S130

S130

S646167-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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)

S130 是一种高亲和力的 ATG4B（一种主要的半胱氨酸蛋白酶）选择性抑制剂，IC50 为 3.24 µM。S130 可抑制自噬通量。

1160852-22-1

C24H25N3O2

387.47 g/mol

44128205

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

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

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)

DZUCZYXRADUTMW-UHFFFAOYSA-N

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

44128205

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

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

1

4

7

387.195 Da

387.195 Da

62.300 Ų

29

0

591

0

1

4