CA-5f _Late-Stage Autophagy 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECA-5fCat. No.: HY-112698CAS No.: 1370032-19-1分式: CHNO分量: 388.46作靶點(diǎn): Autophagy作通路: Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 77.5 mg/mL (199.51 mM; Need ultrasonic)H2O : 40% P

2、EG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.35 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.35 mM); Suspended solution; Need ultrasonic3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL

3、 (5.35 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 CA-5f種有效的晚期巨噬/噬 (macroautophagy/autophagy) 抑制劑，通過(guò)抑制噬體-溶酶體融合起作。CA-5f 能夠增加 LC3B-II (種監(jiān)控噬的標(biāo)記物) 和 SQSTM1 蛋平，促進(jìn) ROS 的產(chǎn)。具有抗腫瘤活性 1。IC50 & Target Macroautophagy/autophagy 1體外研究 CA-5f (0-40 M, 6 hour) concentration- and time-dependently elevates the level of L

4、C3B-II (a marker tomonitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs 1.CA-5f (20 M, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combinationBafilomycin A1 (100 nM) or Chloroquine (30 M) in A549 cells and HUVECs 1.CA-5f (20 M) neither impairs the hydr

5、olytic function nor the quantity of lysosomes 1.CA-5f (20 M, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs 1.Cell Viability Assay 1Cell Line: A549, HUVECsConcentration: 20 MIncubation Time: 96 hoursResult: Exhibited more cytotoxicity against A549 cells compared wit

6、h normal HUVECs.Western Blot Analysis 1Cell Line: A549 cells and HUVECsConcentration: 0-40 MIncubation Time: 6 hoursResult: Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in aconcentration- and time-dependent manner.體內(nèi)研究CA-5f (40 mg/kg, i.p., every 2 days for up to 30 day

7、s) is well tolerated, and potently inhibits the growth oftumor in nude mice bearing A549 lung cancer cells 1.CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lungcancer cells 1.Animal Model: Nude mice bearing A549 lung cancer cells 1Dosage: 40 mg/kg2/

8、3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration: Injected via caudal vein, every 2 days for up to 30 daysResult: Significantly suppressed tumor volume and weight in mice, increased the number ofapoptotic cells in mice.REFERENCES1. Zhang L, et al. Identification of compound CA-5f as a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-smallcell lung cancer. Autophagy. 2019 Mar;15(3):391-406.McePdfHeightCaution: Product has not been fully validated for medical appli