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 Á¦Ç°¾È³»  ºÐÀÚ»ý¹°ÇР  COVID-19 Research

[COVID-19] Tocris compounds & inhibitors

SARS-CoVÀÇ homology¿Í 80% ÀÏÄ¡ÇÏ´Â COVID-19´Â, ÃÖ±Ù ¿¬±¸¿¡ µû¸£¸é human mucosal Ç¥¸éÀÇ ACE2¿¡ virus Ç¥¸éÀÇ spike°¡ binding µÇ¾î virus°¡ ¼÷ÁÖ¼¼Æ÷¿¡ °áÇյǴ mechanismÀ¸·Î ÀÌ·¯ÇÑ mechanismÀº antiviral ¾à¹° Ä¡·á¸¦ À§ÇÑ targetÀ¸·Î ¾Ë·ÁÁ® ÀÖÀ¸¸ç, COVID-19 ȯÀÚ Ç÷¾×¿¡¼­ ¸é¿ª¼¼Æ÷ÀÇ Áõ°¡ ¶ÇÇÑ Áõ¸í ÇÏ¿´½À´Ï´Ù.

±âÁ¸ ¿¬±¸¸¦ ÅëÇØ ¿ªÇÒÀÌ È®ÀÎµÈ compound Áß COVID-19 ±âÀü°ú °ü·ÃÀÌ ÀÖ´Â ¾à¹°µéÀ» ¾È³»µå¸³´Ï´Ù.

TOCRIS
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¡¡ Cat. No. Product Name / Activity
¡¡ 4274 AP 24534
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; potent multi-kinase and pan-Bcr-Abl inhibitor
¡¡ 7283 Apilimod dimesylate 
¡¡ ¡¡ Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions; potent and selective PIKfyve inhibitor
¡¡ 7235 Arbidol 
¡¡ ¡¡ Inhibits replication of SARS-CoV-2 in vitro; broad spectrum antiviral
¡¡ 6358 Atovaquone
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; DHODH inhibitor
¡¡ 4600 Auranofin
¡¡ ¡¡ Inhibits SARS-CoV-2 infection in vitro
¡¡ 7222 Baricitinib 
¡¡ ¡¡ In silico modelling predicts inhibition of SARS-CoV-2 cell entry; highly potent JAK inhibitor
¡¡ 3193 Camostat mesylate
¡¡ ¡¡ Inhibits entry of SARS-Cov-2 into lung cells; TMPRSS2 inhibitor
¡¡ 4109 Chloroquine diphosphate
¡¡ ¡¡ Inhibits SARS-CoV-2 infection in vitro
¡¡ 6357 Ciclesonide
¡¡ ¡¡ Inhibits replication of SARS-CoV-2 in vitro; glucocorticoid
¡¡ 0460 Cinanserin hydrochloride
¡¡ ¡¡ Inhibits replication of SARS-CoV; Mpro inhibitor and 5-HT2 antagonist
¡¡ 0970 Cycloheximide
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; protein synthesis inhibitor
¡¡ 1101 Cyclosporin A
¡¡ ¡¡ Inhibits coronavirus replication; cyclophilin inhibitor
¡¡ 7223 Dabrafenib mesylate 
¡¡ ¡¡ Targets human proteins in the SARS-CoV-2 interactome; potent and selective B-Raf, CDK16 and NEK9 inhibitor
¡¡ 1467 Daunorubicin hydrochloride
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; DNA topoisomerase II inhibitor
¡¡ 4583 Digoxin
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; Na+/K+ ATPase inhibitor
¡¡ 3807 Disulfiram
¡¡ ¡¡ SARS-CoV-2 Mpro inhibitor; also reversibly stimulates SERCA Ca2+-ATPase
¡¡ 4545 E 64d
¡¡ ¡¡ Inhibts entry of SARS-CoV-2 into lung cells in combination with Camostat (Cat. No. 3193); cathepsin inhibitor
¡¡ 3631 FK 506
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; potent calcineurin inhibitor
¡¡ 3259 Gemcitabine hydrochloride
¡¡ ¡¡ Inhibits replication of coronaviruses; DNA synthesis inhibitor
¡¡ 7280 GRL 0617 
¡¡ ¡¡ Coronavirus PLpro inhibitor
¡¡ 7227 GS 441524 
¡¡ ¡¡ Displays antiviral activity against MERS-CoV, SARS-CoV and SARS-CoV-2; viral RNA-dependent RNA polymerase (RdRp) inhibitor; active metabolite of Remdesivir (Cat. No. 7226)
¡¡ 1416 Homoharringtonine
¡¡ ¡¡ Inhibits SARS-CoV-2 infection in vitro; inhibits protein synthesis
¡¡ 5648 Hydroxychloroquine sulfate
¡¡ ¡¡ Inhibits SARS-CoV-2 viral infection in vitro
¡¡ 1708 Indomethacin
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome
¡¡ 1260 Ivermectin
¡¡ ¡¡ Inhibits replication of SARS-Cov-2 in vitro; antiparasitic and antiviral
¡¡ 2959 Lercanidipine hydrochloride
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; CaV1.x blocker
¡¡ 3765 Linezolid
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; antibiotic
¡¡ 0840 Loperamide hydrochloride
¡¡ ¡¡ Inhibits replication of coronaviruses in vitro; peripherally acting μ opioid agonist and Ca2+ channel blocker
¡¡ 7052 Lopinavir 
¡¡ ¡¡ Inhibits SARS-CoV-2 replication in vitro; highly potent and selective HIV-1 protease inhibitor
¡¡ 6819 Mefloquine hydrochloride
¡¡ ¡¡ Exhibits antiviral activities against SARS-CoV-2; also Cx36 and Cx50 gap channel blocker
¡¡ 2864 Metformin hydrochloride
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; antidiabetic
¡¡ 7230 MPro N3 
¡¡ ¡¡ Coronavirus Mpro inhibitor
¡¡ 3766 Nelfinavir mesylate
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; potent HIV-1 protease inhibitor
¡¡ 2583 Omeprazole
¡¡ ¡¡ Enhances anti-SARS-CoV-2 activity of serine protease inhibitors
¡¡ 1076 Ouabain
¡¡ ¡¡ Exhibits anti-MERS-CoV activity in vitro; Na+/K+ ATPase inhibitor
¡¡ 1125 Quercetin
¡¡ ¡¡ Inhibits SARS-CoV Mpro; also non-selective PI 3-kinase inhibitor
¡¡ 1292 Rapamycin
¡¡ ¡¡ Inhibits MERS-CoV infection; mTOR inhibitor and immunosuppressant
¡¡ 7226 Remdesivir 
¡¡ ¡¡ Displays antiviral activity against MERS-CoV, SARS-CoV and SARS-CoV-2; viral RNA-dependent RNA polymerase (RdRp) inhibitor
¡¡ 4501 Ribavirin
¡¡ ¡¡ Inhibits cytopathic effect of SARS-CoV in vitro; guanosine analog and IMPDH inhibitor
¡¡ 7064 Ruxolitinib
¡¡ ¡¡ Targets human proteins in the SARS-CoV-2 interactome; potent and selective JAK1/JAK2 inhibitor
¡¡ 7191 Santacruzamate A 
¡¡ ¡¡ Identified as targeting human host proteins that interact with SARS-CoV-2
¡¡ 7189 Saracatinib 
¡¡ ¡¡ Inhibits MERS-CoV, other coronaviruses and dengue virus
¡¡ 2815 Valproic acid, sodium salt
¡¡ ¡¡ Identified as targeting human proteins in the SARS-CoV-2 interactome; HDAC inhibitor
¡¡ 0654 Verapamil hydrochloride
¡¡ ¡¡ Targets human proteins in the SARS-CoV-2 interactome; CaV1.x blocker
¡¡   ¡¡

 

 ACE Small Molecule Compound
Cat.No. Product Description
2578 Benazepril hydrochloride ACE inhibitor
4302 Perindopril erbumine ACE inhibitor
4455 Captopril ACE inhibitor also inhibits LTA4 hydrolase
¡¡ ¡¡ ¡¡
 Cathepsin B/L Small Molecule Compounds
Cat.No. Product Description
0448 Calpeptin Calpain and cathepsin L inhibitor
3625 SID 26681509 Cathepsin L inhibitor
4863 CA 074 Selective cathepsin B inhibitor
0384 N-Acetyl-L-leucyl-
L-leucyl-L-methional
Cathepsin inhibitor
4545 E 64d Cathepsin inhibitor; interferes with autolysosomal digestion
1146 MDL 28170 Potent and selective Calpain and Cathepsin B inhibitor 
¡¡ ¡¡ ¡¡
 IL-1 beta Small Molecule Compound
Cat.No. Product Description
1793 AF 12198 potent, selective human type IL-1 receptor antagonist
¡¡ ¡¡ ¡¡
 TNF-alpha Small Molecule Compound
Cat.No. Product Description
5484 C 87 TNF-α inhibitor
¡¡ ¡¡ ¡¡
 VEGFR-2 Small Molecule Compounds
Cat.No. Product Description
3882 (E)-FeCP-oxindole Selective VEGFR-2 inhibitor
2542 Ki 8751 potent, selective VEGFR-2 inhibitor
 Aminopeptidase Small Molecule Compounds
Cat.No. Product Description
3595 CHR 2797 Aminopeptidase inhibitor, also called Tosedostat
¡¡ ¡¡ ¡¡
 DPPIV/CD26 Small Molecule Compounds
Cat.No. Product Description
2783 DPPI 1c DPPIV/CD26 inhibitor
2790 K 579 DPPIV/CD26 inhibitor
3506 NVP DPP 728 Potent DPPIV/CD26 inhibitor; orally active
6507 Saxagliptin High affinity DPPIV/CD26 inhibitor; active in vivo
¡¡ ¡¡ ¡¡
 Human Neutrophil Elastase 1 (HNE1) Small Molecule Compounds
Cat.No. Product Description
5651 ONO 6818 High affinity and selective Human Neutrophil Elastase 1 (HNE1) inhibitor; orally active
5706 BAY 678 Potent Human Neutrophil Elastase (HNE) inhibitor;
cell permeable
6389 BAY 677 Inactive control for BAY 678 (Catalog # 5706)
¡¡ ¡¡ ¡¡
 Furin Small Molecule Compounds
Cat.No. Product Description
1793 AF 12198 Potent Furin inhibitor
¡¡ ¡¡ ¡¡
 TMPRSS2 Small Molecule Compounds
Cat.No. Product Description
3193 Camostat TMPRSS2 inhibitor
3081¡¡

Nafamostat¡¡

Inhibits SARS-CoV-2 infection in vitro
¡¡
 Autophagy Small Molecule Compounds
Cat.No. Product Description
5648 Hydroxychloroquine sulfate   Autophagy inhibitor, also inhibits TLR9; inhibits SARS-CoV-2 viral infection
¡¡ ¡¡ ¡¡
 Topo I inhibitor
Cat. No. product size
TG4100 Topotecan Hydrochloride
(Hycamtin)
0.25 mL
TG4101 Irinotecan (CPT-11) 0.25 mL
TG4110 Camptothecin 0.25 mL
¡¡ ¡¡ ¡¡
 Topo II inhibitor
Cat. No. product size
TG4140 Etoposide (VP16) 0.25 mL
 ¢¹ There is current research linking the inhibition of topoisomerase and the "cytokine storm"  that follows SAR CoV2 infections (COVID-19).

 

  ¢º Drug Repurposing (¾à¹°ÀçâÃâ) : Tocriscreen Compound Library º¸·¯°¡±â




¡¡ SARS-CoV-2 Viral Lifecyle. Host cell entry is effected by the binding of receptor binding domain (RBD) of the spike (S) protein on the nucleocapsid to ACE2, a protease on the host cell surface. The binding of the S protein to ACE2 is facilitated by another host cell protease, TMPRSS2 (transmembrane protease, serine 2). Following binding of S protein the virus is internalized. The internalized virus is uncoated and the SARS-CoV-2 genome is released into the cytoplasm. The viral RNA is then replicated and translated. This generates two polyproteins PP1A and PP1AB. These proteins contain within their sequence, papain-like protease (PLpro) and the coronavirus main protease (Mpro, also known as 3CLpro), which cleave the polyproteins into a variety of other functional proteins. The viral RNA also encodes the structural components of the virus, i.e. spike, nucleocapsid, membrane and envelope proteins. Following reproduction of all the viral components, coronavirus is assembled and released via vesicular exocytosis.


ÁÖ¹®Á¤º¸(Ordering Information)
CATNUM PRODUCT SIZE
3882(E)-FeCp-oxdole10mg
6960ABT 19910 mg
6960ABT 19950 mg
1793AF 12198 1mg
4274AP 2453450 mg
4274AP 2453410 mg
4139Aprotinin10 mg
6358Atovaquone10 mg
6358Atovaquone50 mg
3771Azithromycin50mg
6389BAY 6775 mg
5706BAY 6785 mg
2578Benazepril hydrochloride 50mg
5484C 8710 mg
4863CA 0741 mg
0448Calpeptin 10mg
3193Camostat mesylate10mg
TG4110Camptothecin 10mM0.25ml
4455Captopril50 mg
4109Chloroquine diphosphate50 mg
3595CHR 27971mg
6357Ciclesonide25 mg
6357Ciclesonide5 mg
1364Colchicine 1g
0970Cycloheximide 100mg
1101Cyclosporin A 100mg
6710Darunavir 50 mg
6710Darunavir 10 mg
6793Dasatinib100 mg
1467Daunorubicin hydrochloride 10mg
4583Digoxin50 mg
3807Disulfiram50 mg
2783DPPI 1c hydrochloride1mg
4545E 64d (1 MG)1 mg
TG4140Etoposide 10mM0.25ml
3631FK 50610mg
3259Gemcitabine hydrochloride10mg
3259Gemcitabine hydrochloride50mg
0931Haloperidol hydrochloride 100mg
5648Hydroxychloroquine sulfate10 mg
5906Imatinib mesylate100 mg
1708Indomethacin 100mg
TG4101Irinotecan 10mM0.25ml
1260Ivermectin 100mg
2790K 57910mg
2542Ki 875110mg
2959Lercanidipine hydrochloride10mg
2959Lercanidipine hydrochloride50mg
3765Linezolid10mg
0840Loperamide hydrochloride 1g
3798Losartan potassium50mg
1146MDL 2817010mg
6819Mefloquine hydrochloride50 mg
2864Metformin hydrochloride100mg
0384N-Acetyl-L-leucyl-L-leucyl-L-methional 10mg
3081Nafamostat mesylate10mg
3081Nafamostat mesylate50mg
3766Nelfinavir mesylate10mg
3766Nelfinavir mesylate50mg
3506NVP DPP 728 dihydrochloride10mg
2583Omeprazole 50mg
5651ONO 681810 mg
1076Ouabain 100mg
4302Perindopril erbumine50mg
2992PKC 4121mg
1292Rapamycin 1mg
4501Ribavirin50mg
5856Ritonavir50 mg
7064Ruxolitinib50 mg
4418Saquinavir mesylate50mg
4418Saquinavir mesylate10mg
6507Saxagliptin hydrochloride10 mg
3625SID 2668150910mg
3784Sildenafil citrate10mg
3784Sildenafil citrate50mg
0652Thalidomide 100mg
TG4100Topotecan 10mM0.25ml
2815Valproic acid, sodium salt100mg
0654Verapamil hydrochloride 1g