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1160852-22-1

中文名稱 化合物 T12819
英文名稱 S130
CAS 1160852-22-1
分子式 C24H25N3O2
分子量 387.47
MOL 文件 1160852-22-1.mol
1160852-22-1 結(jié)構(gòu)式 1160852-22-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12819
英文別名
S130
S130,S-130
7H-Dibenzo[de,g]quinoline-4-carboxamide, N-[3-(diethylamino)propyl]-7-oxo-

物理化學(xué)性質(zhì)

沸點(diǎn)641.5±50.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 125 mg/mL (322.61 mM; Need ultrasonic)
酸度系數(shù)(pKa)13.15±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
化合物 T12819價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2026/06/05HY-112818化合物 T12819
S130
1160852-22-11 mg1590元
2026/06/05HY-112818暫無
S130
1160852-22-15mg3500元
2026/06/05HY-112818暫無
S130
1160852-22-110mM * 1mLin DMSO3850元

常見問題列表

生物活性
S130 是一種高親和力、選擇性的半胱氨酸蛋白酶 ATG4B 的抑制劑, IC50 值為 3.24 μM。S130 可以抑制自噬通量。
靶點(diǎn)

IC50: 3.24 μM (ATG4B)

體外研究

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 (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 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.
體內(nèi)研究

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 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.
"1160852-22-1" 相關(guān)產(chǎn)品信息
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