calu-3 cells

BMS-265246 is a potent and selective CDK1/2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity that inhibits the replication of severe acute respiratory syndrome coronavirus [SARS-CoV] in Vero 76 cells, Middle East respiratory syndrome coronavirus [MERS-CoV] in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s = 0.1, 0.15, and 0.3 μM, respectively).

Auranofin (SKF-39162) is an antirheumatic agent, is used to treat rheumatoid arthritis, improves arthritis symptoms including painful or tender and swollen joints and morning stiffness.

9-AMN is an inhibitor of the SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro), effectively reducing its deubiquitinating (DUB) activity and protease activity, with IC50 values of 4.55 µM and 4.15 µM, respectively. Additionally, 9-AMN suppresses the replication of the SARS-CoV variants Delta and Omicron in Calu-3 cells, with IC50 values of 1.04 µM and 2.35 µM, respectively.

N-0920 is a potent TMPRSS2 inhibitor with an IC50 value of 0.35 nM. It effectively inhibits the entry of SARS-CoV-2 variants [EG.5.1] and [JN.1] into Calu-3 cells, exhibiting EC50 values of 300 pM and 90 pM, respectively.

PROTACSARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent SARS-CoV-2 Mpro PROTAC degrader. It exhibits broad-spectrum antiviral activity against coronaviruses, including SARS-CoV-2 (EC50 = 10.8 μM), HCoV-OC43 (EC50 = 1.6 μM), and HCoV-229E (EC50 = 6.5 μM). In Calu-3 cells, it shows effective anti-SARS-CoV-2 activity with an EC50 of 0.89 μM.

SARS-CoV-2-IN-77 (compound 11e) is an inhibitor of cathepsin L and cathepsin S, with Ki values of 111 nM and 103 nM, respectively. It effectively inhibits SARS-CoV-2 in Calu-3 cells with an EC50 value of 38.4 nM and does not exhibit cytotoxicity.

RH12 is a dual inhibitor of SARS-CoV-2-related RNA-dependent RNA polymerase (RdRp, IC50 of 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC50 of 4.2 nM). It demonstrates antiviral activity by inhibiting viral replication and absorption, showing 90.5% virucidal effect in Vero-E6 cells. Additionally, RH12 inhibits Calu-3 cell viability with an IC50 of 17.5 nM.

SARS-CoV-2-IN-115 (Compound 3e) is a potent inhibitor of SARS-CoV-2, showing strong antiviral activity in infected Calu-3 cells with an EC50 of 1.7 μM. It effectively inhibits human dihydroorotate dehydrogenase (HsDHODH) activity with an IC50 of 1.5 μM. Importantly, SARS-CoV-2-IN-115 maintains immune response without affecting the proliferation of CD4 T cells.

Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19.

SARS-CoV-2-IN-44, an inhibitor of SARS-CoV-2, effectively suppresses viral replication with an EC50 value of 0.6μM and exhibits negligible cytotoxicity in Calu-3 cells, rendering it suitable for antiviral research [1].

SARS-CoV-2-IN-45 (Compound 8p) is an effective inhibitor of SARS-CoV-2 that hinders viral replication in Calu-3 cells with an EC50 of 0.5 μM and exhibits negligible cytotoxicity [1].

SARS-CoV-2-IN-65 (compound 2f (81)) is a potent, orally active reversible inhibitor of SARS-CoV-2 entry, mainly blocking the RBD:ACE2 interaction and TMPRSS2 activity in the ACE2-dependent pathway in Calu-3 cells [1].

SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication, exhibiting low cytotoxicity and effectively suppressing viral replication in Vero E6 and Calu-3 cells, with half-maximal effective concentration (EC50) values of 1.99 μM and 1.92 μM, respectively [1].

SARS-CoV-2-IN-62 (Compound R3b) effectively inhibits SARS-CoV-2 replication in Vero E6 and Calu-3 cells, demonstrating low cytotoxicity with EC50 values of 2.97 μM and 3.82 μM, respectively [1].