low cytotoxicity

Topovale (ARC111) is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.

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.

Eugenitin, a polyketide from Mycoleptodiscus indicus, exhibits inhibitory activity against Leishmania major with an LD50 of 39.9 μM and demonstrates low cytotoxicity (IC50 >131 μM) in various human cancer cell lines [1].

SARS-CoV-2-IN-62 (Compound R3b) effectively inhibits SARS-CoV-2 replication in Vero E6 and Calu-3 cells, demonstrating low cytotoxicity and EC50 values of 2.97 μM and 3.82 μM, respectively [1].

Penduletin has anti-inflammatory,anti-tumor cells, and anti-bacterical activities,it inhibits growth of the Gram-negative pathogen neisseria gonorrhoeae. Penduletin has strong activity in vitro against EV71 with low cytotoxicity.

CB2R Probe 1, a cannabinoid 2 receptor (CB2R) fluorescent probe, exhibits both safety and environmental friendliness, boasting a dissociation constant (K i) of 130 nM. Notably, it demonstrates low cytotoxicity within cancer cells [1].

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.

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

2,3-Dehydro-3,4-dihydro ivermectin, an ivermectin analog and anthelmintic, demonstrates efficacy against L. amazonensis promastigotes and amastigotes, with IC50 values of 13.8 and 3.6 µM, respectively, while maintaining a low cytotoxicity profile in macrophages (IC50 = 65.5 µM).

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.

SARS-CoV-2-IN-63 (Compound R3e) serves as an inhibitor of SARS-CoV-2 replication, demonstrating low cytotoxicity. It effectively suppresses viral replication within Vero E6 cells and Calu-3 cells, yielding half-maximal effective concentration (EC50) values of 1.99 μM and 1.92 μM, respectively [1].

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

Decarine has high antibacterial activity against mycobacterial, gram-positive and gram-negative bacteria, and low cytotoxicity towards human macrophages.Decarine inhibits fMLP/CB-induced elastase release with IC(50) values < or = 5.53 microg/mL.

2,3-Dihydroxy-olean-12-en-28-oic acids show a low cytotoxicity towards several human tumor cell lines.

MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein. It effectively prevents MLKL phosphorylation and oligomerization, which are critical steps in cell necrosis. Additionally, MLKL-IN-6 restrains the death of immune cells, diminishes the expression of adhesion factors, and exhibits low cytotoxicity. Furthermore, it impedes the activation of hepatic stellate cells, decreases levels of liver fibrosis markers, and exerts anti-fibrotic effects [1].

ZIKV-IN-6 (compound 22) acts as a direct inhibitor of the Zika virus (ZIKV) by binding to its RNA-dependent RNA polymerase (RdRp) and obstructing viral RNA synthesis mediated by the ZIKV NS5 protein. This compound also demonstrates low cytotoxicity (CC50 >50 μM) and mitigates the excessive inflammatory response and pyroptosis [1].

Tazettine, an alkaloid, exhibits low cytotoxicity towards mammalian cell lines, with a CC50 value exceeding 100 μg/mL [1].

Cisplatin-resistant cells-IN-1 (Compound 8) exhibits high cytotoxicity against Cisplatin-resistant cells and effectively diminishes metabolic activity at low nanomolar concentrations, with an IC50 ranging from 0.14 to 1.79 μM in various resistant cell lines, including A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR [1].

19-Hydroxy-10-deacetylbaccatin III (compound 13), a taxane potentially active against tumors, exhibits low cytotoxicity towards A498 and NCI-H226 cell lines. At a concentration of 30 μg/mL, it inhibits A498 and NCI-H226 cell growth by 16.6% and 32%, respectively [1].

Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul

Antiviral agent 20 (Compound 17b) is a selective inhibitor of Zika virus (EC50: 4.5 μM) and exhibits low cytotoxicity.

SARS-CoV-2-IN-55 (compound 65) is an inhibitor of SARS-CoV-2 exhibiting low cytotoxicity, characterized by an IC50 of 0.3 μM, effectuated through direct interaction with VSV-S pseudoparticles [1].

Cholicamideβ (compound 6), a self-assembling small molecule cancer vaccine adjuvant, forms low cytotoxicity virus-like particles and upon binding to peptide antigens, enhances dendritic cell-mediated antigen presentation and induces antigen-specific T-cell responses, with the ability to induce apoptosis and necrosis [1].

HIV-1 inhibitor-29 is a potent inhibitor of HIV-1 and acts against HIV-1 IIIB (EC50: 2.18 μM). HIV-1 inhibitor-29 shows high resistance to the F227L/V106A strain with an EC50 value of 0.974 μM. HIV-1 inhibitor-29 showed low cytotoxicity against MT-4 cells with a CC50 value of 211 μM. HIV-1 inhibitor-29 can be used in AIDS research.

HIV-1 inhibitor-21 (compound 9b) is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) and acts on HIV-1 RT (IC50: 0.55 μM). HIV-1 inhibitor-21 inhibits both wild-type HIV-1 (EC50: 12.7 nM) and mutant virus strain K103N (EC50: 10.4 nM) with relatively low cytotoxicity (CC50 for MT-4: 10.2 μM).

α-Synuclein inhibitor 8 effectively impedes α-Synuclein aggregation and disaggregation with an IC50 of 2.5 µM, demonstrating substantial reduction in neuronal inclusion formation, which contributes to reparative effects in damaged neurons and symptomatic improvement in Parkinson’s disease (PD)-like models. The compound also exhibits high antioxidant activity and low cytotoxicity [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

HDAC-IN-49 is a potent, non-selective inhibitor of HDAC (HDAC), demonstrating IC50 values of 13 nM for HDAC1, 14 nM for HDAC2, 21 nM for HDAC3, 1880 nM for HDAC4, and 10 nM for HDAC6. This compound exhibits significant antileukemic activity while maintaining low cytotoxicity towards healthy cells.

FtsZ-IN-8, a potent inhibitor of FtsZ, both promotes FtsZ polymerization and inhibits its GTPase activity, leading to the inhibition of bacterial division and subsequent bacterial cell death. This compound exhibits bactericidal activity without significant induction of bacterial resistance and possesses rapid bactericidal properties. Additionally, FtsZ-IN-8 demonstrates low hemolytic activity and cytotoxicity towards mammalian cells [1].

FtsZ-IN-6 is a potent inhibitor of FtsZ, enhancing its polymerization while inhibiting its GTPase activity, thereby obstructing bacterial cell division and causing bacterial cell death. This compound exhibits bactericidal properties without significant induction of bacterial resistance and demonstrates rapid bactericidal effects. Moreover, FtsZ-IN-6 has low hemolytic activity and cytotoxicity towards mammalian cells [1].

Influenza virus-IN-3 (compound 9) is a potent inhibitor of selective influenza viruses, acting on H5N1 (IC50: 0.88 μM), H5N2 (IC50: 0.10 μM), H5N6 (IC50: 5.5 μM), H5N8 (IC50: 0.51 μM). Influenza virus-IN-3 has antiviral and NA (neuraminidase) inhibitory effects and low cytotoxicity (CC50>200 μM).

Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent that inhibits viral 2C protein. Viral 2C protein inhibitor 1 has relatively low cytotoxicity and high selectivity index that inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC 50 s of 0.1~3.6 μM [1].

Antiparasitic agent-8 (Compound 9) exhibits potent antiparasitic activity against Hymenolepis nana, while demonstrating low levels of cytotoxicity [1].

Antileishmanial agent-9 (compound 16c) exhibits potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM. In addition, this compound demonstrates relatively low cytotoxicity in L-6 cells, with an IC50 value of 40.1 μM [1].

DprE1-IN-1 is a potent, orally active DprE1 inhibitor that exhibits good hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 has good anti-branched bacilli activity in macrophages, reducing 1.29 log10 CFU.

ZIKV-IN-1 is a potent inhibitor of zika virus (EC50: 2.8 μM, EC90: 6.8 μM). zIKV-IN-1 has anti-ZIKV effects and low cytotoxicity. zIKV-IN-1 shows high affinity for the RdRp domain of ZIKV.

MMG-0358 is a novel potent IDO1 inhibitor, showing low cytotoxicity and higher selectivity for IDO1 over TDO enzyme.

Influenza A virus-IN-7 (compound 16r) is a potent, orally active inhibitor of influenza A virus (IC50: 3.43 μM, CC50>100 μM). Influenza A virus-IN-7 is an anti-IAV agent with low cytotoxicity and inhibits viral RNA transcription and replication.

Antimycobacterial agent-3 is an antimycobacterial agent with low cytotoxicity. antimycobacterial agent-3 is effective against sensitive MTB strain H37Rv and resistant clinical isolates (MIC < 0.029-0.110 μ M).

NDNA4 (compound 17) is a selective Hsp90α inhibitor (IC50: 0.34 μM), characterized by its permanent charge and low membrane permeability. It exhibits minimal cytotoxicity against Ovcar-8 and MCF-10A cell lines (IC50 >100 μM) and maintains hERG channel maturation without eliciting a heat shock response or degrading Hsp90α-dependent client proteins [1].

BChE-IN-16 (compound 87) is a potent inhibitor of human butyrylcholinesterase (hBChE) exhibiting an inhibition concentration half-maximum (IC50) of 3.8 nM. It demonstrates low cytotoxicity and potential for central nervous system (CNS) permeability, along with unique adaptability, rendering it a valuable tool for research into Alzheimer's disease (AD).

Antimicrobial agent-22 (THI 6c) is an antimicrobial agent with low cytotoxicity, anti-biofilm activity and rapid bactericidal action.

Tyrosinase-IN-14 (compound 7m), a tyrosinase inhibitor, modulates the enzyme's secondary structure to diminish its catalytic function, exhibits low cytotoxicity, and possesses anti-browning properties that effectively prevent banana discoloration during storage [1].

MPI60 is a potent inhibitor of SARS-CoV-2 main protease (M^pro) exhibiting high antiviral efficacy, low cellular cytotoxicity, and considerable in vitro metabolic stability, making it suitable for SARS-CoV-2 research [1].

Acyclovir alanine is a pro-drug of Acyclovir. Acyclovir works by decreasing the production of DNA of the virus and it shows very low cytotoxicity.

OX2R-IN-1 is an OX2R antagonist (a potential OX2R binding agent) that exhibits low cytotoxicity (IC50: 484 μM). oX2R-IN-1 has blood-brain barrier permeability and a short drug half-life.

GRGDSPC, a 7-amino acid peptide, is a thiolated cell adhesion peptide.This peptide is an ideal novel targeted non-viral gene delivery vector, which was easy to be synthesized, high efficient and low cytotoxicity.

Tyrosinase-IN-8, a potent inhibitor of tyrosinase, demonstrates an inhibitory concentration (IC 50) value of 1.6 µM and exhibits low cytotoxicity while effectively inhibiting cell growth.

AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor. AChE/BChE-IN-8 shows Ki of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 has blood-brain barrier permeability and low cytotoxicity.

ZLMT-12 (compound 35) is a tacrine derivative and a potent inhibitor of CDK2 (IC50: 0.011 μM) and CDK9 (IC50: 0.002 μM). ZLMT-12 weakly inhibits AChE (IC50: 19.023 μM) and BuChE (IC50: 2.768 μM). ZLMT-12 has anti-proliferative activity and low cytotoxicity. ZLMT-12 blocks the cell cycle in S-phase and G2/M-phase and induces apoptosis.

GRGDSPC acetate (GRGDSPC acetate (91575-26-7 free base)) is a 7-amino acid peptide of thiolated cell adhesion.