1. Metabolic Enzyme/Protease
    Autophagy
    Apoptosis
  2. Cathepsin
    Autophagy
    Apoptosis
  3. S130

S130 

Cat. No.: HY-112818 Purity: 99.17%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

1160852-22-1

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (322.61 mM; Need ultrasonic)

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
10 mM 0.2581 mL 1.2904 mL 2.5808 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.17%

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