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3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells .
Coronastat is a potent inhibitor of the SARS-CoV-2 3CL protease. The SARS-CoV-2 3CL protease is a critical agent target for small molecule COVID-19, given its likely agentgability and essentiality in the viral maturation and replication cycle .
SARS-CoV-2 3CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-2 3CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases .
Bardoxolone (RTA 401; CDDO) is an orally active activator of nuclear regulatory factor (NRf-2) and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone inhibits SARS-CoV-2 3CL protease with an EC50 value of 0.43 μM in vero cells. Bardoxolone also inhibits necroptosis in HT-29 cells with an EC50 value of 1.30 μM by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. Bardoxolone can be used in research on COVID-19, TNF-induced systemic inflammatory response syndrome (SIRS), and cerebral ischemia-reperfusion injury .
Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity .
Antcin B is a SARS-CoV-2 3-chymotrypsin-like protease (3CL Pro) inhibitor. Antcin B binds to multiple key amino acid residues of 3CL Pro(such as Leu141, Asn142, Glu166, His163, etc.) through hydrogen bonds, salt bridges, and hydrophobic interactions, thereby inhibiting the activity of 3CL Pro, blocking the cleavage process of viral polyproteins, and suppressing the replication of the SARS-CoV-2 virus in host cells. Antcin B is promising for research of COVID-19 .
SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomer
of the octahydroisochromene scaffold, directs the P1 site imidazole .
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CLpro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research .
SARS-CoV-2-IN-71 (compound 8h) is a potent inhibitor of SARS-CoV-2. SARS-CoV-2-IN-71 inhibits coronavirus replication at multiple stages. SARS-CoV-2-IN-71 displays anti-coronaviral effect by simultaneously acting on 3CLpro and TMPRSS2 .
Cinanserin (SQ 10643) is a potent and selective 5-HT2 antagonist with Ki values of 41, 3500 nM for 5-HT2, 5-HT1, respectively. Cinanserin also is a SARS-CoV 3CLpro inhibitor with an KD value of 49.4, 18.2 µM for SARS-CoV 3CLpro, HCoV-229E 3CLpro, respectively. Cinanserin reduces systemic burn edema levels [3].
VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) with a Ki value of 0.55 nM and SARS-CoV-2 3CLpro(3CL-PR) with a Ki value of 2.6 nM. VK13 exhibits anti-CoV-2 activity with an EC50 of 1.25 μM .
D1N8 is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 and CC50 values of 0.44 μM and >20 μM, respectively. D1N8 has the potential for the research of anti-SARS-CoV-2 agents targeting 3CLpro .
INSCoV-614(1B) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CLpro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
INSCoV-600K(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CLpro) are involved with transcription and replication of the virus. INSCoV-600K(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
INSCoV-601I(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CLpro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-2 3CLpro (SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CLpro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research .
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CLpro. 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral agents. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases .
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease(3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease(3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
PF-00835231 is a CoV-2 cysteine 3C-like protease (3CLpro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CLpro, respectively. PF-00835231 is developed for the research of anti-SARS-CoV-2/COVID-19. PF-00835231 can inhibit cell infections and also suppress infections in animal models [3].
DB12055 (MK-0767 analog) is a covalent SARS-CoV-2 3CL protease inhibitor. DB12055 has the potential for the study of dyslipidemia and diabetes mellitus .
Antiviral agent 25 (compound 6g) is a new non-peptide analog covalent inhibitor of SARS-CoV-2 3CLpro. Antiviral agent 25 has a strong inhibitory effect on SARS-CoV-2 3CLpro and SARS-CoV-2 PL pro with IC50 values of 0.118 µM, 0.448 µM, respectively. Antiviral agent 25 has antiviral effect on SARS-CoV-2 with an EC50 value of 7.249 µM .
Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease [3].
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CLpro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CLpro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 4.09 μM .
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Ritonavir (Standard) is the analytical standard of Ritonavir. This product is intended for research and analytical applications. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Walrycin B, an analogue of toxoflavin, is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 of 0.26 μM. Walrycin B is a WalR response regulator inhibitor. Walrycin B has potent activity of inhibiting bacteria growth .
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM . Asunaprevir inhibits SARS-CoV-2 3CLpro activity .
Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections .
SARS-CoV-2 3CLpro-IN-30 (compound 29) is a potent inhibitor of SARS-CoV-2 3CL protease (SARS-CoV-2 3CLpro), with the IC50 and EC50 of 0.04 and 0.3 μM .
SARS-CoV-2 3CLpro-IN-13 is a potent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 21 nM. SARS-CoV-2 3CLpro-IN-13 shows anti-coronavirus activity .
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 µM [3] .
Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Z-L(D-Val)G-CHN2 is the isoform of Z-LVG-CHN2 (HY-108137). Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease [3].
Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM [3].
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM [3].
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 μM [3] .
Bardoxolone (Standard) is the analytical standard of Bardoxolone (HY-14909). This product is intended for research and analytical applications. Bardoxolone is an orally active activator of nuclear regulatory factor (NRf-2) and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone inhibits SARS-CoV-2 3CL protease with an EC50 value of 0.43 μM in vero cells. Bardoxolone also inhibits necroptosis in HT-29 cells with an EC50 value of 1.30 μM by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. Bardoxolone can be used in research on COVID-19, TNF-induced systemic inflammatory response syndrome (SIRS), and cerebral ischemia-reperfusion injury .
ZK-806450 is a compound with antiviral activity. ZK-806450 has a high binding potential to the allosteric binding site of the SARS-CoV-2 3CL protease. ZK-806450 can also specifically and stably bind to the GAG site of the dengue virus envelope protein .
Bardoxolone (CDDO; RTA 401) methyl is an orally active and brain-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) [3] .
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM .
CMX990 is a SARS-CoV-2 3CL protease inhibitor. The EC90s for inhibiting SARS-CoV-2 were 9.6 nM and 101 nM in human bronchial epithelial cells (HBECs) and HeLa-ACE2 cells, respectively. CMX990 has good ADME and pharmacokinetic properties .
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease . Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM [3].
Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay [3] . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
Amprenavir- 13C6 (VX-478- 13C6) is 13C labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
MAC-5576 is a SARS-CoV-2 3CL protease inhibitor, with an IC50 of 81 nM. MAC-5576 also inhibits 3CLpro (IC50=0.5 μM), HAV 3Cpro (IC50=0.5 μM), and thrombin (IC50=13 μM) .
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor [3] .
Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor [3] .
SARS-CoV-IN-5 (compound 49) is a highly selective, nonpeptidic and noncovalent 3CLpro inhibitor with IC50s of 38 nM, 21.1 nM and 86 nM for 3CLpro of SARS-CoV-1, SARS-CoV-2, Bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 delta variant with an EC50 of 0.272 μM. SARS-CoV-IN-5 significantly reduces the lung viral copies in a K18-hACE2 transgenic mouse model. SARS-CoV-IN-5 has good target-specific and potential broad-spectrum anticoronavirus activities against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9 .
Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3].
SARS-CoV-2 3CLpro-IN-27 (Compound 9H) is an inhibitor of SARS-CoV-2 3CLpro with an IC50 value of 21 nM. SARS-CoV-2 3CLpro-IN-27 exhibits excellent anti-SARS-CoV-2 replicon activity, demonstrating an EC50 value of 5 nM .
Nirmatrelvir (Standard) is the analytical standard of Nirmatrelvir. This product is intended for research and analytical applications. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor [3] .
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 [3].
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM [3].
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide [3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity .
Velpatasvir (Standard) is the analytical standard of Velpatasvir. This product is intended for research and analytical applications. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM .
Boceprevir (Standard) is the analytical standard of Boceprevir. This product is intended for research and analytical applications. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay [3] . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
SARS-CoV-2 3CLpro-IN-21 (Compound D6) irreversibly and covalently inhibits SARS-CoV-2 3CLpro with an IC50 of 0.03 μM. SARS-CoV-2 3CLpro-IN-21 also inhibits SARS-CoV-13CL pro with an IC50 of 0.12μM .
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM [3].
SARS-CoV-2 3CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-2 3CL protease (3CLpro). SARS-CoV-2 3CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds .
Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
Tipranavir (Standard) is the analytical standard of Tipranavir. This product is intended for research and analytical applications. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CLpro activity [3].
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir inhibits SARS-CoV-2 3CLpro activity [3].
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir sodium salt inhibits SARS-CoV-2 3CLpro activity [3].
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir hydrate inhibits SARS-CoV-2 3CLpro activity [3].
Velpatasvir-d3(GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM [3].
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir potassium salt inhibits SARS-CoV-2 3CLpro activity [3].
(S)-Velpatasvir- 13C,d3 ((S)-GS-5816- 13C,d3) is 13C labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM [3].
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM [3].
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CLpro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 [3] .
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
SARS-CoV-2 3CLpro-IN-31 (Compound 13c) is a potent SARS-CoV-2 3CL protease (3CLpro) inhibitor of with an IC50 value of 37.33 nM. SARS-CoV-2 3CLpro-IN-31 blocks viral polyprotein cleavage and inhibits SARS-CoV-2 replication. SARS-CoV-2 3CLpro-IN-31 is promising for research of SARS-CoV-2 infection .
[Ru(phen)3]Cl2 is an important photocatalyst with photosensitivity and has the activity of promoting reactions in the fields of organic synthesis and photoelectrochemistry. [Ru(phen)3]Cl2 can drive chemical reactions under light conditions and shows good catalytic performance. [Ru(phen)3]Cl2's applications include photocatalytic water decomposition and synthesis of complex organic molecules.
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM [3].
Indinavir- 13C4, 15N (MK-639 (free base)- 13C4, 15N) is 13C and 15N labeled Indinavir. Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor [3] .
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome [3].
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome [3].
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity [3]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) [3] .
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) [3] .
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM) . Danoprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 0.05 μM [3].
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3] .
CX3CL1 Human Pre-designed siRNA Set A contains three designed siRNAs for CX3CL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cx3cl1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cx3cl1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cx3cl1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cx3cl1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
(2R)-Atecegatran ((2R)-AZD-0837; (Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab)) is a thrombin inhibitor. (2R)-Atecegatran can be used in research related to thromboembolic disorders .
SARS-CoV-2 Mpro-IN-10 (27h) is a potent M pro inhibitor with IC50 value and EC50 values of 10.9 nM and 43.6 nM, respectively. SARS-CoV-2 Mpro-IN-10 can be used for the research of SARS-CoV-2 virus .
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [3] .
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3].
COVID-19 poses a serious threat to people's health, and it is urgent to develop drugs to treat COVID-19 quickly. The screening of anti-COVID-19 drugs by using the clinical and approved compounds can greatly shorten the research and development cycle. In addition, the virtual screening technology can effectively narrow the scope of screening and improve the screening efficiency in the pre-screening of new drugs.
Taking advantage of our virtual screening, we conduct virtual screening of approved compound library and clinical compound library based on the 3CL protease (PDB ID: 6LU7), Spike Glycoprotein (PDB ID: 6VSB), NSP15 (PDB ID: 6VWW), RDRP, PLPro and ACE2 (Angiotensin Converting Enzyme 2) structure. We design a unique collection of 1,449 compounds which may have anti-COVID-19 activity. Anti-COVID-19 Compound Library will be a powerful tool for screening new anti-COVID-19 activity drugs.
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3].
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3].
Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity .
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 [3].
Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
Antcin B is a SARS-CoV-2 3-chymotrypsin-like protease (3CL Pro) inhibitor. Antcin B binds to multiple key amino acid residues of 3CL Pro(such as Leu141, Asn142, Glu166, His163, etc.) through hydrogen bonds, salt bridges, and hydrophobic interactions, thereby inhibiting the activity of 3CL Pro, blocking the cleavage process of viral polyproteins, and suppressing the replication of the SARS-CoV-2 virus in host cells. Antcin B is promising for research of COVID-19 .
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
SARS-CoV-2 3CLpro/3C-like protease Protein is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by E. coli, with tag free.
SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) is the recombinant virus-derived SARS-CoV-2 3CLpro/3C-like protease, expressed by E. coli , with tag Free labeled tag. ,
SARS-CoV-2 3C-like Proteinase (His), His, expressed in E.coli, mediates viral polyprotein maturation and multiple cleavages of host proteins to modulate viral translation and transcription with a His tag at the N-terminus.
SARS-CoV-2 3C-like Proteinase (His), His, expressed in E.coli, mediates viral polyprotein maturation and multiple cleavages of host proteins to modulate viral translation and transcription with a His tag at the N-terminus.
SARS-CoV-2 3CLpro/3C-like protease Protein (His-Avi) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by E. coli, with N-His, N-Avi labeled tag.
SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by Sf9 insect cells, with N-His labeled tag.
SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His-Avi) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by Sf9 insect cells, with N-His, N-Avi labeled tag.
The Fractalkine/CX3CL1 protein is a member of the intercrine beta family and plays a key role in chemokines that are critical for intercellular communication and immune responses. In this family, Fractalkine/CX3CL1 may significantly regulate inflammatory processes and cellular interactions. Fractalkine/CX3CL1 Protein, Canine (HEK293) is the recombinant canine-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with tag free.
The Fractalkine/CX3CL1 protein is a member of the intercrine beta family and plays a key role in chemokines that are critical for intercellular communication and immune responses. In this family, Fractalkine/CX3CL1 may significantly regulate inflammatory processes and cellular interactions. Fractalkine/CX3CL1 Protein, Canine (HEK293, Fc) is the recombinant canine-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-hFc labeled tag.
The Fractalkine/CX3CL1 protein is a member of the intercrine beta family and plays a key role in chemokines that are critical for intercellular communication and immune responses. In this family, Fractalkine/CX3CL1 may significantly regulate inflammatory processes and cellular interactions. Fractalkine/CX3CL1 Protein, Canine (HEK293, His) is the recombinant canine-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-His labeled tag.
The Fractalkine/CX3CL1 protein is a multifunctional chemokine that binds to CX3CR1 and the integrins ITGAV:ITGB3 and ITGA4:ITGB1.It regulates immune responses, inflammation, cell adhesion, and chemotaxis.Fractalkine/CX3CL1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-6*His labeled tag.
Fractalkine/CX3CL1 protein, a chemokine, binds CX3CR1 and integrins ITGAV:ITGB3 and ITGA4:ITGB1. It regulates immune response, inflammation, adhesion, chemotaxis, and leukocyte migration. It activates integrins via CX3CR1-dependent and -independent pathways, binding to site 1 with CX3CR1 and site 2 without CX3CR1. Soluble Fractalkine/CX3CL1 attracts T-cells and monocytes, not neutrophils. Fractalkine/CX3CL1 Protein, Cynomolgus (HEK293, Fc) is the recombinant Cynomolgus-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-hFc labeled tag.
Fractalkine/CX3CL1 protein, a chemokine, binds CX3CR1 and integrins ITGAV:ITGB3 and ITGA4:ITGB1. It regulates immune response, inflammation, adhesion, chemotaxis, and leukocyte migration. It activates integrins via CX3CR1-dependent and -independent pathways, binding to site 1 with CX3CR1 and site 2 without CX3CR1. Soluble Fractalkine/CX3CL1 attracts T-cells and monocytes, not neutrophils. Fractalkine/CX3CL1 Protein, Cynomolgus (HEK293, His) is the recombinant Cynomolgus-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-His labeled tag.
Fractalkine/CX3CL1 protein, a chemokine, binds CX3CR1 and integrins ITGAV:ITGB3 and ITGA4:ITGB1. It regulates immune response, inflammation, adhesion, chemotaxis, and leukocyte migration. It activates integrins via CX3CR1-dependent and -independent pathways, binding to site 1 with CX3CR1 and site 2 without CX3CR1. Soluble Fractalkine/CX3CL1 attracts T-cells and monocytes, not neutrophils. Fractalkine/CX3CL1 Protein, Human (315a.a, HEK293, His) is the recombinant human-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-His labeled tag.
The Fractalkine/CX3CL1 protein is a multifunctional chemokine that binds to CX3CR1 and the integrins ITGAV:ITGB3 and ITGA4:ITGB1.It regulates immune responses, inflammation, cell adhesion, and chemotaxis.Fractalkine/CX3CL1 Protein, Mouse (Biotinylated, HEK293, His-Avi) is the recombinant mouse-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
Fractalkine/CX3CL1 is a chemokine that acts as a ligand to CX3CR1 and the integrins ITGAV: ITGB3 and ITGA4: ITGB1. CX3CL1 promotes lung cancer cell migration and invasion through the Src/FAK signaling pathway. CX3CL1 plays an important role in immune response, inflammation, cell adhesion and chemotaxis. Fractalkine/CX3CL1 Protein, Human (Biotinylated, HEK293, His, Avi) is the recombinant human-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-Avi, C-10*His labeled tag.
The Fractalkine/CX3CL1 protein is a member of the intercrine beta family and plays a key role in chemokines that are critical for intercellular communication and immune responses. In this family, Fractalkine/CX3CL1 may significantly regulate inflammatory processes and cellular interactions. Fractalkine/CX3CL1 Protein, Cynomolgus (317a.a, HEK293, His) is the recombinant cynomolgus-derived Fractalkine/CX3CL1 protein, expressed by HEK293 , with C-His labeled tag.
Fractalkine/CX3CL1 protein is a versatile chemokine that acts as a ligand for CX3CR1 and integrins ITGAV:ITGB3 and ITGA4:ITGB1. It regulates immune response, inflammation, adhesion, and chemotaxis. It activates integrins via CX3CR1-dependent and -independent pathways, binding to site 1 with CX3CR1 and site 2 without CX3CR1. Soluble Fractalkine/CX3CL1 attracts T-cells and monocytes, not neutrophils. Fractalkine/CX3CL1 Protein, Rat is the recombinant rat-derived Fractalkine/CX3CL1 protein, expressed by E. coli , with tag free.
The Fractalkine/CX3CL1 protein is a multifunctional chemokine that binds to CX3CR1 and the integrins ITGAV:ITGB3 and ITGA4:ITGB1. It regulates immune responses, inflammation, cell adhesion, and chemotaxis. Fractalkine/CX3CL1 Protein, Mouse is the recombinant mouse-derived Fractalkine/CX3CL1 protein, expressed by E. coli , with tag free.
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Amprenavir- 13C6 (VX-478- 13C6) is 13C labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM [3].
Velpatasvir-d3(GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM [3].
(S)-Velpatasvir- 13C,d3 ((S)-GS-5816- 13C,d3) is 13C labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM [3].
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM [3].
Indinavir- 13C4, 15N (MK-639 (free base)- 13C4, 15N) is 13C and 15N labeled Indinavir. Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor [3] .
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [3] .
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity [3]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3] .
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [3] .
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
CX3CL1 Human Pre-designed siRNA Set A contains three designed siRNAs for CX3CL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cx3cl1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cx3cl1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cx3cl1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cx3cl1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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