CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity[1].
HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 µM. HBV-IN-23 inhibits HBV DNA replication in both drug sensitive and resistant HBV strains. HBV-IN-23 shows anti-hepatocellular carcinoma cell (HCC) activities. HBV-IN-23 induces HepG2 cells apoptosis[1].
Deleobuvir (BI-207127, BI207127) is a potent, selective HCV NS5B polymerase inhibitor with IC50 of 50 nM against GT-1 HCV polymerase activity; demonstrates subgenomic antiviral activity against GT1b and GT1a with EC50 of 11 and 23 nM in cell-based replicon assays; shows weak or no inhibition in specificity assays that include poliovirus RdRp, mammalian DdRp II, and DNA polymerase α, β, and γ; displays good antiviral potency and tolerability in early clinical trials of short-term treatment either as a single agent or in combination with pegylated IFN-α2a/ribavirin in HCV GT1 patients. HCV Infection Phase 3 Clinical
Deoxylapachol is a major cytotoxic component of New Zealand brown alga, Landsburgia quercifolia. Deoxylapachol has antifungal and anti-cancer activity[1].
Anthrarobin is an antipsoriatic agent with antibacterial and oxidative potential.
Cotrimoxazole (Trimethoprim/sulfamethoxazole 1:19), an antimicrobial agent, is a Trimethoprim and Sulfamethoxazole mixture. The ratio of Trimethoprim to Sulfamethoxazole in the combination mixture is 1 : 19[1].
Antifungal agent 48 (Example 308) is an antifungal agent. Antifungal agent 48 is active against Cryptococcus neoformans with a MIC value of 11 μM[1].
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM[1].
Methyl 1-hydroxy-4-oxocyclohexaneacetate (Compound7) is a lactone. Methyl 1-hydroxy-4-oxocyclohexaneacetate is isolated from the natural Senecio scandens. Methyl1-hydroxy-4-oxocyclohexaneacetate has anti-inflammatory andantibacterialactivity [1].
Triclocarban is an antimicrobial agent used in personal cleaning products.
Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities[1][2].
Plm IV inhibitor-1 (compound 6) is a potent plasmepsin IV (Plm IV) inhibitor with IC50s of 4.1, 0.80, 0.25, 0.35 µM for Plm I, Plm II, Plm IV, Cat D, respectively[1].
Stephanine ((-)-Stephanine) is an isoquinoline aporphine-type alkaloid. Stephanine induce apoptosis through the reverse of mitotic exit. Stephanine exhibits Antiplasmodial activity. Stephanine can be used for the research of stomach pain, abdominal pain, arthritis and cancer[1][2].
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication[1]. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation [2].
Derquantel is a potent anthelmintic. Derquantel causes flaccid paralysis and expulsion of nematodes[1].
Astromicin (KW-1070) is a water-soluble aminoglycoside antibiotic that can be isolated from the genus Micromonospora. Astromicin exhibits broad spectrum antibacterial activity against gram positive and negative bacteria[1][2][3].
Gentamicin C1a is the precursor of the semi-synthetic antibiotic Etimicin, and has antibacterial activity. Gentamicin C1a is the major component of the Gentamicin complex[1][2].
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].
trans-4-Methylcyclohexanamine is an intermediate and can be used for the development of T. cruzi enzyme inhibitor[1].
LW3 is a potent antifungal agent. LW3 has antifungal activity with EC50 values of 0.54, 0.09, 1.52, and 2.65 mg/L against B. cinerea, R. solani, S. sclerotiorum, and F. graminearum, respectively[1].
NHC-diphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form[1]. NHC is a pyrimidine ribonucleoside and behaves as a potent anti-virus agent. NHC effectively inhibits the replication of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV)[1].
ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research[1][2].
3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot[1].
STING agonist-24 (CF504) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
HBV Seq1 aa:63-71 is the fragment of hepatitis B virus (HBV)[1].
Alisporivir intermediate-1 is an intermediate in the synthesis of Alisporivir. Alisporivir is used for the treatment of inflammatory and viral diseases.
Tecovirimat(ST-246) is an orally bioavailable antipoxvirus compound; potent and selective active against multiple orthopoxviruses with EC50 about 10 nM.IC50 value: 10 nM [1]Target: antipoxvirusin vitro: ST-246 targets the cowpox virus V061 gene, which encodes a major envelope protein homologous to the vaccinia virus F13L gene product. The antiviral potency and selectivity of ST-246 was measured in CPE assays against a panel of DNA- and RNA-containing viruses. In these assays, the EC50 for inhibition of vaccinia virus was determined to be 0.01 μM, while the EC50 values for inhibition of unrelated viruses were >40 μM [1]. ST-246 was evaluated for activity against cowpox virus (CV), vaccinia virus (VV), and ectromelia virus (ECTV) and had an in vitro 50% effective concentration (EC50) of 0.48 microM against CV, 0.05 microM against VV, and 0.07 microM against ECTV. The selectivity indices were >208 and >2,000 for CV and VV, respectively. The in vitro antiviral activity of ST-246 was significantly greater than that of cidofovir, which had an EC50 of 41.1 microM against CV and 29.2 microM against VV, with selectivity indices of >7 and >10, respectively [2]. in vivo: Mice were treated with placebo (vehicle), ST-246 administered by oral gavage at 50 mg/kg twice a day (b.i.d.) for 14 days, or CDV administered as a single intraperitoneal (i.p.) injection at 100 mg/kg. ST-246-treated mice mounted a protective immune response to vaccinia virus infection [1]. ST-246 administered once daily by oral gavage to mice infected intranasally with CV beginning 4 h or delayed until 72 h postinoculation was highly effective when given for a 14-day duration using 100, 30, or 10 mg/kg of body weight. When 100 mg/kg of ST-246 was administered to VV-infected mice, a duration of 5 days was sufficient to significantly reduce mortality even when treatment was delayed 24 h postinoculation. Viral replication in liver, spleen, and kidney, but not lung, of CV- or VV-infected mice was reduced by ST-246 compared to levels for vehicle-treated mice [2].
CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs.
3-O-α-L-Rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl hederagenin28-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranosyl ester is a hederagenin-type saponin with antitumor and anti-inflammatory properties[1].