S130

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

S130（ATG4B抑制剂S130）是一种有效的、特异性的ATG4B抑制剂，IC50为3.24 uM，具有很强的亲和力（Kd=4 uM）并特异性抑制ATG4B的活性。

S130 (ATG4B inhibitor S130) is a potent, specific ATG4B inhibitor with IC50 of 3.24 uM, shows strong affinity (Kd=4 uM) and specifically suppresses the activity of ATG4B, but not other proteases; displays no inhibitory effects on cysteine proteases such as CASP3 (caspase 3), CASP8 (caspase 8) and CASP9 (caspase 9), or aspartic proteases; does not cause the impairment of autophagosome fusion, nor does it result in the dysfunction of lysosomes; causes cell death of colorectal cancer cells in vitro and in vivo.

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. Cell Cytotoxicity Assay 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 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 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.

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

ATG4B inhibitor S130

Autophagy

Atg

Atg

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1160852-22-1

387.483

C24H25N3O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (322.61 mM)

CCN(CC)CCCNC(=O)C1=CN=C2C3=C1C=CC=C3C4=CC=CC=C4C2=O

N-(3-(diethylamino)propyl)-7-oxo-7H-dibenzo[de,g]quinoline-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years