2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Atg4 Cathepsin Autophagy Apoptosis
  4. S130

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux.

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

S130 Chemical Structure

S130 Chemical Structure

CAS No. : 1160852-22-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

S130 Related Antibodies

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • Biological Activity

  • Purity & Documentation

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Description

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux[1].

IC50 & Target

IC50: 3.24 µM (ATG4B)[1]
In Vitro

S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity[1].
S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage[1].
S130 accumulates autolysosomes with more lipidated LC3[1].
S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis[1].
Nutrient deprivation enhances S130-induced cytotoxicity[1].
S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 µM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B[1].

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

S130 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HeLa cells, HCT116 cells, HL60 cells
Concentration: 0 μM, 3.1 μM, 6.3 μM, 12.5 μM, 25 μM
Incubation Time: 48 hours
Result: Had significant cytotoxic effects on HeLa cells (IC50 =16.1 µM), HCT116 cells(IC50 =9.0 µM) and HL60 cells (IC50 =4.7 µM) at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis.

Cell Autophagy Assay[1]

Cell Line: HeLa cells and MEF cells
Concentration: 10 μM
Incubation Time: 6 hours
Result: Suppressed autophagy at the early LC3 priming step or late autolysosome degradation stage.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: Suppressed approximately 79% of the cleavage of full-length LC3-GST at 10 µM, while no substrates were processed in ATG4B KO cells.
In Vivo

S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs[1].

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

Animal Model: BALB/c nude female mice (4 weeks), with HCT116 cells xenograft[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; daily; 3 weeks
Result: Was able to suppress tumor growth and with a sound safety on vital organs.
Molecular Weight

387.47

Formula

C24H25N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC=CC=C2C3=C4C1=NC=C(C(NCCCN(CC)CC)=O)C4=CC=C3
Shipping

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

DMSO : 125 mg/mL (322.61 mM; Need ultrasonic; 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 2.5808 mL 12.9042 mL 25.8084 mL
5 mM 0.5162 mL 2.5808 mL 5.1617 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 2.25 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
  • Protocol 2

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

    Solubility: ≥ 2.25 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: 99.43%

COA (245 KB) LCMS (267 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5808 mL 12.9042 mL 25.8084 mL 64.5211 mL
5 mM 0.5162 mL 2.5808 mL 5.1617 mL 12.9042 mL
10 mM 0.2581 mL 1.2904 mL 2.5808 mL 6.4521 mL
15 mM 0.1721 mL 0.8603 mL 1.7206 mL 4.3014 mL
20 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2261 mL
25 mM 0.1032 mL 0.5162 mL 1.0323 mL 2.5808 mL
30 mM 0.0860 mL 0.4301 mL 0.8603 mL 2.1507 mL
40 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2904 mL
60 mM 0.0430 mL 0.2151 mL 0.4301 mL 1.0754 mL
80 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8065 mL
100 mM 0.0258 mL 0.1290 mL 0.2581 mL 0.6452 mL
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S130 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:

S1301160852-22-1S 130S-130Atg4CathepsinAutophagyApoptosisAutophagy-related 4Inhibitorinhibitorinhibit

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