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HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM [1].
HIV-1 inhibitor-74 (compound 10c) is a potent HIV-1 inhibitor with an EC50 value of 0.0047 µM for HIV-1 IIIB. HIV-1 inhibitor-74 shows cytotoxicity. HIV-1 inhibitor-74 inhibits WT HIV-1 RT activity with an IC50 value of 0.134 µM. HIV-1 inhibitor-74 shows broad-spectrum anti HIV-1 activity [1].
HIV-1 inhibitor-32 (compound 3c) is a potent HIV-1 inhibitor with an IC50 value of 34 nM for WT HIV-1. HIV-1 inhibitor-32 can be used for researching AIDS [1].
HIV-1 inhibitor-81 (Compound 14g) is an HIV-1 protease inhibitor with a Ki of 1.6 nM. HIV-1 inhibitor-81 exhibits certain antiviral activity, with an EC50 of 250 nM for HIV-1[1].
HIV-1 inhibitor-65 (compound 3c) is an inhibitor of HIV-1 (EC50: 2.9 nM) and an activator of protein kinase C (PKC). HIV-1 inhibitor-65 inhibits syncytium formation (EC50: 7.0 nM) and inhibits HIV-1 entry and HIV-1 reverse transcriptase [1].
HIV-1 inhibitor-12 is potent HIV-1 inhibitor. HIV-1 inhibitor-12 inhibits HIV-1 capsid protein polymerization with an IC50 of 9 nM (WO2021104413A1, compound 1-1a) [1].
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection [1].
HIV-1 inhibitor-63 (compound S17) is a potent HIV-1 inhibitor. HIV-1 inhibitor-63 inhibits integrase-Ku70 complex formation with an IC50 value of 12 µM. HIV-1 inhibitor-63 inhibits HIV-1 post-integration DNA repair [1].
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier [1].
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection [1].
HIV-1 inhibitor-68 (compound 26) is a protein kinase C (PKC) activator derivative with reversal activity in HIV-1 latency. HIV-1 inhibitor-68 may be able to eliminate cells latently infected with HIV-1, [1].
HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM [1].
HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM [1].
HIV-1 inhibitor-77 (compound 13) is a HIV-1 inhibitor. HIV-1 inhibitor-77 can neutralize all three tested viruses with the IC50 values of 0.14 μM, 8.28 μM and 2.92 μM for HIV-1CH58TF , HIV-1JRFL and HIV-1AD8, respectively [1].
HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS [1].
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS) [1].
HIV-1 inhibitor-34 (compound 5q) is a potent and selective HIV-1 inhibitor with an EC50 of 6.4 nM for HIV-1 and a CC50 of 16 μM in MT-4 cells. HIV-1 inhibitor-34 can be used for researching AIDS [1].
HIV-1 inhibitor-33 (compound 5n) is a potent and selective HIV-1 inhibitor with an EC50 of 8.6 nM for HIV-1 and a CC50 of 18 μM in MT-4 cells. HIV-1 inhibitor-33 can be used for researching AIDS [1].
HIV-1 inhibitor-38 (Compound 91) is a potent HIV-1. HIV-1 inhibitor-38 has the potential for further development as novel latency reversing agents [1].
HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1. HIV-1 inhibitor-37 has the potential for further development as novel latency reversing agents [1].
HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM [1].
HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM [1].
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent [1].
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability [1].
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT [1].
HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM [1].
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS [1].
HIV-1 inhibitor-76 (compound 9t-2) is a non-nucleoside reverse transcriptase inhibitor of HIV-1. HIV-1 inhibitor-76 can be used in anti-HIV research [1].
HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity [1].
HIV-1 inhibitor-18 (compound II-13c) is a potent HIV-1 capsid inhibitor with an EC50 value of 5.14 μM for HIV-1 NL4-3. HIV-1 inhibitor-18 has certain cytotoxicity (MT-4 cells CC50 >9.51) [1].
HIV-1 inhibitor-18 (compound V-25i) is a potent HIV-1 capsid inhibitor with an EC50 value of 2.57 μM for HIV-1 NL4-3. HIV-1 inhibitor-18 has certain cytotoxicity (MT-4 cells CC50 >8.55) [1].
HIV-1 inhibitor-80 (compound M44) is an HIV-1 inhibitor with an EC50 of 5-148 nM. HIV-1 inhibitor-80 shows good metabolic stability and cytotoxicity in human plasma and human liver microsomes [1].
HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC50 > 227 μM) [1]
HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS [1].
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity [1].
HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS [1].
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM [1].
HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains [1].
HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) [1].
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model [1].
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity [1].
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS [1].
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability [1].
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety [1].
HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC50 =10.2 μM) [1].
HIV-1 inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3 nM for wild-type HIV-1. HIV-1 inhibitor-78 can be used for the research of HIV infection [1].
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS [1].
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants [1].
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants [1].
HIV-1 inhibitor-43 is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24 expression [1].
HIV-1 inhibitor-64 (Compound 7c) is a wild-type HIV-1 inhibitor that effectively suppresses the activity of HIV-1 mutants E138K/Q148K and G140S/Q148R with EC50 values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS [1].
HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity [1].
HIV-1 inhibitor-75 is a human immunodeficiency virus 1(HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes [1].
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM [1].
HIV-1 inhibitor-71 (compound 2a) blocks the transport of endocytosed HIV-1 particles into nuclear envelope invagination (NEIs) that can inhibit productive infection [1].
HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1(HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant [1].
HIV-1 protease-IN-12 (compound 35b) is a HIV-1 protease inhibitor with an IC50 of 0.51 nM. HIV-1 protease-IN-12 also inhibits drug-resistant variant [1].
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch [1].
HIV-1 protease-IN-9 (compound 5b) is a HIV-1 protease inhibitor, with a Ki of 0.028 nM. HIV-1 protease-IN-9 shows potent antiviral activity, with an IC50 of 66.8 nM [1].
HIV-1 inhibitor-47 is an inhibitor of HIV-1, and inhibits vif-dependent degradation of human APOBEC3G, with an IC50 value of 14.33 μM. HIV-1 inhibitor-47 also involves in derivatives of 1-(2-pyrimidinyl)piperazine synthesis, with potential antianxiety, antidepressant, and antipsychotic effect [1] .
HIV-1 protease-IN-11 (compound 34a) is a HIV-1 protease inhibitor with an IC50 of 0.41 nM. HIV-1 protease-IN-11 also exhibits significant activity against drug-resistant variant [1].
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) [1].
HIV-1 inhibitor-79 (Compound 3k) is an HIV inhibitor that exhibits significant inhibitory activity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) [1].
HIV-1protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie [1].
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent [1].
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS [1].
HIV-1 protease-IN-13 (compound 18d) is a potent HIV-1 protease inhibitor with an IC50 value of 0.54 nM. HIV-1 protease-IN-13 also shows potent activity against HIV-1DRVRS (DRV-resistant mutation) and HIV-1NL4_3 variant (wild type) [1].
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus [1].
HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor for HIV-1 integrase with an IC50 of 1.8 nM. HIV-1 integrase inhibitor 13 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 21 and 580 nM, respectively [1].
HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1,HIV-2 protease. And there are 4 residues for conservative substitutions of the substrate binding residues of HIV-1 and HIV-2 protease [1].
HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats [1].
HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1) [1].
HIV-1 TAT (48-60) is a cell-penetrating peptide derived from the human immunodeficient virus (HIV)-1 Tat protein residue 48-60. It has been used to deliver exogenous macromolecules into cells in a non-disruptive way.
18A (HIV-1 inhibitor 18A) is a reversible broad-spectrum HIV-1 inhibitor. 18A exhibits broad inhibitory activity against multiple HIV-1 strains by blocking the function of Env [1].
HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity [1].
HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
HIV-1 gag Protein p24 (194-210) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development [1].
Pol (476-484), HIV-1 RT Epitope is a biological active peptide. (This is a reverse transcriptase (RT) epitope (Pol residues 476-484). Within HIV-1 RT the peptide appears to be the dominant HLA A*0201-restricted epitope. Was used to investigate possible mechanisms behind HIV-1 escape from CTL. IV9 is the actual epitope processed and presented in HIV-1-infected cell lines.)
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
GSK3532795 hydrochloride is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively [1].
GSK3532795 oxalate is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively [1].
GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively [1].
L-697639 is an inhibitor for HIV-1 reverse transcriptase(HIV-1 RT) with IC50 of 20-400 nM (in a template-primer-dependent manner). L-697639 exhibits antiviral activity, that inhibits 95% HIV-1 infection at concentrations of 12-200 nM in human T lymphocyte cultures [1].
UMB-136 is a bromodomain inhibitor. UMB-136 is a promising latency-reversing agent (LRA) for HIV-1 eradication. UMB-136 reactivates HIV-1 in multiple cell models. UMB-136 enhances HIV-1 transcription and increases viral production through the release of P-TEFb [1].
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro[1] .
Talviraline is a non-nucleoside reverse transcriptase (NNRT) inhibitor that is primarily used to inhibit the replication of human immunodeficiency virus type 1 (HIV-1). Talviraline inhibits the viral replication process by binding to a specific site of HIV-1 reverse transcriptase (RT). Talviraline can be used to study the potential countermeasures and safety of HIV-1 infection [1].
SMAPP1 is an activator of protein phosphatase-1(PP1). SMAPP1 increases phosphorylation of CDK9’s Ser90 and Thr186 residues, but not Ser175. SMAPP1 induces HIV-1 replication, upregulates HIV-1 transcription that led to the reactivation of latent HIV-1 provirus [1].
Tivirapine (R86183) is a nonnucleoside HIV-1 RT inhibitor against HIV-1-induced cytopathic effects with an EC50 value of 4 nM. Tivirapine inhibits the Yl8lC mutant of HIV-1 RT[1].
L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture [1] .
NBD-14270, a pyridine analogue, is a potent HIV-1 entry antagonist with an IC50 of 180 nM against 50 HIV-1 Env-pseudotyped viruses. NBD-14270 binds to HIV-1 gp120 and shows potent antiviral activity. NBD-14270 shows low cytotoxicity (CC50>100 μM) [1] .
TMC310911 is a potent and orally active HIVtype-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity [1] .
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection [1].
Methyl salvionolate A is a potent inhibitor of HIV-1. Methyl salvionolate A inhibits P24 antigen in HIV-1 infected MT-4 cell with an EC50 of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with
IC50s of 50.58, 10.73 and 7.58 μg/ml, respectively [1].
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity [1] .
HI-253 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase that has demonstrated greater activity than multiple anti-HIV compounds against both resistant and sensitive HIV-1 strains.
Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
Sennoside A (Standard) is the analytical standard of Sennoside A. This product is intended for research and analytical applications. Sennoside A is an anthraquinone glycoside, found in Senna (Cassia angustifolia) [1]. Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication .
Fumagillin(NSC9168) is an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatu. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC50s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively. Islatravir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC50 values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV .
VIRIP (human α1-AT(353-372)) is a HIV-1 inhibitor. VIRIP blocks the entry of HIV-1 by interacting with gp41 fusion peptide. VIRIP can be used for virus research [1].
Reverse transcriptase-IN-3 is a pyrimidine-5-carboxamide derivative, acts as an inhibitor of HIV-1. Reverse transcriptase-IN-3 shows potent activity against the HIV-1 wild-type and mutant strains [1].
RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1[1].
CGP 53820 is an inhibitor for HIV protease, inhibits the complex of HIV-1 and HIV-2 protease with Ki of 9 and 53 nM for HIV-1 protease and HIV-2 protease. CGP 53820 can be used in AIDS research [1].
Fostemsavir sodium (BMS-663068 sodium) is an HIV-1 attachment inhibitor with antiviral activity against multidrug-resistant HIV-1. Co-inhibition with fostemsavir sodium also showed a trend toward reduction in markers of monocyte activation and coagulation abnormalities [1].
Sennoside A is an anthraquinone glycoside found in senna (Cassia angustifolia). Sennoside A is an HIV-1 inhibitor (IC50=3.8 μM) that inhibits HIV-1 replication. Sennoside A also inhibits HIV-1 reverse transcriptase (RT)-related DNA polymerase (RDDP) and ribonuclease H (Ribonuclease H) with IC50s of 1.9 μM and 5.3 μM, respectively [1] .
Integracin B is a potent dimeric alkyl aromatic inhibitor of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. Integracin B inhibits both coupled and strand transfer activity of HIV-1 integrase [1].
UK-88947 hydrochloride is a protease inhibitor with activity in inhibiting the replication of human immunodeficiency virus HIV-1. UK-88947 hydrochloride can be added to cells before infection to block the early steps of HIV-1 replication. The use of UK-88947 hydrochloride shows its specific inhibitory effect on HIV-1. At the same time, when the virus infects cells, it inhibits the action of viral protease and affects the virus replication process [1].
QYL-685 is a Z-methenylcyclopropane nucleoside analog containing 2,6-diaminopurine, which has strong antiviral activity against HIV-1. QYL-685 showed activity against Zidovudine (HY-17413) resistant and Didanosine (HY-B0249) resistant HIV-1 infected clones in vitro. QYL-685 can be developed as a therapeutic drug for HIV-1 infection [1].
ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs [1].
F9170 is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 is able to cross the blood-brain barrier (BBB) [1].
GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins.
AQ148 is a HIV-1 protease inhibitor (Ki=137 nM). The IC50 values ??of AQ148 for the inhibition of HIV-1, HIV-2 and SIV aspartic proteases are 1.5 μM, 3.4 μM and 5 μM, respectively [1].
Globotriaosylceramide porcine RBC is a trihexosylceramide (Gb3) in porcine erythrocytes. Globotriaosylceramide porcine RBC is a natural resistance factor against HIV-1 infection. The synthetase α-galactosyltransferase (A4GALT) of Globotriaosylceramide porcine RBC is associated with HIV-1 resistance.
U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with Ki of 20 nM, 560 nM and 2100 nM, respectively [1].
2,4-Dihydroxypyridine (compound 2) is a pyridine derivative which is active against both Topo IIKHIV activity and HIV-1 replication, with a pIC50 of 5.05 and 4.07 against Topo IIKHIV and HIV-1 replication, reespectively [1].
(Rac)-Efavirenz is the isomer of Efavirenz (HY-10572). Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase(HIV-1 RT) with IC50 of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC50 of 6.2-250 nM [1].
S-2720 is a potent inhibitor of both immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and HIV-1 replication. The binding sites of S-2720 and the nonnucleoside compounds overlap. The small pocket in the p66 subunit-BI-RG-587 (HY-10570) complex is most likely the target of S-2720. S-2720 is a quinoxaline derivative, which is promising for research of HIV-1 infection [1].
NBD-14189 is a potent HIV-1 entry antagonist with an IC50 of 89 nM against the HIV-1HXB2 pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC50<200 nM) [1] .
IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM [1].
Claficapavir (A1752) is a specific nucleocapsid protein (NC) inhibitor with an IC50 around 1 μM. Claficapavir strongly binds the HIV-1 NC (Kd=20 nM) thereby inhibiting the chaperone properties of NC and leading to good antiviral activity against the HIV-1[1].
Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells [1].
U-104489 is a HIV-1 inhibitor with the Ki values of 0.13, 0.12 and ＞ 100 μM aganist HIV-1 RT p66/p51 wild type (G190), G190A and G190E, respectively [1].
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection [1].
L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture [1] .
Amphotericin B methyl ester hydrochloride is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester hydrochloride is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester hydrochloride disrupts HIV-1 particle production and potently inhibits HIV-1 replication [1] .
Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) is a HIV-1 integrase (IN) and HIV-1 reverse transcriptase (RT) ribonuclease H (RNase H) inhibitor with an IC50 value of 6.32, 5.9 µM, respectively [1].
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs [1].
Amphotericin B methyl ester is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester disrupts HIV-1 particle production and potently inhibits HIV-1 replication [1] .
BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.
Sifuvirtide (SFT) acetate is a potent HIV fusion inhibitor. Sifuvirtide acetate inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide acetate can be used in the research of anti-HIV drugs [1].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
Efavirenz (Standard) is the analytical standard of Efavirenz. This product is intended for research and analytical applications. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
IMB-301 is a specific HIV-1 replication inhibitor that binds to hA3G (human APOBEC3G), interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. IMB-301 inhibits the replication of HIV-1 in H9 cells (IC50=8.63 uM). Human APOBEC3G is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication [1].
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme[1].
Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease. Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 can be used to test HIV-1 protease activity [1].
Thiamine disulfide (Standard) is the analytical standard of Thiamine disulfide. This product is intended for research and analytical applications. Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity [1] .
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd [1], Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope . Neuroprotective effects [1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells .
Fumagillin (Standard) is the analytical standard of Fumagillin. This product is intended for research and analytical applications. Fumagillin(NSC9168) is an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatu. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
H-Gly-Pro-Gly-NH2 is a tripeptide that inhibits HIV-1 replication. H-Gly-Pro-Gly-NH2 inhibits the activity of HIV-1 IIIB and HIV-2 ROD with EC50 values of 35 µM and 30 µM, respectively. H-Gly Pro Gly NH2 inhibits HIV-1 replication in vitro by interfering with capsid formation. H-Gly Pro Gly NH2 has antiviral activity and can be used for virus research [1] .
DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS [1].
JTK-101 is a selective HIV inhibitor. JTK-101 selectively reduces HIV-1 mRNA synthesis by inhibiting Tat cofactors, including CDK9 and cyclin T1, thereby suppressing the transcriptional activity of HIV-1. JTK-101 may be used in the field of anti-HIV virus research [1].
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
DMJ-I-228 is a CD4-mimetic. DMJ-I-228 binds to HIV-1 gp120 within the conserved Phe 43 cavity near the CD4-binding site, thereby blocking CD4 binding and inhibiting HIV-1 infection [1].
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 µM and an CC50 of >30 µM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup [1].
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 [1] . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1(HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates [1].
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS [1].
PL-100 is a potent HIV-1 protease inhibitor with a Ki of 36 pM and an EC50 of 16 nM. PL-100 inhibits viral replication by suppressing HIV-1 protease activity and demonstrates excellent antiviral efficacy against drug-resistant HIV strains. PL-100 can be used in research on drug-resistant HIV disease [1].
Lenacapavir (GS-6207) sodium is a HIV-1 capsid inhibitor. Lenacapavir sodium shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir sodium displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs) [1].
(Rac)-Efavirenz (Standard) is the analytical standard of (Rac)-Efavirenz. This product is intended for research and analytical applications. (Rac)-Efavirenz is the isomer of Efavirenz (HY-10572). Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics [1].
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) [1] .
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (compound 8) is an HIV-1 integrase inhibitor that effectively inhibits both the 3'-processing (3'-P) and strand transfer (ST) steps of the integration reaction. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide can be utilized in HIV-1 research [1].
BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) [1].
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis [1].
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) [1] .
BMS-663749 lysine is a prodrug of an HIV-1 attachment inhibitor with the potential to enhance the delivery of the parent compound following oral administration.
Trilobatin (Standard) is the analytical standard of Trilobatin. This product is intended for research and analytical applications. Trilobatin, a natural sweetener derived from?Lithocarpus polystachyus?Rehd [1], Trilobatin?is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope . Neuroprotective effects [1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells .
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
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 [1] . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively [1].
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) [1] .
Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication [1].
Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity [1].
MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection [1].
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). 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 [1] . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
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 [1] . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively [1] .
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities [1] . Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells . Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma .
Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432[1].
(S)-BMS-378806 ((S)-BMS-806) is an orally bioavailable HIV-1 inhibitor with activity against gp120-CD4 interactions. (S)-BMS-378806 exhibits micromolar inhibition of HIV-1 gp120-CD4 binding. The design and synthesis of (S)-BMS-378806 was based on a comprehensive study of protein-ligand interactions, which guided the identification and design of novel symmetrical N,N'-disubstituted aminoureas and thioureas. (S)-BMS-378806, synthesized in aqueous media using microwave irradiation, was validated for its inhibitory activity in HIV-1 gp120-CD4 capture ELISA [1].
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus
by targeting HIV-1 integrase or reverse transcriptase.
BM 21.1298 is a selective and high specific nonnucleoside immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) inhibitor with antiviral activity [1].
Tenofovir diphosphate (TFV-DP) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1(HIV-1)reverse transcriptase (RT) [1].
Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs [1].
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing [1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity [1].
EP39 is a potent HIV-1 maturation inhibitor. EP39 interacts with the SP1 domain of Gag. EP39 decreases the dynamics of CA-SP1 junction, by binding to the QVT motif of the SP1 domain, and perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure. EP39 acts by arresting maturation of HIV-1 thereby blocking its infectivity [1].
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs [1].
Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies [1] .
BMS 488043 (BMS 043) is an orally active and well-tolerated inhibitor of the attachment of human immunodeficiency virus type 1(HIV-1) to CD4+ lymphocytes [1].
BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains [1].
Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1(HIV-1)reverse transcriptase (RT) [1].
Benanomicin A is a microbial metabolite and can be isolated from Actinomycetes.Benanomicin has antifungal activitya and inhibits HIV-1 viral infection in MT-4 cells [1] .
Bictegravir (Standard) is the analytical standard of Bictegravir. This product is intended for research and analytical applications. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase (
IC50: 20 nM). The EC50, and CC50 of S 1360
in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants [1].
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 [1] . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
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 [1] . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
(Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. (Rac)-Efavirenz-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease [1] .
Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease [1] .
BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency [1] .
KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo [1].
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
Agrocybin is an antifungal peptide that exerts antifungal activity against several fungal species but lacks inhibitory activity against bacteria. Agrocybin attenuates the activity of HIV-1 reverse transcriptase[1].
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitory activity against HIV-1 protease, with IC50 >100 μg/mL [1].
Capsid assembly inhibitor is a 12-mer peptide that binds the capsid (CA) domain of Gag and inhibits assembly of immature- and mature-like HIV-1 capsid particles in vitro [1].
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively [1] . AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Nevirapine-d4 is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
TAT TFA (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins [1].
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent [1] .
Glycolithocholic acid 3-sulfate (disodium) inhibits replication of HIV-1in vitro. Glycolithocholic acid 3-sulfate (disodium) can be used for the research of HIV infection and gallbladder disease [1] .
HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor [1].
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. 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[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
Panobinostat (Standard) (LBH589 (Standard)) is the analytical standard of Panobinostat (HY-10224). This product is intended for research and analytical applications. Panobinostat is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities [1] . Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells . Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma .
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs) [1]. Lenacapavir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. Efavirenz-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors [1].
Ulonivirine (MK-8507) is an orally active non-nucleoside reverse transcriptase inhibitor with high antiviral activity. Ulonivirine can be used for the research of HIV-1 infection [1] .
Dolutegravir intermediate-1 is a synthetic intermediate of Dolutegravir extracted from patent WO 2016125192 A2. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.
Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent [1] .
Tenofovir diphosphate disodium is an antiretroviral agent and an inhibitor of DNA polymerases. Tenofovir diphosphate disodium is a substrate of HIV-1 reverse transcriptase (RT). Tenofovir diphosphate disodium can be used for the research of Aids [1].
TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins [1].
Formycin A (NSC 102811), a purine nucleoside antibiotic, is a potent human immunodeficiency virus type 1(HIV-1) inhibitor with an EC50 of 10 μM. Formycin A shows antitumor and antiviral activities [1] .
Ibalizumab (TMB-355) is a humanised IgG4 monoclonal antibody that prevents HIV cell entry by binding to CD4 receptor. Ibalizumab has the potential for HIV-1 infection research [1].
Palinavir is a potent human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) protease inhibitor with an IC50 of 0.5-30 nM . Palinavir has antiviral activity [1].
9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
Nevirapine (Standard) is the analytical standard of Nevirapine. This product is intended for research and analytical applications. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM [1].
Antiviral agent 9 reaches a single-digit picomolar EC50 value (0.006 nM) against HIV-1 and nearly 300-fold higher selectivity index (SI) compared to tenofovir alafenamide fumarate (TAF).
β-Rubromycin is a potent and selective inhibitor of human immunodeficiency virus-1 (HIV-1) RNA-directed DNA polymeras (reverse transcriptase). β-Rubromycin is a class of quinone antibacterials [1].
Delavirdine (Standard) is the analytical standard of Delavirdine. This product is intended for research and analytical applications. Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26?μM) over DNA polymerase?α?(IC50=440 μM) and polymerase?δ (IC50>550?μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs[1].
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) [1].
Bevirimat (Standard) is the analytical standard of Bevirimat. This product is intended for research and analytical applications. Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies[1][2][3][4].
Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing [1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) [1]. 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 3CL pro inhibitor with an IC50 of 14.2 μM .
Delavirdine (mesylate) (Standard) is the analytical standard of Delavirdine (mesylate). This product is intended for research and analytical applications. Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26?μM) over DNA polymerase?α?(IC50=440 μM) and polymerase?δ (IC50>550?μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs[1].
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-kD protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities [1] .
Obefazimod (ABX464) is a potent anti-HIV agent. Obefazimod inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.
Uncaric acid (6β,19α-Dihydroxyursolic acid) (compound 6) is a triterpene that can be found in Eriobotrya japonica. Uncaric acid shows anti HIV-1, HRV 1B, SNV activity [1].
Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria [1].
BILR 355 is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). BILR 355 is highly specific toward HIV-1 reverse transcriptase (RT). BILR 355 can be used for HIV infections research [1].
GSK-364735 is a potent antiretroviral agent against human immunodeficiency virus type 1 (HIV-1) and serves as an integrase inhibitor with an IC50 of 8 ± 2 nM. GSK-364735 can be utilized in antiviral research [1].
Mvt-101 is a hexapeptide-based inhibitor of HIV-1 protease. Mvt-101 is also reduced-peptide-bond inhibitor. Mvt-101 inhibits reproduction of the HIV virus by blocking protease action [1].
7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate, which can inhibit HIV-1 reverse transcriptase with a Ki of 25 nM [1].
Hinokinin (Standard) is the analytical standard of Hinokinin. This product is intended for research and analytical applications. Hinokinin (Compound 1) is a compound isolated from the stems of Hypoestes aristate. Hinokinin exhibits moderate activity of HIV-1 protease enzyme [1].
Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
GSK5750 is a specific and potent HIV-1 reverse transcriptase ribonuclease H inhibitor with an IC50 value of 0.33 μM. GSK5750 is bound at the RNase H active site through a metalion chelation mechanism [1].
Clavirolide L (Compound 3) is a dolabellane-type diterpenoid that can be isolated from Clavularia viridis. Clavirolide L shows significant inhibition against HIV-1 without RT enzyme inhibition and can be used for HIV infection research [1].
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle [1] . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS [1] .
[(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) is a selective inhibitor of HIV-1. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) inhibits viral infection and cell fusion by blocking the interaction between HIV-1 and CD4 molecules. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) can completely inhibit fusion formation at a concentration of 25 μM [1].
L-708906 is a potent human immunodeficiency virus type 1(HIV-1) inhibitor with an IC50 value of 12 μM. L-708906 inhibits HIV strains resistant to nonnucleoside or nucleoside reverse transcriptase inhibitors [1].
Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity [1].
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model [1] .
HIV gag peptide (197-205) is a H-2K d-restricted epitope derived from the p24 portion of the HIV-1 gag protein, consists of amino acids 197-205 (AMQMLKETI) [1].
(Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity [1].
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells [1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells .
Nevirapine-d5 (BI-RG 587-d5) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM [1].
A-77003 is an inhibitor for HIV protease, with IC50 of 0.1 to 0.2 μg/ml, for HIV-1 and HIV-2 protease. A-77003 exhibits high levels of antiretroviral activity and low cytotoxicity in vitro [1].
Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity [1].
Ingenol-3-palmitate, an ingenane diterpenoid, is a nature product that could be isolated from the roots of Euphorbia ebracteolata. Ingenol-3-palmitate is a potent HIV-1 (HIV) inhibitor with an IC50 value of 4.1 nM [1].
4-isocyanato TEMPO is a spin labeling reagent used to label the 2’-position in RNA. It has been used to study HIV-1 transactivation response RNA and hammerhead ribosome dynamics by electron paramagnetic resonance (EPR) spectroscopy.
(S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC50 of 28 nM, an EC50 of 450 nM and a Kd of 4.7 μM [1].
Nevirapine-d8 (BI-RG 587-d8) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM [1].
12-Oxocalanolide A (compound 6) is a potent inhibitor of reverse transcriptase from human immunodeficiency virus type 1 (HIV-1) with an IC50 and EC50 of 2.8 and 12 μM, respectively. 12-Oxocalanolide A is the analogue of Calanolide [1].
Vif-ElonginC interaction inhibitor 1 (compound VEC-5) is a potent Vif inhibitor. Vif-ElonginC interaction inhibitor 1 can restrict HIV-1 in Vif-nonpermissive cells. Vif-ElonginC interaction inhibitor 1 can protect A3G, APOBEC3C (A3C), and APOBEC3F (A3F) from Vif-mediated degradation and drastically inhibit Vif function through blocking the interaction between Vif and ElonginC. Vif-ElonginC interaction inhibitor 1 enhances A3G incorporation into HIV-1 virions to reduce viral infectivity [1].
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K [1]. Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Nevirapine-d3 (BI-RG 587-d3) is the deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
Hinnuliquinone is a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease. Hinnuliquinone is a bis-indolyl-2,5-dihydroxybenzoquinone pigment, that can be isolated from Nodulisphorium hinnuleum[1] .
Glycolithocholic acid 3-sulfate (SLCG) is a cholic acid derivative and a metabolite of glycolithocholic acid. Glycolithocholic acid 3-sulfate inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate can be used for the research of HIV infection and gallbladder disease [1] .
GSK-364735 potassium (S/GSK-364735 potassium) is the potassium salt form of GSK-364735 (HY-16907). GSK-364735 potassium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1(HIV-1) with an IC50 of 7.8 nM [1].
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits Raf/MEK/MAPK pathway [1].
TAT-CBD3, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization [1].
4-Nitrobenzofuroxan is an antiviral compound with HIV-1 inhibitory activity. 4-Nitrobenzofuroxan also exhibits an inhibitory effect on IDO1. The application potential of 4-Nitrobenzofuroxan lies in its ability to be used to inhibit viral infection [1].
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms [1].
GSK-364735 sodium (S/GSK-364735 sodium) is the sodium salt form of GSK-364735 (HY-16907). GSK-364735 sodium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1(HIV-1) with an IC50 of 7.8 nM [1].
Lucidenic lactone is a terpene compound, is a DNA polymerase inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively [1].
Lucidenic acid O is a terpene compound, is a DNA polymerases inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively [1].
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 [1].
Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl proagent of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
3β-Hydroxy-27-p-Z-coumaroyloxyurs-12-en-28-oic acid (compound 8) is a triterpenoid ester HIV-1 protease inhibitor with the potential for use in the antiretroviral combination therapy of AIDS [1].
BIT-225 is an inhibitor for Vpu protein through block of Vpu ion channel, and thus inhibits the release of HIV-1, especially in monocyte-derived macrophages (EC50 is 2.25 μM), without significant cytotoxicity (TC50 is 284 μM) [1].
Tenofovir alafenamide hemifumarate (Standard) is the analytical standard of Tenofovir alafenamide hemifumarate. This product is intended for research and analytical applications. Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Fosalvudine tidoxil is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Fosalvudine tidoxil is a prodrug derived from Alovudine (HY-B1516). Fosalvudine tidoxil is less toxic than Alovudine and can be used for the research of HIV-1 infection [1].
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV [1] .
Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 μM. Lavendustin B is also a weak inhibitor of tyrosine kinases[1] .
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor [1].
Indoline is a derivative of Indole (HY-W001132). Indoline can used as the basic structure for CD4 mimetic compounds (CD4mcs), which triggers conformational changes of the HIV-1 envelope glycoprotein (Env) in advance, and causes viral inactivation [1]
VIR-165 is a modified form of virus inhibitory peptide (VIRIP) that binds the fusion peptide of the gp41 subunit and prevents its insertion into the target membrane. VIRIP inhibits a wide variety of human immunodeficiency virus type 1 (HIV-1) strains [1].
IN-RNA-IN-2 (compound 1a) is an inhibitor (IC50=70 nM) of the interaction between HIV-1 integrase and the viral RNA genome. IN-RNA-IN-2 exerts its anti-HIV activity by inhibiting the viral replication process [1].
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B [1] .
ssRNA40 (sodium) is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. ssRNA40 is a uridine-rich ssRNA derived from the HIV-1 long terminal repeat on activation of NK cells via TLR7/8[1][2].
(S)-Batylalcohol (1-O-Octadecyl-sn-glycerol) is a phosphonoformic acid (PFA) analog that exhibits higher in vitro antiviral activity against human immunodeficiency virus type 1(HIV-1) than PFA. (S)-Batylalcohol can be used in antiretroviral research [1].
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives [1] .
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1(HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection [1].
RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates [1].
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) [1] .
EFdA-TP tetralithium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetralithium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetralithium inhibits HIV-1 RT with multiple mechanisms [1].
Nelfinavir (Standard) is the analytical standard of Nelfinavir. This product is intended for research and analytical applications. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent [1] .
Darunavir (Ethanolate) (Standard) is the analytical standard of Darunavir (Ethanolate). This product is intended for research and analytical applications. Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
Nelfinavir-d4 is deuterated labeled Nelfinavir (HY-15287). Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent [1] .
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1] .
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine is a polyunsaturated phospholipid that is a constituent of lipid monolayers and small unilamellar vesicles. 1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine can be used to prepare endoplasmic reticulum-targeted liposomes (PERLs) in a molar ratio of 1.5:1.5:1:1 with 1,2-didocosahexaenoyl-sn-glycero-3-phosphoethanolamine, l-α-phosphatidylinositol, and l-α-phosphatidylserine. PERLs can reduce cholesterol levels in human peripheral blood mononuclear cells (PBMCs) and reduce HIV-1 particle secretion from HIV-1 infected PBMCs [1].
Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively [1].
GS-9148 is a ribose-modified HIV-1 nucleotide reverse transcriptase (RT) inhibitor with an EC50 value of 10.6 µM. GS-9148 shows antiretroviral activity for K65R, L74V, or M184V RT mutation [1].
MPG, HIV related is 27-aa peptide, derived from both the nuclear localisation sequence of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41 and is a potent delivery agent for the generalised delivery of nucleic acids and of oligonucleotides into cultured cells.
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations [1] .
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models [1].
Erythromycin Ethylsuccinate (Standard) is the analytical standard of Erythromycin Ethylsuccinate. This product is intended for research and analytical applications. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM [1] .
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research [1].
Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties [1].
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer [1].
Limonin (Standard) is the analytical standard of Limonin. This product is intended for research and analytical applications. Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities [1] .
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function [1].
c-PB2(OH)2 is a 4-carboxyphenyl / 4-hydroxyphenyl meso-substituted porphyrin compound. c-PB2(OH)2 shows anti HIV-1 activity under non-photodynamic and photodynamic conditions [1].
NBD-556, a CD4 mimetic, is a potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction. NBD-556 shows potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels [1] .
PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction [1].
Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a substrato peptídico of HIV-1 protease. Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 acts as the variable substrate in a peptidolytic assay to quantify the inhibition of the protease [1] .
Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1[1].
Scirpusin A is a naturally occurring compound extracted from the legume plant Caragana rosea Turcz, exhibiting anti-HIV activity. Scirpusin A demonstrates significant inhibitory effects against HIV-1 (EC50=7 μg/mL). Scirpusin A is utilized in research towards the development of anti-HIV therapeutics [1].
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity [1] .
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Gardiquimod (Standard) is the analytical standard of Gardiquimod. This product is intended for research and analytical applications. Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
Fostemsavir (Standard) is the analytical standard of Fostemsavir. This product is intended for research and analytical applications. Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) [1]. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
UC-781 (NSC 675186) is a highly potent and selective nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an IC50 value of 5 nM. UC-781 is stable under low PH or various temperatures conditions. UC-781 has antiviral activity and resistance [1] .
HIV capsid modulator 1(compound 21a2) is a potent HIV capsid modulator. HIV capsid modulator 1 is a quinazolin-4-one-bearing phenylalanine derivative. HIV capsid modulator 1 has antiviral activities against both HIV-1 and HIV-2 [1].
Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression [1] .
Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4 [1] .
Inophyllum B ((+)-Inophyllum B) is a potent HIVReverse Transcriptase inhibitor with an IC50 value of 38 nM. Inophyllum B inhibits HIV-1(IC50=1.4 μM) in vitro cell culture. Inophyllum B can be isolated from the acetone extract of the giant African snail, Achatina fulica[1].
Teicoplanin is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity [1] .
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1IC50 in vitro for ERK2 is 29 μM [1] .
Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1(RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects [1] .
2F5 epitope, a peptide gp41 (659-671), comprises the entire epitope for one of the three known antibodies capable of neutralizing a broad spectrum of primary HIV-1 isolates and is the only such epitope that is sequential. 2F5 epitope is recognized by broadly neutralizing antibodies 2F5 [1] .
Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity [1] .
Teicoplanin sodium is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity [1] .
mC46 (C46) peptide is a membrane-associated fusion peptide inhibitor. mC46 peptide potently inhibits HIV-1 replication and entry. mC46 also inhibits CCR5-tropic, CXCR4-tropic, and dual-tropic HIVs, SIV, and SHIV [1].
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
9-Propenyladenine (Standard) is the analytical standard of 9-Propenyladenine. This product is intended for research and analytical applications. 9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
9-Aminoacridine (Standard) is the analytical standard of 9-Aminoacridine. This product is intended for research and analytical applications. 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for the research of tumour, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza [1].
RPR103611, the betulinic acid derivative, is a potent HIV-1 entry inhibitor with IC50s of 80, 0.27, and 0.17 for CCR5-tropic virus YU2, CXCR4-tropic virus NL4-3 and dual tropic virus 89.6, respectively [1].
Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina?L. Rosamultin has inhibitory effects against HIV-1 protease[1]. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects .
R-82150 (TIBO-R 82150) is an HIV-1 reverse transcriptase inhibitor that blocks the reverse transcription of viral RNA by binding to the non-substrate binding site of reverse transcriptase, thereby inhibiting viral replication. R-82150 does not inhibit the replication of HIV-2, other RNA viruses, and DNA viruses [1].
Des(benzylpyridyl) Atazanavir (compound M1) is a N-dealkylation product of Atazanavir (HY-17367) metabolite. Atazanavir is a highly selective HIV-1 protease inhibitor. Des(benzylpyridyl) Atazanavir may contribute to the effectiveness Atazanavir but also to the toxicity and interactions. Des(benzylpyridyl) Atazanavir can be used for further research of Atazanavir effects [1].
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties [1].
BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 μM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity [1].
Fostemsavir-d8 (BMS-663068-d8) is deuterium labeled Fostemsavir. Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
PF-46396 is a potent HIV-1 inhibitor with an EC50 value of 0.206 µM. PF-46396 shows antiviral activity. PF-46396 inhibits the processing of capsid (CA)/spacer peptide 1 (SP1) (p25) Gag precursor proteins and blocks maturation of the viral core particle [1].
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 3CL pro inhibitor [1] .
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM [1].
gp120-IN-2 (compound 4i) is a potent HIV-1 gp120 inhibitor with an IC50 of 7.5 µM and CC50 of 112.93 µM. gp120-IN-2 shows anti-HIV-1 activity. gp120-IN-2 shows cytotoxicity in a dose dependent manner in SUP-T1 cells [1].
Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity [1] .
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 3CL pro inhibitor [1] .
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis [1] .
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine [1].
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G [1] .
Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis [1] .
HIV-IN-5 (compound 5r) is a potent HIV-1 inhibitor, with an IC50 of 0.16 μM. HIV-IN-5 shows inhibition of HIV DNA-dependent DNA polymerization activity, with an IC50 of 2.18 μM. HIV-IN-5 can bind to NNIBP (NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding pocket) [1].
Gardiquimod (diTFA) (Standard) is the analytical standard of Gardiquimod (diTFA). This product is intended for research and analytical applications. Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
ODN 6016 sodium is a CpG-A oligonucleotides. ODN 6016 sodium can induce IFN-α production, and can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G [1] .
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM [1].
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
BMS-818251 is a potent, small-molecule inhibitor of HIV-1 entry with an EC50 value of 0.019 nM. BMS-818251 shows >10-fold higher potency than BMS-626529 (HY-15440) on a cross-clade panel of 208-HIV-1 strains. BMS-818251 interacts with gp120 residues from the conserved β20-β21 hairpin to improve potency [1].
Ganoderic acid B (Standard) is the analytical standard of Ganoderic acid B. This product is intended for research and analytical applications. Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) [1] .
Retrocyclin-1 is a kind of Theta-defensin. Retrocyclin-1 recognizes and binds to carbohydrate-containing surface molecules, to protect cells from HIV-1 infection. Retrocyclin-1 exhibits high affinity to fetuin, gp120 (Kd=35.4 nM), CD4 (Kd=31 nM), and galactosylceramide (Kd=24.1 nM) [1].
DSPE-PEG2000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
DSPE-PEG1000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
HIV capsid modulator 2 (Compound 7t) is a modulator for the HIV capsid (CA) protein. HIV capsid modulator 2 exhibits antiviral activity, which inhibits HIV-1 IIIB strain and HIV-2 ROD strain with EC50 of 0.04 and 0.13 μM. HIV capsid modulator 2 is metabolically stable in human liver microsomes [1].
16,16-Dimethyl prostaglandin A1 (di-Me-PGA1) is a prostaglandin analog that can inhibit DNA synthesis in Lewis lung carcinoma and B 16 amelanotic melanoma cells. 16,16-Dimethyl prostaglandin A1 also inhibits viral replication in both HSV and HIV-1 infection systems [1] .
R82913 (9-Cl-TIBO) is a potent and high selective inhibitor of HIV-1 reverse transcriptase with antiviral activity on both an RNA template (negative strand synthesis) and a DNA template (positive strand synthesis). R82913 inhibits the replication of different strains of HIV-I in CEM cells with a median IC50 value of of 0.15 μM [1] .
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc [1] .
Rp-dGTPαS is the nucleotide substrate of SAMHD1 and is one of the enantiomers of the dNTPαS nucleotide. SAMHD1 is an essential regulator of cellular dNTPs that limits virus (HIV-1, etc.) replication in the CD4+ myeloid lineage and resting T cells. The SAMHD1 tetrameric complex catalyzes the hydrolysis of Rp-dGTPαS into 2'-deoxynucleosides and triphosphates [1].
NSC727447 is an inhibitor of ribonuclease H (Rnase H) of HIV-1 and HIV-2. NSC727447 has little activity against E. coli RNase H, but great selectivity over human Rnase H, with IC50s value of 2.0 μM, 2.5 μM, 100 μM, 10.6 μM, respectively [1].
Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM [1] .
Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
DSPE-PEG5000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
GS-9770 is an orally active inhibitor for HIV protease with Ki of 0.16 nM. GS-9770 exhibits antiviral activity aginst HIV-1 strains and HIV-2 strains with EC50 of 1.9-26 nM, and 26 nM. GS-9770 is metabolic stable in human liver microsomes. GS-9770 exhibits good pharmacokinetic characters in Sprague Dawley rats [1].
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability [1].
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect [1] .
Nevirapine quinone methide is an active metabolite of Nevirapine, serving as a non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infection and AIDS. Nevirapine quinone methide is associated with severe skin and liver injuries due to its metabolic activation pathways. Nevirapine quinone methide has been shown to inhibit CYP3A4, which could contribute to its hepatic toxicity.
I-XW-053 is an inhibitor of HIV-1 capsid protein that can suppress the replication of HIV-189BZ167 with an IC50 value of 164.2 μM. I-XW-053 exhibits antiviral activity and can block the interface between capsid protein (CA) N-terminal domains (NTD-NTD interface) with micromolar affinity [1].
I-XW-053 is an inhibitor of HIV-1 capsid protein that can suppress the replication of HIV-189BZ167 with an IC50 value of 164.2 μM. I-XW-053 exhibits antiviral activity and can block the interface between capsid protein (CA) N-terminal domains (NTD-NTD interface) with micromolar affinity [1].
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 3CL pro inhibitor [1] .
CE-2072 is an inhibitor of serine proteases neutrophil elastase and proteinase-3. CE-2072 inhibits HIV-1 production and p24 production in response to IL-18 or NaCl in infected U1 monocytic cells, reduces virus replication in infected peripheral blood mononuclear cells and blocks infection of permissive HeLa cells. CE-2072 suppresses activation of the HIV-1-inducing transcription factor NF-kB in U1 cells. CE-2072 is promising for research of HIV-1-related disease [1].
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome [1].
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys [1].
Vicriviroc (SCH 417690) is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer [1] .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure [1] .
FGI-106 is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively [1].
VRC-01 is a fully human IgG1 antibody that targets envelope glycoprotein gp120 Protein. VRC-01 blocks viral entry by partially mimicking the interaction of the CD4 receptor with HIV-1 gp120 envelope glycoprotein. The isotype control for VRC-01 can refer to Human IgG1 kappa, Isotype Control (HY-P99001) [1].
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1[1].
Dapivirine-d4 (TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations [1] .
GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Mavorixafor can be used for the study of WHIM syndrome [1].
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 nM and 9 nM, respectively. Mavorixafor hydrochloride can be used for the study of WHIM syndrome [1].
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively [1].
Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively [1] . Censavudine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Vicriviroc (SCH 417690) malate is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc malate can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer [1] .
Escin IA (Standard) is the analytical standard of Escin IA. This product is intended for research and analytical applications. Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression [1] .
RJS308 is the PROTAC degrader for cyclosporin A (CypA) with a DC50 of 284 nM. RJS308 exhibits antiviral activcity through inhibition of HIV-1 and HCV replication [1]. (Pink: ligand for target protein CypA ligand-2 (HY-173012); Black: linker (HY-W123015); Blue: ligand for E3 ligase VHL (S,R,S)-AHPC-Me (HY-112078))
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis[1][2][3][4].
TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe [1].
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
Astodrimer (SPL7013 free base) is a large (3-4 nm,?~?16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
Stavudine (Standard) is the analytical standard of Stavudine. This product is intended for research and analytical applications. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis [1] .
(Rac)-Telinavir ((Rac)-SC-52151) is a racemate of Telinavir (HY-106395A). Telinavir (SC-52151) is a potent and selective HIV protease inhibitor. Telinavir inhibits lymphotropic, monocytotropic strains and field isolates of HIV type 1 (HIV-1), HIV-2, and simian immunodeficiency virus with EC50s of 26 ng/mL (43 nM). Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes [1].
FGI-106 tetrahydrochloride is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 tetrahydrochloride is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively [1].
gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an IC50 of 2.2 µM and CC50 of 100.90 µM. gp120-IN-1 shows anti-HIV-1 activity. gp120-IN-1 shows cytotoxicity in a dose dependent manner in SUP-T1 cells. gp120-IN-1 shows inhibition of gp120-mediated virus enter into cells [1].
Cyclotriazadisulfonamide (CADA) hydrochloride is a specific CD4-targeted HIV entry inhibitor with activity against HIV-1 replication. Cyclotriazadisulfonamide hydrochloride can specifically downregulate the expression of CD4 receptors on the cell surface, effectively inhibiting HIV transmission. Cyclotriazadisulfonamide hydrochloride can inhibit HIV-1(NL4.3) and SIV(mac251), and has a synergistic effect when used in combination with cellulose acetate (CAP). Cyclotriazadisulfonamide hydrochloride can also be used as a microbial gel formulation to maintain CD4 downregulation and antiviral activity, and is a broad-spectrum anti-HIV agent.
Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Tat-HA-NR2B9 contains a fragment of the cellmembrane transduction domain of HIV-1 Tat, a influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c). Tat-HA-NR2B9 reduces infarct size and improves neurological functions in ischemia-induced cerebral injury in the rats [1]
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively [1].
12-Hydroxynevirapine (12-hydroxy-NVP; 12-OH-NVP) is a major oxidative metabolite of Nevirapine (HY-10570). Nevirapine is a non-nucleoside reverse transcriptase inhibitor indicated for the HIV-1 infections. Nevirapine causes idiosyncratic hepatotoxicity and mild-to-severe skin rashes. 12-Hydroxynevirapine, a non-reactive metabolite, can be bioactivated by sulphotransferases (SULTs) in the liver and skin, yielding the reactive species 12-Sulphoxy-nevirapine [1] .
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity [1] .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms [1]. EFdA-TP (tetraammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1 RT with multiple mechanisms [1]. EFdA-TP (tetrasodium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration [1]. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of
3.49 μM .
Asterriquinone (ARQ), a Asterriquinone analog, is a Grb-2 binding inhibitor. Asterriquinone inhibits the Grb-2 binding activity to tyrosine phosphorylated EGFR, with an IC50 of 8.37 μM. Asterriquinone is a HIV1 reverse transcriptase inhibitor with a Ki of 2.3 μM. Asterriquinone also inhibits Grb-7 and PLC-γ binding activities. [1] .
HIV gp120 (318-327) is a short sequence of the HIV-1 strain IIIB envelope peptide (rgpgrafvti) that corresponds to the conserved C-terminal region of the glycoprotein. HIV gp120 (318-327) is part of the HIV vaccine V3 peptide epitope, also known as the I10 peptide. However, HIV gp120 (318-327) lacks the A2 anchor residues recognized by epitope-specific CTLs but has structural features that confer promiscuous A2 binding [1] .
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ [1] .
Dextran sulfate sodium salt (DSS) (MW 450000-550000) is a polymer of dehydrated glucose with a molecular weight of approximately 450000-550000. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 450000-550000) inhibits replication of HIV-1 and influenza A virus. Dextran sulfate sodium salt (MW 450000-550000) can be formulated as nanoparticles and shows antibacterial activity. Dextran sulfate sodium salt (MW 450000-550000) can be used for functional material preparation [1] .
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env [1] .
Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker [1] . Ebselen potently inhibits M pro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM) .Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1[1] .
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1[1] .
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity [1].
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ [1] .
TX-1918 is an inhibitor for eukaryotic elongation factor 2 kinase (eEF2-K) and Src kinase with IC50 of 0.44 and 4.4 μM, respectively. TX-1918 exhibits cytotoxicity in cell HepG2 and HCT116, with IC50 of 2.07 and 230 μM, respectively. TX-1918 inhibits the C-terminal domain of HIV-1 CA (CA CTD)(IC50 =3.81 μM), and inhibits the viral replication (IC50 =15.16 μM) [1] .
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
N.41 is an antiviral agent. N.41 protects APOBEC3G (an antiviral factor) from HIV Vif protein-mediated degradation. N.41 inhibits the Vif-A3G interaction and increases cellular A3G levels and incorporation of A3G into virions, thereby attenuating virus infectivity in a Vif-dependent manner. N.41 inhibits HIV-1 viral replication in PBMCs (IC50: 8.4 μM) [1].
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 3CL pro inhibitor [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively [1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection [2].
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation [1] . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects [1] .
Diphyllin is an orally active V-ATPase inhibitor (IC50=17 nM) and HIV-1 inhibitor (IC50=0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC50=0.6 nM for acid influx inhibition)， thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption [1] .
Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively [1] .
AMD 3329 octahydrobromide is a potent and selective anti-HIV-1 and HIV-2 compound with activity to inhibit viral replication. AMD 3329 blocks viral invasion by binding to the chemokine receptor CXCR4. AMD 3329 exhibits EC50 values as low as 0.8 and 1.6 nM when inhibiting HIV-1 and HIV-2 replication, showing better antiviral efficacy than AMD3100. AMD 3329 significantly inhibits the binding of specific CXCR4 monoclonal antibodies and the Ca(2+) flux induced by SDF-1alpha. AMD 3329 is also able to effectively interfere with virus-induced syncytium formation, with an EC50 value of 12 nM [1].
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment [1].
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
5M038 is an inhibitor of HIV envelope-mediated fusion with potent inhibitory activity against gp41-mediated membrane fusion. 5M038 prevents the formation of the gp41 post-fusion conformation and inhibits envelope-mediated membrane fusion in cell-cell fusion and viral infectivity assays. 5M038 has shown broad fusion inhibition in tests against multiple HIV-1 subtypes, including M and T strains. 5M038 targets a highly conserved hydrophobic pocket and binds to the gp41 trimer, thereby exerting its inhibitory effect [1].
(Cys47)-HIV-1 tat Protein (47-57) has membrane translocation function and can be used to derivatize the surface of magnetic pharmaceuticals and substantially facilitated their uptake into target cells [1] .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Dextran sulfate sodium salt (DSS) (MW 5000) is a polymer of dehydrated glucose with a molecular weight of approximately 5000. Dextran sulfate sodium salt (DSS) with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 5000) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 5000) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (DSS) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 5000) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 5000) inhibits instant blood-mediated inflammatory reaction (IBMIR) [1] .
RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 [1] .
α-Lipoic Acid (sodium) (Standard) is the analytical standard of α-Lipoic Acid (sodium). This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4]. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1[5].
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1(BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [1] . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Dextran sulfate sodium salt (DSS) (MW 4500-5500) is a polymer of dehydrated glucose with a molecular weight of approximately 4500-5500. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 4500-5500) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 4500-5500) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (MW 4500-5500) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 4500-5500) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) inhibits instant blood-mediated inflammatory reaction (IBMIR) [1] .
Dextran sulfate sodium salt (DSS) (MW 6500-10000) is a polymer of dehydrated glucose with a molecular weight of approximately 5000. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 6500-10000) has antiviral activity against HIV-1 and HIV-2. Dextran sulfate sodium salt (MW 6500-10000) blocks the binding of virions to CD4 ⁺ T lymphocytes and inhibits syncytia formation. Dextran sulfate sodium salt (MW 6500-10000) also prevents experimental urolithiasis due to its cytoprotective actions. Moreover, because of its biocompatible and highly charged properties, Dextran sulfate sodium salt (MW 6500-10000) is a suitable choice for pharmaceutical systems[1] .
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains [1]. Azvudine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains [1]. Azvudine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Theaflavin 3,3'-digallate (Standard) is the analytical standard of Theaflavin 3,3'-digallate. This product is intended for research and analytical applications. Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research [1] .
DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets [1].
RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 [1][2] .
Ivermectin (Standard) is the analytical standard of Ivermectin. This product is intended for research and analytical applications. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1(BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [1] . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells [1]. 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity [1]. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection . Azt-pmap is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN,HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection [1] .
Scutellarin (Standard) is the analytical standard of Scutellarin. This product is intended for research and analytical applications. Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
L 696229 is a specific inhibitor ofhuman immunodeficiency virus type 1(HIV-1)reverse transcriptase (RT) activity that possesses antiviral activity [1].
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
Palicourein is a 37 amino acid cyclic polypeptide. Palicourein inhibits the in vitro cytopathic effects of HIV-1RF infection of CEM-SS cells with an EC50 value of 0.1 μM and an IC50 value of 1.5 μM [1].
Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
4-Deoxy-4α-phorbol is a tetracyclic diterpene found in E. desmondi. It has been used in the semisynthesis of inhibitors of the HIV-1-induced cytopathic effect on MT-4 cells and 4α-phorbol esters [1].
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Elvitegravir (Standard) is the analytical standard of Elvitegravir. This product is intended for research and analytical applications. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Wikstrol A is a potent antifungal, antimitotic and anti-HIV-1 Agent. Wikstrol A induces morphological deformation of P. oryzae mycelia with an MMDC value of 70.1 µM. Wikstrol A shows activity against microtubule polymerization with an IC50 value of 131 µM. Wikstrol A shows anti-HIV-1 activity with an IC50 value of 67.8 µM [1].
DENV-IN-5 (Compound 4b) is a dengue virus (DENV) inhibitor with EC50s of 1.47, 9.23, 7.08 and 8.91 μM against DENV-I ∼ IV replication, respectively. DENV-IN-5 also inhibits HIV-1IIIB strain with an EC50 of 0.1512 μM [1].
Carbovir triphosphate (CBV-TP) is a phosphorylated metabolite. Carbovir triphosphate can be used for the research of human immunodeficiency virus (HIV) .
Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful agent against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent [1].
Elvitegravir- 13C6 (GS-9137- 13C6) is 13C labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
NRTT-IN-1 (Compound 1) is inhibitor for nucleoside reverse transcriptase translocation (NRTT), that inhibits the DNA synthesis and viral replication of HIV .
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively [1].
Schineolignin C is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities [1].
Schineolignin B is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities [1].
Etravirine-d8 is the deuterium labeled Etravirine. Etravirine (R165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV[1][2].
Kadsuracoccinic acid A is a tetracyclic natural compound that can be isolated from the stems of Kadsura coccinea. Kadsuracoccinic acid A has vitro anti-HIV-1 activitiy with an EC50 value of 68.7 μM [1].
20(21)-Dehydrolucidenic acid A is a triterpenoid isolated from the fruiting body of the fungus Ganoderma sinense. 20(21)-Dehydrolucidenic acid A has weak anti-HIV-1 protease activity [1].
Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells [1].
Lamellarin E is a biologically active marine alkaloid, while the Lamellarin series of alkaloids show potential cytotoxicity, topoisomerase I inhibition, protein kinase inhibition, multidrug resistance reversal, and anti-HIV-1 activity [1].
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV .
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities [1].
5-Dexyexcoecafolin B is a tigliane-type diterpenoid isolated from the EtOAc extract of Excoecaria acerifolia Didr. 5-Dexyexcoecafolin B has anti-HIV-1 activity with a EC50 value of 0.036 μM [1].
Docosyl trans-ferulate (compound 2) is an antiviral compound. Docosyl trans-ferulate exhibits anti-HIV-1 activity in anti-syncytial assays using the ΔTat/revMC99 virus and 1A2 cell line systems [1].
Isoescin IA (Standard) is the analytical standard of Isoescin IA. This product is intended for research and analytical applications. Isoescin IA is a triterpenoid saponin isolated from the seeds of Aesculus chinensis. Isoescin IA has anti-HIV-1 protease activity [1].
AMD-3329 is a potent and selective anti-HIV-1 and HIV-2 agent, exhibiting activity by inhibiting virus replication through binding to the chemokine receptor CXCR4, which serves as a co-receptor for the entry of X4 viruses.
Tizoxanide-d4 is the deuterium labeled Tizoxanide. Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities[1][2].
R-87366 is a water-soluble human immunodeficiency virus (HIV) protease inhibitor. R-87366 has potent inhibitory for HIV protease with a Ki value of 11 nM. R-87366 can be used for the research of anti-human immunodeficiency virus (HIV) .
Didanosine (Standard) is the analytical standard of Didanosine. This product is intended for research and analytical applications. Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
Rovafovir etalafenamide (GS-9131), a proagent of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity [1] .
Periglaucine A, a hasubanane-type alkaloid, can be isolated from Pericampylus glaucus. Periglaucine A can inhibits HBV surface antigen (HBsAg) secretion in Hep G2.2.15 cells. Periglaucine A also shows anti-HIV-1 activity in C8166 cells (EC50: 204 μM) [1].
Acetohydroxamic acid is the inhibitor for bacterial and plant urease that can be used for chronic urinary tract infections. Acetohydroxamic acid selectively inhibits arachidonic acid 5-lipoxygenase that is useful in the research of asthma. Acetohydroxamic acid inhibits the formation of advanced glycation end products, and reduces oxidative stress and inflammatory responses. Acetohydroxamic acid exhibits antiviral activity against HIV .
Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum[1].Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM .
DENV-IN-6 is a potent DENV (I-IV) inhibitor with EC50s of 17.5, 13.20, 6.8 and 11.41 μM for the inhibition of DENV (I-IV) replication, respectively. DENV-IN-6 also exhibits activity of anti-HIV-1IIIB (EC50=0.0181 µM; CC50=64.92 µM) [1].
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM [1].13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis .
Nipamovir is a nitroimidazole prodrug. Nipamovir shows comparable antiviral activity to SAMT-247 (HY-102077) and NS-1040 in both cellular assays and a human ex vivo model of HIV infection, along with low toxicity. Nipamovir has EC50 values of 3.64±3.28 and 3.23±2.81 μM for CEM-SS/HIV-1RF and hPBMC/HIV-192HT599, respectively [1].
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties [1] .
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
Rilpivirine (Standard) is the analytical standard of Rilpivirine. This product is intended for research and analytical applications. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
Rilpivirine- 13C6 (R278474- 13C6) is 13C labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity [1]. 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity [1].
Zingibroside R1 possesses some anti-HIV-1 activity.
Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM) .
Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells [1] .
GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) [1].
Tizoxanide (Standard) is the analytical standard of Tizoxanide. This product is intended for research and analytical applications. Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells [1] .
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
9-Aminoacridine (Standard) is the analytical standard of 9-Aminoacridine. This product is intended for research and analytical applications. 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
Indoline is a derivative of Indole (HY-W001132). Indoline can used as the basic structure for CD4 mimetic compounds (CD4mcs), which triggers conformational changes of the HIV-1 envelope glycoprotein (Env) in advance, and causes viral inactivation [1]
1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine is a polyunsaturated phospholipid that is a constituent of lipid monolayers and small unilamellar vesicles. 1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine can be used to prepare endoplasmic reticulum-targeted liposomes (PERLs) in a molar ratio of 1.5:1.5:1:1 with 1,2-didocosahexaenoyl-sn-glycero-3-phosphoethanolamine, l-α-phosphatidylinositol, and l-α-phosphatidylserine. PERLs can reduce cholesterol levels in human peripheral blood mononuclear cells (PBMCs) and reduce HIV-1 particle secretion from HIV-1 infected PBMCs [1].
Dextran sulfate sodium salt (DSS) (MW 5000) is a polymer of dehydrated glucose with a molecular weight of approximately 5000. Dextran sulfate sodium salt (DSS) with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 5000) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 5000) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (DSS) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 5000) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 5000) inhibits instant blood-mediated inflammatory reaction (IBMIR) [1] .
DSPE-PEG2000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
DSPE-PEG1000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
DSPE-PEG5000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway [1].
Dextran sulfate sodium salt (DSS) (MW 6500-10000) is a polymer of dehydrated glucose with a molecular weight of approximately 5000. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 6500-10000) has antiviral activity against HIV-1 and HIV-2. Dextran sulfate sodium salt (MW 6500-10000) blocks the binding of virions to CD4 ⁺ T lymphocytes and inhibits syncytia formation. Dextran sulfate sodium salt (MW 6500-10000) also prevents experimental urolithiasis due to its cytoprotective actions. Moreover, because of its biocompatible and highly charged properties, Dextran sulfate sodium salt (MW 6500-10000) is a suitable choice for pharmaceutical systems[1] .
HIV-1 TAT (48-60) is a cell-penetrating peptide derived from the human immunodeficient virus (HIV)-1 Tat protein residue 48-60. It has been used to deliver exogenous macromolecules into cells in a non-disruptive way.
HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1,HIV-2 protease. And there are 4 residues for conservative substitutions of the substrate binding residues of HIV-1 and HIV-2 protease [1].
HIV-1 gag Protein p24 (194-210) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development [1].
Pol (476-484), HIV-1 RT Epitope is a biological active peptide. (This is a reverse transcriptase (RT) epitope (Pol residues 476-484). Within HIV-1 RT the peptide appears to be the dominant HLA A*0201-restricted epitope. Was used to investigate possible mechanisms behind HIV-1 escape from CTL. IV9 is the actual epitope processed and presented in HIV-1-infected cell lines.)
VIRIP (human α1-AT(353-372)) is a HIV-1 inhibitor. VIRIP blocks the entry of HIV-1 by interacting with gp41 fusion peptide. VIRIP can be used for virus research [1].
F9170 is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 is able to cross the blood-brain barrier (BBB) [1].
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs [1].
Sifuvirtide (SFT) acetate is a potent HIV fusion inhibitor. Sifuvirtide acetate inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide acetate can be used in the research of anti-HIV drugs [1].
Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease. Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 can be used to test HIV-1 protease activity [1].
H-Gly-Pro-Gly-NH2 is a tripeptide that inhibits HIV-1 replication. H-Gly-Pro-Gly-NH2 inhibits the activity of HIV-1 IIIB and HIV-2 ROD with EC50 values of 35 µM and 30 µM, respectively. H-Gly Pro Gly NH2 inhibits HIV-1 replication in vitro by interfering with capsid formation. H-Gly Pro Gly NH2 has antiviral activity and can be used for virus research [1] .
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
Capsid assembly inhibitor is a 12-mer peptide that binds the capsid (CA) domain of Gag and inhibits assembly of immature- and mature-like HIV-1 capsid particles in vitro [1].
TAT TFA (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins [1].
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors [1].
TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins [1].
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-kD protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
Mvt-101 is a hexapeptide-based inhibitor of HIV-1 protease. Mvt-101 is also reduced-peptide-bond inhibitor. Mvt-101 inhibits reproduction of the HIV virus by blocking protease action [1].
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
[(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) is a selective inhibitor of HIV-1. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) inhibits viral infection and cell fusion by blocking the interaction between HIV-1 and CD4 molecules. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) can completely inhibit fusion formation at a concentration of 25 μM [1].
Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity [1].
HIV gag peptide (197-205) is a H-2K d-restricted epitope derived from the p24 portion of the HIV-1 gag protein, consists of amino acids 197-205 (AMQMLKETI) [1].
TAT-CBD3, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization [1].
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 [1].
VIR-165 is a modified form of virus inhibitory peptide (VIRIP) that binds the fusion peptide of the gp41 subunit and prevents its insertion into the target membrane. VIRIP inhibits a wide variety of human immunodeficiency virus type 1 (HIV-1) strains [1].
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1(HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection [1].
MPG, HIV related is 27-aa peptide, derived from both the nuclear localisation sequence of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41 and is a potent delivery agent for the generalised delivery of nucleic acids and of oligonucleotides into cultured cells.
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models [1].
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function [1].
Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a substrato peptídico of HIV-1 protease. Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 acts as the variable substrate in a peptidolytic assay to quantify the inhibition of the protease [1] .
Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1[1].
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1IC50 in vitro for ERK2 is 29 μM [1] .
2F5 epitope, a peptide gp41 (659-671), comprises the entire epitope for one of the three known antibodies capable of neutralizing a broad spectrum of primary HIV-1 isolates and is the only such epitope that is sequential. 2F5 epitope is recognized by broadly neutralizing antibodies 2F5 [1] .
mC46 (C46) peptide is a membrane-associated fusion peptide inhibitor. mC46 peptide potently inhibits HIV-1 replication and entry. mC46 also inhibits CCR5-tropic, CXCR4-tropic, and dual-tropic HIVs, SIV, and SHIV [1].
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
Retrocyclin-1 is a kind of Theta-defensin. Retrocyclin-1 recognizes and binds to carbohydrate-containing surface molecules, to protect cells from HIV-1 infection. Retrocyclin-1 exhibits high affinity to fetuin, gp120 (Kd=35.4 nM), CD4 (Kd=31 nM), and galactosylceramide (Kd=24.1 nM) [1].
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect [1] .
GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
Astodrimer (SPL7013 free base) is a large (3-4 nm,?~?16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties [1] .
Tat-HA-NR2B9 contains a fragment of the cellmembrane transduction domain of HIV-1 Tat, a influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c). Tat-HA-NR2B9 reduces infarct size and improves neurological functions in ischemia-induced cerebral injury in the rats [1]
HIV gp120 (318-327) is a short sequence of the HIV-1 strain IIIB envelope peptide (rgpgrafvti) that corresponds to the conserved C-terminal region of the glycoprotein. HIV gp120 (318-327) is part of the HIV vaccine V3 peptide epitope, also known as the I10 peptide. However, HIV gp120 (318-327) lacks the A2 anchor residues recognized by epitope-specific CTLs but has structural features that confer promiscuous A2 binding [1] .
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ [1] .
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ [1] .
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
(Cys47)-HIV-1 tat Protein (47-57) has membrane translocation function and can be used to derivatize the surface of magnetic pharmaceuticals and substantially facilitated their uptake into target cells [1] .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ [1] .
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research [1] .
Palicourein is a 37 amino acid cyclic polypeptide. Palicourein inhibits the in vitro cytopathic effects of HIV-1RF infection of CEM-SS cells with an EC50 value of 0.1 μM and an IC50 value of 1.5 μM [1].
Ibalizumab (TMB-355) is a humanised IgG4 monoclonal antibody that prevents HIV cell entry by binding to CD4 receptor. Ibalizumab has the potential for HIV-1 infection research [1].
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer [1].
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN,HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection [1] .
VRC-01 is a fully human IgG1 antibody that targets envelope glycoprotein gp120 Protein. VRC-01 blocks viral entry by partially mimicking the interaction of the CD4 receptor with HIV-1 gp120 envelope glycoprotein. The isotype control for VRC-01 can refer to Human IgG1 kappa, Isotype Control (HY-P99001) [1].
L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture [1] .
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity [1] .
Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
Fumagillin(NSC9168) is an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatu. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
Sennoside A is an anthraquinone glycoside found in senna (Cassia angustifolia). Sennoside A is an HIV-1 inhibitor (IC50=3.8 μM) that inhibits HIV-1 replication. Sennoside A also inhibits HIV-1 reverse transcriptase (RT)-related DNA polymerase (RDDP) and ribonuclease H (Ribonuclease H) with IC50s of 1.9 μM and 5.3 μM, respectively [1] .
Methyl salvionolate A is a potent inhibitor of HIV-1. Methyl salvionolate A inhibits P24 antigen in HIV-1 infected MT-4 cell with an EC50 of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with
IC50s of 50.58, 10.73 and 7.58 μg/ml, respectively [1].
Sennoside A (Standard) is the analytical standard of Sennoside A. This product is intended for research and analytical applications. Sennoside A is an anthraquinone glycoside, found in Senna (Cassia angustifolia) [1]. Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication .
Integracin B is a potent dimeric alkyl aromatic inhibitor of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. Integracin B inhibits both coupled and strand transfer activity of HIV-1 integrase [1].
L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture [1] .
Efavirenz (Standard) is the analytical standard of Efavirenz. This product is intended for research and analytical applications. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture [1].
Thiamine disulfide (Standard) is the analytical standard of Thiamine disulfide. This product is intended for research and analytical applications. Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity [1] .
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd [1], Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope . Neuroprotective effects [1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells .
Fumagillin (Standard) is the analytical standard of Fumagillin. This product is intended for research and analytical applications. Fumagillin(NSC9168) is an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatu. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
Trilobatin (Standard) is the analytical standard of Trilobatin. This product is intended for research and analytical applications. Trilobatin, a natural sweetener derived from?Lithocarpus polystachyus?Rehd [1], Trilobatin?is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope . Neuroprotective effects [1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively [1] .
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing [1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs [1].
Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies [1] .
Benanomicin A is a microbial metabolite and can be isolated from Actinomycetes.Benanomicin has antifungal activitya and inhibits HIV-1 viral infection in MT-4 cells [1] .
Agrocybin is an antifungal peptide that exerts antifungal activity against several fungal species but lacks inhibitory activity against bacteria. Agrocybin attenuates the activity of HIV-1 reverse transcriptase[1].
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitory activity against HIV-1 protease, with IC50 >100 μg/mL [1].
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins [1].
Bevirimat (Standard) is the analytical standard of Bevirimat. This product is intended for research and analytical applications. Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies[1][2][3][4].
Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing [1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities [1] .
Uncaric acid (6β,19α-Dihydroxyursolic acid) (compound 6) is a triterpene that can be found in Eriobotrya japonica. Uncaric acid shows anti HIV-1, HRV 1B, SNV activity [1].
Hinokinin (Standard) is the analytical standard of Hinokinin. This product is intended for research and analytical applications. Hinokinin (Compound 1) is a compound isolated from the stems of Hypoestes aristate. Hinokinin exhibits moderate activity of HIV-1 protease enzyme [1].
Clavirolide L (Compound 3) is a dolabellane-type diterpenoid that can be isolated from Clavularia viridis. Clavirolide L shows significant inhibition against HIV-1 without RT enzyme inhibition and can be used for HIV infection research [1].
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model [1] .
Ingenol-3-palmitate, an ingenane diterpenoid, is a nature product that could be isolated from the roots of Euphorbia ebracteolata. Ingenol-3-palmitate is a potent HIV-1 (HIV) inhibitor with an IC50 value of 4.1 nM [1].
Hinnuliquinone is a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease. Hinnuliquinone is a bis-indolyl-2,5-dihydroxybenzoquinone pigment, that can be isolated from Nodulisphorium hinnuleum[1] .
Glycolithocholic acid 3-sulfate (SLCG) is a cholic acid derivative and a metabolite of glycolithocholic acid. Glycolithocholic acid 3-sulfate inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate can be used for the research of HIV infection and gallbladder disease [1] .
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits Raf/MEK/MAPK pathway [1].
Lucidenic lactone is a terpene compound, is a DNA polymerase inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively [1].
Lucidenic acid O is a terpene compound, is a DNA polymerases inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively [1].
3β-Hydroxy-27-p-Z-coumaroyloxyurs-12-en-28-oic acid (compound 8) is a triterpenoid ester HIV-1 protease inhibitor with the potential for use in the antiretroviral combination therapy of AIDS [1].
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B [1] .
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives [1] .
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) [1] .
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1] .
Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
Erythromycin Ethylsuccinate (Standard) is the analytical standard of Erythromycin Ethylsuccinate. This product is intended for research and analytical applications. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Limonin (Standard) is the analytical standard of Limonin. This product is intended for research and analytical applications. Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities [1] .
Scirpusin A is a naturally occurring compound extracted from the legume plant Caragana rosea Turcz, exhibiting anti-HIV activity. Scirpusin A demonstrates significant inhibitory effects against HIV-1 (EC50=7 μg/mL). Scirpusin A is utilized in research towards the development of anti-HIV therapeutics [1].
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity [1] .
Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression [1] .
Inophyllum B ((+)-Inophyllum B) is a potent HIVReverse Transcriptase inhibitor with an IC50 value of 38 nM. Inophyllum B inhibits HIV-1(IC50=1.4 μM) in vitro cell culture. Inophyllum B can be isolated from the acetone extract of the giant African snail, Achatina fulica[1].
Teicoplanin is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity [1] .
Teicoplanin sodium is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity [1] .
Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina?L. Rosamultin has inhibitory effects against HIV-1 protease[1]. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects .
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine [1].
Ganoderic acid B (Standard) is the analytical standard of Ganoderic acid B. This product is intended for research and analytical applications. Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) [1] .
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc [1] .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure [1] .
Escin IA (Standard) is the analytical standard of Escin IA. This product is intended for research and analytical applications. Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration [1]. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of
3.49 μM .
Asterriquinone (ARQ), a Asterriquinone analog, is a Grb-2 binding inhibitor. Asterriquinone inhibits the Grb-2 binding activity to tyrosine phosphorylated EGFR, with an IC50 of 8.37 μM. Asterriquinone is a HIV1 reverse transcriptase inhibitor with a Ki of 2.3 μM. Asterriquinone also inhibits Grb-7 and PLC-γ binding activities. [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation [1] . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects [1] .
Diphyllin is an orally active V-ATPase inhibitor (IC50=17 nM) and HIV-1 inhibitor (IC50=0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC50=0.6 nM for acid influx inhibition)， thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption [1] .
Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation [1] . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
α-Lipoic Acid (sodium) (Standard) is the analytical standard of α-Lipoic Acid (sodium). This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4]. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1[5].
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1(BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [1] . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Theaflavin 3,3'-digallate (Standard) is the analytical standard of Theaflavin 3,3'-digallate. This product is intended for research and analytical applications. Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
Ivermectin (Standard) is the analytical standard of Ivermectin. This product is intended for research and analytical applications. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1(BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [1] . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
Scutellarin (Standard) is the analytical standard of Scutellarin. This product is intended for research and analytical applications. Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
4-Deoxy-4α-phorbol is a tetracyclic diterpene found in E. desmondi. It has been used in the semisynthesis of inhibitors of the HIV-1-induced cytopathic effect on MT-4 cells and 4α-phorbol esters [1].
Wikstrol A is a potent antifungal, antimitotic and anti-HIV-1 Agent. Wikstrol A induces morphological deformation of P. oryzae mycelia with an MMDC value of 70.1 µM. Wikstrol A shows activity against microtubule polymerization with an IC50 value of 131 µM. Wikstrol A shows anti-HIV-1 activity with an IC50 value of 67.8 µM [1].
Schineolignin C is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities [1].
Schineolignin B is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities [1].
Kadsuracoccinic acid A is a tetracyclic natural compound that can be isolated from the stems of Kadsura coccinea. Kadsuracoccinic acid A has vitro anti-HIV-1 activitiy with an EC50 value of 68.7 μM [1].
20(21)-Dehydrolucidenic acid A is a triterpenoid isolated from the fruiting body of the fungus Ganoderma sinense. 20(21)-Dehydrolucidenic acid A has weak anti-HIV-1 protease activity [1].
Lamellarin E is a biologically active marine alkaloid, while the Lamellarin series of alkaloids show potential cytotoxicity, topoisomerase I inhibition, protein kinase inhibition, multidrug resistance reversal, and anti-HIV-1 activity [1].
5-Dexyexcoecafolin B is a tigliane-type diterpenoid isolated from the EtOAc extract of Excoecaria acerifolia Didr. 5-Dexyexcoecafolin B has anti-HIV-1 activity with a EC50 value of 0.036 μM [1].
Docosyl trans-ferulate (compound 2) is an antiviral compound. Docosyl trans-ferulate exhibits anti-HIV-1 activity in anti-syncytial assays using the ΔTat/revMC99 virus and 1A2 cell line systems [1].
Isoescin IA (Standard) is the analytical standard of Isoescin IA. This product is intended for research and analytical applications. Isoescin IA is a triterpenoid saponin isolated from the seeds of Aesculus chinensis. Isoescin IA has anti-HIV-1 protease activity [1].
Periglaucine A, a hasubanane-type alkaloid, can be isolated from Pericampylus glaucus. Periglaucine A can inhibits HBV surface antigen (HBsAg) secretion in Hep G2.2.15 cells. Periglaucine A also shows anti-HIV-1 activity in C8166 cells (EC50: 204 μM) [1].
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum[1].Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM .
13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM [1].13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis .
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties [1] .
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity [1].
Zingibroside R1 possesses some anti-HIV-1 activity.
Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM) .
HIV-1 gp140 Protein is the gp160 ectodomain, and can lead to the production of trimers that can mimic the native Env spike. HIV-1 gp140 trimers is able to elicit neutralizing antibody responses in immunized animals. HIV-1 gp140 Protein (646a.a, HEK293, Fc) is the recombinant Virus-derived HIV-1 gp140 protein, expressed by HEK293 , with C-hFc labeled tag.
The capsid protein p24 forms the conical core of the genome RNA-nucleocapsid complex in the virion. Promote immune invasion by hiding the viral DNA detected by CGAS. The viral capsid protein p24 is considered to be another early virological biomarker of infection. p24 Protein, HIV-1 (AAB50258, His) is the recombinant Virus-derived p24 protein, expressed by E. coli , with C-His labeled tag.
The capsid protein p24 forms the conical core of the genome RNA-nucleocapsid complex in the virion. Promote immune invasion by hiding the viral DNA detected by CGAS. The viral capsid protein p24 is considered to be another early virological biomarker of infection. p24 Protein, HIV-1 (BAH97658, His) is the recombinant Virus-derived p24 protein, expressed by E. coli , with C-His labeled tag.
The capsid protein p24 forms the conical core of the genome RNA-nucleocapsid complex in the virion. Promote immune invasion by hiding the viral DNA detected by CGAS. The viral capsid protein p24 is considered to be another early virological biomarker of infection. p24 Protein, HIV-1 (ACI05538, His) is the recombinant Virus-derived p24 protein, expressed by E. coli , with C-His labeled tag. The total length of p24 Protein, HIV-1 (ACI05538, His) is 231 a.a., with molecular weight of ~26.5 kDa.
The capsid protein p24 forms the conical core of the genome RNA-nucleocapsid complex in the virion. Promote immune invasion by hiding the viral DNA detected by CGAS. The viral capsid protein p24 is considered to be another early virological biomarker of infection. p24 Protein, HIV-1 (AAB61122, His) is the recombinant Virus-derived p24 protein, expressed by E. coli , with C-His labeled tag. The total length of p24 Protein, HIV-1 (AAB61122, His) is 231 a.a., with molecular weight of ~27 kDa.
The capsid protein p24 forms the conical core of the genome RNA-nucleocapsid complex in the virion. Promote immune invasion by hiding the viral DNA detected by CGAS. The viral capsid protein p24 is considered to be another early virological biomarker of infection. p24 Protein, HIV-1 (AAA44868, His) is the recombinant Virus-derived p24 protein, expressed by E. coli , with C-His labeled tag.
envelope glycoprotein gp120 Protein is a glycoprotein exposed on the surface of the HIV envelope.Gp120 is essential for viral infection as it facilitates HIV entry into the host cell.gp120 may also be facilitating viral persistence and continuing HIV infection by influencing the T cell immune response to the virus.gp140 Protein, HIV-1 (647a.a, HEK293, Fc) is the recombinant Virus-derived gp140 protein, expressed by HEK293 , with C-hFc labeled tag.
gp140 is a non-cleaved exodomain of (gp160)3, with both its transmembrane segment (TM) and cytoplasmic tail (CT) truncated, and is often considered a possible replacement for natural Env spikes.However, most HIV-1 gp140 preparations are unstable and have an uneven conformation.gp140 Protein, HIV-1 (HEK293, Fc) is the recombinant Virus-derived gp140 protein, expressed by HEK293 , with C-hFc labeled tag.
Envelope glycoprotein gp160 Protein (HIV-1 gp160 Protein) is the sole antigenic protein on the surface of the HIV-1 virion and mediates HIV-1 entry into target cells. The endoproteolytic processing of HIV-1 gp160 membrane glycoprotein precursor into gp120 and gp41 is necessary for formation of infectious HIV particles. HIV-1 gp160 induces endothelial cell apoptosis, which is mediated by CXCR4 chemokine receptor. envelope glycoprotein gp160 Protein, HIV-1 (ADD25380, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp160 protein, expressed by HEK293 , with C-His labeled tag.
The envelope glycoprotein gp120 protein facilitates viral capture and dissemination by dendritic cells and endothelial cells by attaching the virus to host lymphocytes through binding to the CD4 receptor.HIV exploits the migratory properties of dendritic cells to access CD4+ T cells, leading to infection.envelope glycoprotein gp120 Protein, HIV-1 (AAC31819, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp120 protein, expressed by HEK293 , with C-His labeled tag.
gp160 is an envelope glycoprotein that oligomerizes into major trimers in the host endoplasmic reticulum.gp160 is transported in the host Golgi apparatus to complete the glycosylation process.The precursors are proteolytic cleaved in the trans-Golgi apparatus to produce gp120 and gp41.envelope glycoprotein gp160 Protein, HIV-1 (AAT67478, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp160 protein, expressed by HEK293 , with C-His labeled tag.
envelope glycoprotein gp120 Protein is a glycoprotein exposed on the surface of the HIV envelope.Gp120 is essential for viral infection as it facilitates HIV entry into the host cell.gp120 may also be facilitating viral persistence and continuing HIV infection by influencing the T cell immune response to the virus.envelope glycoprotein gp120 Protein, HIV-1 (ACY40659, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp120 protein, expressed by HEK293 , with C-His labeled tag.
envelope glycoprotein gp120 Protein is a glycoprotein exposed on the surface of the HIV envelope.Gp120 is essential for viral infection as it facilitates HIV entry into the host cell.gp120 may also be facilitating viral persistence and continuing HIV infection by influencing the T cell immune response to the virus.envelope glycoprotein gp120 Protein, HIV-1 (AFM77980, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp120 protein, expressed by HEK293 , with C-His labeled tag.
CCR5 Protein, a receptor for inflammatory CC-chemokines like CCL3/MIP-1-alpha, CCL4/MIP-1-beta, and RANTES, transduces signals, elevating intracellular calcium levels. It regulates granulocytic lineage and facilitates T-lymphocyte migration to infection sites. In microbial infection, CCR5 acts as a coreceptor, along with CD4, for HIV-1, emphasizing its role in the cellular response to infections. CCR5 Protein, Human (HEK293, Flag, His, Strep) is the recombinant human-derived CCR5 protein, expressed by HEK293 Cell-free , with N-Flag, C-His, C-Strep labeled tag.
envelope glycoprotein gp120 Protein is a glycoprotein exposed on the surface of the HIV envelope.Gp120 is essential for viral infection as it facilitates HIV entry into the host cell.gp120 may also be facilitating viral persistence and continuing HIV infection by influencing the T cell immune response to the virus.envelope glycoprotein gp120 Protein, HIV-1 (AAC57427, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp120 protein, expressed by HEK293 , with C-His labeled tag.
envelope glycoprotein gp120 Protein is a glycoprotein exposed on the surface of the HIV envelope.Gp120 is essential for viral infection as it facilitates HIV entry into the host cell.gp120 may also be facilitating viral persistence and continuing HIV infection by influencing the T cell immune response to the virus.envelope glycoprotein gp120 Protein, HIV-1 (AAA44191, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp120 protein, expressed by HEK293 , with C-10*His labeled tag.
CCR5 protein is a receptor for inflammatory CC chemokines, including CCL3/MIP-1-alpha, CCL4/MIP-1-beta, and RANTES, and plays a crucial role in signal transduction by increasing intracellular calcium levels. . It acts as a chemoattractant receptor and contributes to granulocyte lineage control and T lymphocyte migration to sites of infection. CCR5 Protein, Mouse (P. pastoris, His) is the recombinant mouse-derived CCR5 protein, expressed by P. pastoris , with N-6*His labeled tag.
OTUD2 is a key hydrolase in cellular processes that actively participates in endoplasmic reticulum-associated degradation (ERAD) by deubiquitinating misfolded luminal proteins. It trims ubiquitin chains from the substrate, helping them pass through the VCP/p97 pore. OTUD2 Protein, Human is the recombinant human-derived OTUD2 protein, expressed by E. coli , with tag free.
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). 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 [1] . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
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 [1] . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
(Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. (Rac)-Efavirenz-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Nevirapine-d4 is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. 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[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. Efavirenz-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) [1]. 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 3CL pro inhibitor with an IC50 of 14.2 μM .
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria [1].
Nevirapine-d5 (BI-RG 587-d5) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM [1].
Nevirapine-d8 (BI-RG 587-d8) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM [1].
Nevirapine-d3 (BI-RG 587-d3) is the deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor [1].
Nelfinavir-d4 is deuterated labeled Nelfinavir (HY-15287). Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent [1] .
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) [1]. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [1] .
Fostemsavir-d8 (BMS-663068-d8) is deuterium labeled Fostemsavir. Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
Dapivirine-d4 (TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations [1] .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis[1][2][3][4].
Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively [1].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 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 3CL pro inhibitor [1] .
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 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [1] .
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Elvitegravir- 13C6 (GS-9137- 13C6) is 13C labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB,HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively [1].
Etravirine-d8 is the deuterium labeled Etravirine. Etravirine (R165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV[1][2].
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
Tizoxanide-d4 is the deuterium labeled Tizoxanide. Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities[1][2].
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
Rilpivirine- 13C6 (R278474- 13C6) is 13C labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively [1] . AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively [1] . Censavudine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains [1]. Azvudine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
HIV-1 inhibitor-71 (compound 2a) blocks the transport of endocytosed HIV-1 particles into nuclear envelope invagination (NEIs) that can inhibit productive infection [1].
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K [1]. Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms [1].
EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms [1]. EFdA-TP (tetraammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1 RT with multiple mechanisms [1]. EFdA-TP (tetrasodium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains [1]. Azvudine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells [1]. 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity [1]. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection . Azt-pmap is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
NRTT-IN-1 (Compound 1) is inhibitor for nucleoside reverse transcriptase translocation (NRTT), that inhibits the DNA synthesis and viral replication of HIV .
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity [1]. 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
ssRNA40 (sodium) is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. ssRNA40 is a uridine-rich ssRNA derived from the HIV-1 long terminal repeat on activation of NK cells via TLR7/8[1][2].
1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine is a polyunsaturated phospholipid that is a constituent of lipid monolayers and small unilamellar vesicles. 1,2-Didocosahexaenoyl-sn-glycero-3-phosphocholine can be used to prepare endoplasmic reticulum-targeted liposomes (PERLs) in a molar ratio of 1.5:1.5:1:1 with 1,2-didocosahexaenoyl-sn-glycero-3-phosphoethanolamine, l-α-phosphatidylinositol, and l-α-phosphatidylserine. PERLs can reduce cholesterol levels in human peripheral blood mononuclear cells (PBMCs) and reduce HIV-1 particle secretion from HIV-1 infected PBMCs [1].
ODN 6016 sodium is a CpG-A oligonucleotides. ODN 6016 sodium can induce IFN-α production, and can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G [1] .
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains [1]. Azvudine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains [1]. Azvudine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G [1] .
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