ars

ARS-1630 is a mutant K-ras G12C inhibitor. It is a less active enantiomer of ARS-1620.

ARS-1620 is a covalent inhibitor of K-RASG12C.

ARS-1323 is the racemate of ARS-1620 and a mutant K-ras G12C inhibitor.

ARS-1323-alkyne is a switch-II pocket (S-IIP) inhibitor and a conformational specific chemical reporter of KRASG12C nucleotide state in living cells.

ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells

ARS-2102 is a potent covalent KRAS G12C inhibitor used in cancer research.

1588-A4 (ARS-1620 Intermediate) is an intermediate of ARS-1620 which is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.

Carsalam (2H-1,3-Benzoxazine-2,4(3H)-dione) is a nonsteroidal anti-inflammatory drug.

Sarsasapogenin (Parigenin) is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin. It is named after sarsaparilla (Smilax sp.), a family of climbing plants found in subtropical regions. It was one of the first sapogenins to be identified, and the first spirostan steroid to be identified as such.

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.

SARS-CoV-2 3CLpro-IN-16 is a covalent inhibitor of SARS-CoV-2 3CLpro activity, exerting its effect by forming a covalent bond with Cys145.

SARS-CoV-2 Mpro-IN-2 is a selective SARS-CoV-2M pro inhibitor with an IC50 value of 0.40 μM.SARS-CoV-2 Mpro-IN-2 has good antiviral activity and can be used to study COVID-19.

SARS-CoV-2-IN-38 is an orally available SARS-CoV-2 inhibitor with potential antiviral activity for the study of SARS viral infections.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

Larsucosterol is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Octopamine hydrochloride ((±)-p-Octopamine hydrochlorid) is a biogenic monoamine structurally associated with noradrenaline. It can serve as a neurohormone, a neurotransmitter, and a neuromodulator in invertebrates.

Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IOP) reduction.

ARS-CoV-2-IN-53 (Compd 5d) shows an inhibitory effect on SARS-CoV-2 replication with an EC50 value of 14.3 μM and exhibits significant antiviral activity against human coronavirus 229E (HCoV-229E) [1].

SARS-CoV-2-IN-33 is an inhibitor of COVID-19. SARS-CoV-2-IN-3 exhibits good binding affinity (-8.0 Kcal/mole) for COVID-19 major protease (Mpro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 exhibits good anti-proliferative effects on cancer cells. SSARS-CoV-2-IN-33 can be used to study cancer and COVID-19.

Acridarsine,10-phenyl- is a biochemical.

SARS-CoV-2 3CLpro-IN-4 (Compound 5g) is a multifunctional inhibitor of SARS-CoV-2 3CLpro with antiviral, antibacterial, and antifungal properties.

SARS-CoV-2-IN-10 is a powerful and non-toxic inhibitor of SARS-CoV-2 3CL protease, with IC50 and EC50 values of 0.13 nM and 1.03 nM, respectively. The SARS-CoV-2 3C-like protease (3CLpro) is critical for viral replication and serves as an ideal target for intervention. By targeting the SARS-CoV-2 3CL protease, SARS-CoV-2-IN-10 has the potential to facilitate the development of effective antiviral drugs specific to SARS-CoV-2.

Phenylarsine Oxide (Oxophenylarsine) is a membrane-permeable tyrosine phosphatase inhibitor with an IC50 value of 18 µM that stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle.

Compound 8h, also known as SARS-CoV-2-IN-43, is a powerful inhibitor effective in obstructing the replication of SARS-CoV-2, exhibiting significant antiviral activity [1].

SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active inhibitor of SARS-CoV-2 3CLpro, demonstrating potent anti-SARS-CoV-2 properties with an EC50 of 0.18 μM and exhibits minimal cytotoxicity, having a CC50 greater than 50 μM, in Vero E6 cells [1].

SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent SARS-CoV-2 inhibitor with an IC50 of 80 nM, and shows high affinity for the Sigma Receptor, with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) [1].

SARS-CoV-2 3CLpro-IN-19 (Compound C5a), a non-covalent, non-peptide inhibitor of the SARS-CoV-2 3CLpro enzyme, exhibits potent in vitro activity with an IC50 of 0.7 μM. It demonstrates broad-spectrum efficacy against infection by Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) in human cells, with EC50 values ranging from 30-69 nM [1].

SARS-CoV-2-IN-55 (compound 65) is a SARS-CoV-2 inhibitor with low cytotoxicity, characterized by an IC50 of 0.3 μM, and acts through direct interaction with VSV-S pseudoparticles [1].

Compound 3h, also known as SARS-CoV-2 3CLpro-IN-17, is a selective inhibitor of the SARS-CoV-2 3CL protease, demonstrating an IC50 of 0.322 μM [1].

SARS-CoV-2 nsp3-IN-1 (Compound 15c) exhibits significant selectivity for coronavirus macrodomains, particularly SARS-CoV-2 Mac1, and can inhibit Mac1 ADP-ribosylhydrolase activity with an IC50 of 6.1 μM [1].

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

Anti-SARS-80R mAb (SARS-80R) is a human IgG1 monoclonal antibody derived from CHO cells, designed to selectively bind the Spike (S1) protein, thereby preventing SARS virus infection in susceptible cells[1].

Anti-SARS-CoV-2 Spike mAb (CR3022) is a human monoclonal IgG1 antibody produced from CHO cells, which specifically targets the S1 domain of the Spike protein in both SARS-CoV and SARS-CoV-2.

Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.

SARS-CoV-2 nsp13-IN-2 (Compound C2) is a small molecule inhibitor targeting the SARS-CoV-2 non-structural protein 13 (nsp13), specifically acting on the nsp13 ssDNA+ATPase with an IC50 of 42 μM.

SARS-CoV-2 3CLpro-IN-10(5d) is a potent inhibitor of the SARS-CoV-2 3CL protease with an IC50 value of 190 nM and demonstrates broad-spectrum antiviral activity, exhibiting IC50 values of 790 nM for SARS-CoV-1 and 70 nM for MERS-CoV.

SARS-CoV MPro-IN-2 effectively inhibits the SARS-CoV-2 main protease (M pro), crucial for the virus's replication and transcription in host cells, with an IC50 value of 72.07 nM. Given its significant role in processing viral polyproteins, M pro is regarded as a key target in drug discovery efforts. Consequently, SARS-CoV MPro-IN-2 holds promise for COVID-19 research.

SARS-CoV-2 Mpro-IN-5 is a dual inhibitor targeting Main Protease (M Pro) and Cathepsin L (CatL) with IC50 values of 1800 nM and 145 nM, respectively. This compound demonstrates antiviral activity by inhibiting SARS-CoV-2 replication in hACE2 expressing A549 cells, with an IC50 value of 14.7 nM.

Tonlamarsen is an angiotensinogen synthesis reducer with antihypertensive activity [1].

SARS-CoV-2-IN-29 disodium, a diphosphate ester featuring a benzene system and molecular tweezers architecture, demonstrates antiviral efficacy by targeting SARS-CoV-2 with half-maximal inhibitory concentrations (IC50s) of 1.5 μM for virus activity and 1.6 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by a half-maximal effective concentration (EC50) of 3.0 μM [1].

SARS-CoV-2-IN-30 disodium, a benzene-system-based two-armed diphosphate ester featuring molecular tweezers, demonstrates antiviral efficacy, with IC50 values of 0.6 μM against SARS-CoV-2 and 6.9 μM for spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes, evidenced by an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-28 disodium, a diphosphate ester featuring a C7 alkyl chain and extended-length molecular tweezers, demonstrates antiviral efficacy by showing IC50 values of 0.4 μM and 1.0 μM against SARS-CoV-2 activity and spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-30, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral properties, achieving IC50 values of 0.6 μM against SARS-CoV-2 activity and 6.9 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes with an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-23 disodium, a medium-length molecular tweezer and two-armed diphosphate ester, demonstrates antiviral properties by inhibiting SARS-CoV-2 activity and spike pseudoparticle transduction with IC50 values of 8.2 μM and 2.6 μM, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-25 (Compound CP026) disodium, a potent inhibitor of SARS-CoV-2 spike pseudoparticle transduction, demonstrates significant efficacy with an IC50 value of 1.6 μM. It also effectively inhibits enveloped viruses and liposomes, highlighting its broad-spectrum antiviral potential.

Narsoplimab (OMS 721) is a selective whole-human immunoglobulin gamma-4 (IgG4) monoclonal antibody and a mannan-binding lectin-associated serine protease-2 (MASP-2) inhibitor that binds MASP-2 to prevent lectin pathway activation and inhibit the agglutinin pathway. It is used to study diseases associated with hematopoietic stem cell transplantation in adults.

SARS-CoV-2-IN-39 is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 has antiviral activity and inhibits SARS-CoV-2 by inhibiting SKP2 protein and stabilizing BECN1.