EBOV Inhibitor

Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC₅₀ of 12.2 μM in HeLa cells. Retro-2 induces cell autophagy.

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy.

K6PC-5, a ceramide derivative, is a sphingosine kinase 1(SPHK1) activator and elicites a rapid transient increase in intracellular calcium levels. K6PC-5 has the potential for skin diseases involving abnormal keratinocyte, and neurodegeneration and virus infection research.

Atoltivimab (REGN3470), or maftivimab/odesivimab (Inmazeb) is the first Food and agent Administration (FDA)-approved monoclonal antibody to target Zaire ebolavirus (EBOVs) infection.

EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC₅₀=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells.

EBOV/MARV-IN-2 (compound 13) is an Ebolavirus (EBOV, IC₅₀=0.9 μM) and Marburg virus (MARV, IC₅₀=2.7 μM) inhibitor.

EBOV-IN-8 (Compound 30) inhibits Ebola pseudotyped virus (pEBOV) infection with an IC₅₀ of 62.1% at 10 μM.

As-358 has inhibitory effects against Ebola virus and Marburg virus, with IC₅₀s of 47.5 μM and 3.7 μM.

Cephaeline hydrochloride ((-)-Cephaeline hydrochloride) is a phenolic alkaloid in Indian Ipecac roots. Cephaeline hydrochloride exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections.

EBOV/MARV-IN-3 (compound 32) is a potent EBOV and MARV inhibitor with IC₅₀ values of 0.5, 1.2 µM, respectively. EBOV/MARV-IN-3 binds to the hydrophobic pocket close to EBOV Y517. EBOV/MARV-IN-3 shows antiviral activity.

EBOV-IN-4 (compound 12), a benzothiazepine, is a potent Ebola virus (EBOV) inhibitor with 64.9% inhibitory for EBOV-GP-pseudotype virus (pEBOV) with 10 μM. EBOV-IN-4 is inactive with ASFV.

As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC₅₀s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety.

CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC₅₀s of 3.4 μM and 29.5 μM, respectively. CP19 has SI values of 29.4 and 3.4 for EBOV and MARV, respectively. CP19 has antiviral activity.

EBOV-IN-3 (compound 9) is benzothiazepine compound. EBOV-IN-6 has anti-pEBOV activity with a IC₅₀ value of 0.37 μM.

EBOV-IN-9 (compound 2b) is Diphyllin derivative that blocks Ebola viral entry with an EC₅₀ of 40 nM. EBOV-IN-9 against EBOV-infected monocyte-derived macrophages with an EC₅₀ of 107 nM.

pEBOV-IN-1 (Comp 2) is a pEBOV inhibitor, with an EC₅₀ value of 0.38 μM. pEBOV: pseudotyped Ebola virus.

EBOV-GP-IN-1 (Compound 28) is a potent Ebola entry inhibitor with an IC₅₀ of 0.05 μM against Ebola virus envelope glycoprotein (EBOV-GP).