S130


Catalog No. Size PriceQuantity
M12488-2 2mg solid $170
M12488-10 10mg solid $555

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.

Product information

CAS Number: 1160852-22-1

Molecular Weight: 387.47

Formula: C24H25N3O2

Chemical Name: N-[3-(diethylamino)propyl]-8-oxo-10-azatetracyclo[7.7.1.0, .0, ]heptadeca-1(17), 2, 4, 6, 9, 11, 13, 15-octaene-12-carboxamide

Smiles: CCN(CCCNC(=O)C1=CN=C2C3C1=CC=CC=3C1=CC=CC=C1C2=O)CC

InChiKey: DZUCZYXRADUTMW-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

References:

  1. Fu Y, et al. Discovery of a small molecule targeting autophagy via ATG4B inhibition and cell death of colorectal cancer cells in vitro and in vivo. Autophagy. 2018 Sep 20:1-17.

Products are for research use only. Not for human use.

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