S130 - 99%, high purity , CAS No.1160852-22-1

  • ≥99%
Item Number
S646167
Grouped product items
SKUSizeAvailabilityPrice Qty
S646167-5mg
5mg
Available within 8-12 weeks(?)
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$293.90
S646167-10mg
10mg
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$461.90
S646167-50mg
50mg
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$1,382.90
S646167-100mg
100mg
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$1,885.90

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsS130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC 50 of 3.24 µM. S130 suppresses autophagy flux.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC 50 of 3.24 µM. S130 suppresses autophagy flux

In Vitro

S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity. S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage. S130 accumulates autolysosomes with more lipidated LC3. 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. Nutrient deprivation enhances S130-induced cytotoxicity. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell 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 (IC 50 =16.1 µM), HCT116 cells(IC 50 =9.0 µM) and HL60 cells (IC 50 =4.7 µM) at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis. Cell Autophagy AssayCell 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 AnalysisCell 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 . 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 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.

Form:Solid

IC50& Target:IC50: 3.24 µM (ATG4B)

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[3-(diethylamino)propyl]-8-oxo-10-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2,4,6,9,11,13(17),14-octaene-12-carboxamide
INCHI InChI=1S/C24H25N3O2/c1-3-27(4-2)14-8-13-25-24(29)20-15-26-22-21-17(11-7-12-18(20)21)16-9-5-6-10-19(16)23(22)28/h5-7,9-12,15H,3-4,8,13-14H2,1-2H3,(H,25,29)
InChi Key DZUCZYXRADUTMW-UHFFFAOYSA-N
Canonical SMILES CCN(CC)CCCNC(=O)C1=CN=C2C3=C1C=CC=C3C4=CC=CC=C4C2=O
Isomeric SMILES CCN(CC)CCCNC(=O)C1=CN=C2C3=C1C=CC=C3C4=CC=CC=C4C2=O
PubChem CID 44128205
MeSH Entry Terms Atg4B inhibitor S130;N-(3-(diethylamino) propyl)-7-oxo-7H-dibenzo(de,g)quinoline-4-carboxamide;N-(3-(Diethylamino)propyl)-8-oxo-10-azatetracyclo(7.7.1.02,7.013,17)heptadeca-1(16),2,4,6,9,11,13(17),14-octaene-12-carboxamide
Molecular Weight 387.47

Certificates

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Chemical and Physical Properties

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

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