lethal

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.

Levosemotiadil(SA 3212) is a novel calcium antagonist and a very potent inhibitor of low-density lipoprotein oxidation.Levosemotiadil may be used to prevent lethal cardiac arrhythmias.

Benzyl benzoate (Benzoic acid benzyl ester) is one of the older preparations used for the therapy of scabies. Scabies is a skin infection caused by the Sarcoptes scabiei. Its symptoms are red spots, severe itching (particularly at night), and may lead to a secondary infection. Benzyl benzoate is useful in the therapy of scabies because it is lethal to this mite. It is also used for the therapy of lice affection of the body and head. Benzyl benzoate is not the therapy of choice for scabies because of its irritant properties.

(E)-Cinnamamide (trans-Cinnamamide) is the less active isomer of Cinnamamide which is an effective non-lethal chemical repellent suitable for reducing avian pest damage.

2'-Deoxycytidine hydrochloride is the hydrochloride form of 2'-Deoxycytidine, an important deoxyribonucleoside analog commonly used in DNA synthesis and potentially anticancer, and its derivative Gemcitabine has been developed as an anticancer drug.2'-Deoxycytidine 2'-Deoxycytidine hydrochloride protects mice from the lethal toxicity of cytosine arabinoside(araC).

1. Naringenin trimethyl ether (5,7,4'-Trimethoxyflavanone) shows significant molluscicidal activity with a median lethal concentration (LC(5)) of 3.9 μg/mL.

FGI-106 tetrahydrochloride demonstrates potent inhibitory activity across a broad spectrum of viruses, including those causing hemorrhagic fevers such as Ebola, Rift Valley, and Dengue Fever, with half-maximal effective concentrations (EC50s) of 100 nM, 800 nM, and 400-900 nM, respectively. Additionally, it effectively inhibits non-hemorrhagic fever viruses, notably HCV and HIV-1, with EC50s of 200 nM and 150 nM, respectively, indicating its broad-spectrum antiviral potential.

alpha-Amanitin (alpha-Amanitin) is the lethal toxin in Trichoderma viride and acts in vivo via the enterohepatic circulation and transport system. alpha-Amanitin induces cell death and can be used in the synthesis of ADCs. alpha-Amanitin has been shown to induce cell death and can be used in the synthesis of ADCs.

Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.

Compound 7l, an acaricide, serves as an effective LSD1 inhibitor. It demonstrates substantial acaricidal activity against the eggs of T. cinnabarinus, with a lethal concentration 50 (LC50) of 0.0035 mg L.

Debio-1452-NH3 is a novel and potent FabI antibody—enoyl-acyl carrier protein reductase inhibitor that demonstrates excellent efficacy in reducing bacterial load in mice. It effectively treats lethal infections caused by clinically isolated strains of Pseudomonas aeruginosa (Acinetobacter baumannii), Klebsiella pneumoniae, and Escherichia coli (E. coli).

H3B-616, as a powerful allosteric inhibitor of Carbamoyl phosphate synthetase 1 (CPS1) with an IC50 of 66 nM, targets CPS1, identified as a potential synthetic lethal target in LKB1-deficient non-small cell lung cancer. This overexpression of CPS1 facilitates pyrimidine synthesis in these cancer cells.

YH250 is a novel specific antagonist of the p300 catenin interaction that can stimulate hematopoiesis in mice exposed to lethal or sublethal doses of radiation.

PF-477736, also known as PF-00477736, is a potent CHK1 inhibitor with potential to enhance chemotherapy. This compound inhibits CHK1, an ATP-dependent serine threonine kinase that is a crucial component of the S G2 checkpoint system for DNA replication monitoring. By bypassing the final checkpoint defenses against DNA damage-induced lethal effects, PF-477736 may improve the antitumor efficacy of various chemotherapeutic agents in tumor cells with inherent checkpoint deficiencies.

WYFA-15 is an inhibitor of sphingomyelin synthase 1 (SMS1) that has been shown to protect mice from lethal SFTSV infection and reduce the replication and pathogenicity of SARS-CoV-2. WYFA-15 is applicable for antiviral research.

MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer properties, exhibiting lethal effects on Ehrlich ascites tumor cells both in vivo and in vitro. It disrupts the MRE11 nuclease-dependent double-strand break repair mechanism without impairing ATM activation. Additionally, MU147 damages the degradation of nascent strands at stalled replication forks and selectively affects BRCA2-deficient cells.

SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.

Alkaline tryptase-IN-1 (compound H-13) is an insecticide that targets alkaline trypsin-like enzymes. It has lethal concentration (LC50) values of 8.72, 13.77, 14.17, 12.96, and 12.35 μg mL against Schizaphis graminum, Sitobion avenae, Brevicoryne brassicae, Aphis gossypii, Aphis spiraecola, and Myzus persicae, respectively.

SDH-IN-23 (Compound B21) is an SDH inhibitor with exceptional nematicidal activity. It can suppress nematode feeding, reproduction, and embryonic development while also inducing lethal effects through mechanisms such as oxidative stress, intestinal damage, and SDH inhibition.

2,3-Dihydroxybutanoic acid is an anticancer agent extracted from the leaves of Corydalis plants. It exhibits anticancer activity both in vivo and in vitro and has a lethal effect on Ehrlich ascites tumor cells.

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

EGA inhibits the intoxication of lethal toxins and prevents the entry of a variety of other acid-dependent bacterial toxins and viruses into mammalian cells.EGA is a powerful tool for the study of membrane trafficking and can be used to treat infectious diseases.

Surfen dihydrochloride (Aminoquinuride dihydrochloride) is a potent small molecule antagonist of heparin sulfate with antibacterial and antiviral activity, and inhibits anthrax lethal factor, coagulation factor X, and lethal factor.Surfen inhibits the anticoagulant activity of both normal and low-molecular-weight heparin and inhibits heparin sulfation and heparin cleavage enzyme degradation.Surfen inhibits the blockade of FGF2 binding and signaling mediated by heparin acetylsulfate. Surfen inhibits the blockade of acetylheparin sulfate-mediated FGF2 binding and signaling.Surfen inhibits SEVI and semen-mediated enhancement of HIV type 1 infection.

J-104132 is a potetn and selective endothelin A B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova