CA-5f

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.

Product information

CAS Number: 1370032-19-1

Molecular Weight: 388.46

Formula: C24H24N2O3

Chemical Name: (3E, 5E)-3-[(3, 4-dimethoxyphenyl)methylidene]-5-[(1H-indol-3-yl)methylidene]-1-methylpiperidin-4-one

Smiles: COC1C=C(/C=C2\CN(C)C/C(=C\C3=CNC4=CC=CC=C34)/C\2=O)C=CC=1OC

InChiKey: JYOLPDWVAMBMQN-UBIAKTOFSA-N

InChi: InChI=1S/C24H24N2O3/c1-26-14-18(10-16-8-9-22(28-2)23(11-16)29-3)24(27)19(15-26)12-17-13-25-21-7-5-4-6-20(17)21/h4-13,25H,14-15H2,1-3H3/b18-10+,19-12+

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 77.5 mg/mL (199.51 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: ≥12 months 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:

CA-5f (0-40 μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs. CA-5f (20 μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1 (100 nM) or Chloroquine (30 μM) in A549 cells and HUVECs. CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes. CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs.

In Vivo:

CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells.

References:

1. Zhang L, et al. Identification of compound CA-5f as a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-small cell lung cancer. Autophagy. 2019 Mar;15(3):391-406.

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