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News - SARS-CoV-2 small molecules

Small molecules for SARS-CoV-2 research

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The novel coronavirus SARS-CoV-2 is rapidly spreading around the globe causing tens of thousands of cases of COVID-19.  As of yet, there are no agents clinically validated to help stop the spread of this virus.   Gordon et al. recently identified 332 SARS-CoV-2-human protein-protein interactions and 67 druggable human proteins as potential targets for developing therapeutics (note that this paper has not yet been subject to peer review).  Focus Biomolecules has created a chart of these targets and validated small molecule modulators.  These are all in stock and ready for immediate shipment.

MC# Name Primary activity COVID-19 rationale
10-1009 Na Valproate 2 HDAC inhibitor HDAC2 interacts with SARS-CoV-2 Nsp5
10-1062 Cycloheximide-N-ethylethanoate2 FKBP12 inhibitor mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-1089 Nafamostat mesylate2 Serine protease inhibitor Targets viral cell entry via inhibition of ACE2
10-1103 FK-5062 FKBP inhibitor mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-1104 Rapamycin2 mTOR inhibitor mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-1105 PKC-412 (Midostaurin)2 Protein kinase inhibitor (pan specific) Inhibits MARK2/3, which interact with SARS-CoV-2 Orf9b
10-1111 Verapamil2 L-type Ca2+ channel blocker Targets Multidrug resistance-associated protein 1 (MRP1), which interacts with SARS-CoV-2 Orf9c
10-1281 Ribavirin2 Antiviral agent Inhibits IMPDH2, which interacts with SARS-CoV-2 Nsp14
10-1311 MLN4924 (Pevonedistat)2 Nedd8 activating enzyme inhibitor Targets Cullin2, which interacts with SARS-CoV-2 Orf10
10-1361 JQ12 Bromodomain inhibitor SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4
10-1379 Hydroxychloroquine sulfate
Autophagy inhibitor In clinical trials (alongside chloroquine) for SARS-CoV-2 infection
10-1458 GBR-12909
Dopamine reuptake inhibitor Sigma receptor agonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-1487 RVX-2082 BET bromodomain inhibitor SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4
10-1569 Dabrafenib (GSK2118436)2 B-Raf mutant inhibitor Inibits NEK9, which interacts with SARS-CoV-2 Nsp9
10-2025 Entacapone2 COMT inhibitor COMT interacts with SARS-CoV-2 Nsp7
10-2057 Apicidin2 HDAC inhibitor HDAC2 interacts with SARS-CoV-2 Nsp5
10-2059 Ascomycin
FKBP ligand mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-2060 Bafilomycin A12 Vacuolar H+ ATPase inhibitor V1-ATPase subunits interact with SARS-CoV-2 Nsp6 and M
10-2087 Mycophenolic acid2 Immunosuppressant Inhibits IMPDH2, which interacts with SARS-CoV-2 Nsp14
10-2144 H892 PKA inhibitor PKA interacts with SARS-CoV-2 Nsp13
10-2196 Camostat mesylate1,2 Serine protease inhibitor Targets viral cell entry via inhibition of ACE2
10-2253 Captopril2 ACE inhibitor Targets viral cell entry via inhibition of ACE2
10-2429 Daunorubicin2 DNA damaging agent Targets Multidrug resistance-associated protein 1 (MRP1), which interacts with SARS-CoV-2 Orf9c
10-2469 Metformin2 Antidiabetic agent Indirect modulator of mTORC1 complex; mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-2473 Chloroquine phosphate2 Autophagy inhibitor Sigma 1 receptor binder (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-2474 Niclosamide3 STAT3 signaling inhibitor Regulates mTORC1 pathway, whose members interact with SARS-CoV-2 N and Orf8 proteins
10-2631 Triptolide
NFkB transcriptional activation inhibitor Also directly inhibits dCTP pyrophosphatase 1 (DCTPP1), which interacts with SARS-CoV-2 Orf9b
10-3362 INK-128 (Sapanisertib)2 mTOR inhibitor mTORC1 pathway members interact with SARS-CoV-2 N and Orf8 proteins
10-3613 Santacruzamate A
Ultrapotent HDAC2 inhibitor HDAC2 interacts with SARS-CoV-2 Nsp5
10-3900 Tigecycline2 Antibiotic Like Azithromycin, has off-target effect on mitochondrial ribosomes, components of which interact with the SARS-CoV-2 Nsp8 protein
10-3970 N4-Hydroxycytidine4 Novel antiviral Has antiviral activity against SARS-CoV-2
10-4003 Pridopidine
Sigma-1 Ligand Sigma 1 receptor agonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4030 Bromosporine
Pan-bromodomain inhibitor SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4
10-4121 BI 2536
Dual Plk/BRD4 inhibitor SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4
10-4122 I-BET762
BET Bromodomain inhibitor SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4
10-4200 NE-100
Selective sigma-1 antagonist Sigma 1 receptor antagonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4201 S1RA (E-52862)2 Selective sigma-1 antagonist Sigma 1 receptor antagonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4203 PRE084
Selective sigma-1 agonist Sigma 1 receptor agonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4204 DTG
High affinity sigma receptor agonist Sigma receptor agonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4210 BD1047 dihydrobromide
Selective sigma-1 antagonist Sigma 1 receptor antagonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4219 SA4503
Potent and selective sigma 1 agonist Sigma 1 receptor agonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor)
10-4511 Ruxolitinib2 JAK inhibitor Inhibits MARK2/3, which interact with SARS-CoV-2 Orf9b
10-4544 7-Cl-O-Nec1
RIPK1 inhibitor RIP kinase 1 interacts with SARS-CoV-2 Nsp12
10-4611 RIPA-56
RIP1 inhibitor (more potent than 7-Cl-Nec1) RIP kinase 1 interacts with SARS-CoV-2 Nsp12
10-4818 Volasertib
Polo-like Kinase 1 inhibitor Also inhibits BRD4; SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4



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