low cytotoxicity

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

Antimicrobial agent-22 (THI 6c) is a broad-spectrum, multi-target antibacterial with rapid bactericidal efficacy, effective anti-biofilm activity, and low cytotoxicity and hemolytic properties [1].

Bictegravir Sodium (GS-9883 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

DODAP is an ionic cationic lipid with low cytotoxicity and high transfection efficiency that can be used to synthesize liposomes and encapsulate biologically active molecules such as mRNA, siRNA and plasmid DNA.

Bz-RS-ISer(3-Ph)-Ome (Methyl (2R,3S)-3-(benzoylamino)-2-hydroxy-3-phenylpropanoate) is a paclitaxel derivative that inhibits the HSV replication cycle at low cytotoxicity, blocks mitosis in Vero cells, affects the size of M-MSV-induced tumors, and influences the immune response by inhibiting PHA-induced proliferation of T lymphocytes.

Antimalarial agent 14 (NSC-102533) is a bioactive chemical.

YYA-021 inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.

Tau-aggregation and neuroinflammation-IN-1 is a potent inhibitor of tau protein aggregates, showing significant inhibitory activity against AcPHF6 and full-length tau protein aggregates. It has anti-inflammatory activity, reduces NO release, exhibits low cytotoxicity against LSP-stimulated BV2 cells, and reverses okadaic acid-induced memory impairment in rats.

Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp/Carbonic anhydrase-IN-2 induced apoptosis.Enpp/Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.

Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside, a flavonoid extracted from Glycyrrhiza roots, exhibits low cytotoxicity on a variety of tumor and normal cells.

Rilematovir (JNJ-678) is an inhibitor of fusion protein with antiviral activity and low cytotoxicity. Rilematovir can be used in studies about respiratory syncytial virus treatment.

MMG-11 inhibits both TLR2 1 and TLR2 6 signaling (IC50s: 1.7 μM for Pam3CSK4-induced hTLR2 1 and 5.7 μM for Pam2CSK4-induced hTLR2 6 responses). MMG-11 is an effective and selective human TLR2 antagonist with low cytotoxicity.

ATP-polyamine-biotin is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM. ATP-polyamine-biotin is shown to promote biotin labeling

LpxC-IN-14 (compound 6i) is an effective inhibitor of LpxC, exhibiting antibacterial activity and low cytotoxicity. It also demonstrates an acceptable plasma protein binding rate.

SARS-CoV-2-IN-97 (Compound CO-01) is an inhibitor of the SARS-CoV-2Nsp15 endoribonuclease, exhibiting an IC50 of 53.5 μM. It demonstrates low cytotoxicity in A549-AT cells with an IC50 value of 134 μM.

HIV-1protease-IN-14 (compound 5ae) is an effective inhibitor of HIV-1protease, exhibiting Ki values of 0.28 nM and 56.9 nM against WTHIV-1PR and R41THIV-1PR, respectively. This compound also demonstrates low cytotoxicity.

SARS-CoV-2-IN-96 (compound 12b) acts as an inhibitor for both HCoV-OC43 (EC50= 97 nM) and SARS-CoV-2 (EC50= 45 nM), while displaying low cytotoxicity in Huh7 cells (CC50=10 μM).

PS-166276 is a potent p38 inhibitor with low cytotoxicity. It exhibits an IC50 value of 28 nM against p38 kinase and an IC50 of 170 nM in the THP-1 TNFα assay.

MDG506 is a novel selective androgen receptor (AR) interaction disruptor that demonstrates low cytotoxicity in prostate cancer (PCa) models and shows a dose-dependent reduction in prostate-specific antigen expression induced by classical antiandrogens.

TXY541 is an orally active antibacterial agent that is converted into PC190723 under physiological conditions. It demonstrates strong antibacterial activity against Staphylococcus aureus and exhibits low cytotoxicity towards mammalian cells.

hDHODH-IN-16 (Compound 3t) is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 0.11 μM. It demonstrates very low cytotoxicity towards healthy HaCaT cells, with an IC50 value exceeding 200 μM.

HIV-1inhibitor-79 (Compound 3k) is an HIV inhibitor that demonstrates significant inhibitory activity against HIV-1 and its common mutants, with IC50 values of 1.9 nM for HIV-1, K103, 8.7 nM for L100I, and 11 nM for E138K. It exhibits low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1inhibitor-79 shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and effectively inhibits HIV-1 reverse transcriptase with an IC50 of 25 nM.