn *

 

Country or Region *

Observaciones

SAFETY DATA SHEET (SDS)

English - EN (479 KB) Français - FR (479 KB) Deutsch - DE (479 KB) Norwegian - NO (479 KB) Español - ES (479 KB) Swedish - SV (479 KB) Italian - IT (479 KB) Korean - KR (479 KB) Portuguese - PT (479 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.