toxicity

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

Methoprene (ZR-515) is a juvenile hormone (JH) mimic and a biological pesticide. Methoprene acts as an insect growth regulator interfering with the lifecycles of insects and preventing insects from reaching maturity or reproducing.

Sodium 2-mercaptoethanesulfonate (Uromitexan) is a sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from antineoplastic agents, such as ifosfamide or cyclophosphamide.

Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).

JNJ-5207852 dihydrochloride is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.

Dimethoate (L-395) is a systemic and contact insecticide for control of cattle grubs and certain other insect pests of farm animals.

Neuronotoxicity-IN-1 is a pyridothiazine derivative. Neuronotoxicity-IN-1 is an inhibitor of kainic acid neurotoxicity with neuroprotective activity[1].

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1 6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

Deferoxamine(Desferrioxamine B) is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Ensaculin (Anseculin), a novel benzopyrone partially substituted with piperazine, showed memory-enhancing effects in passive and conditioned avoidance paradigms in normal and artificially amnesic rodents. It showed neuroprotective activity in a model of NMDA toxicity and neurotrophic effects in primary cultured rat brain cells.Ensaculin can be used for the treatment of dementia.

NAMPT Activator-1 (compound 1) is an effective and specific activator of niacinamide phosphotransferase (Compound 1) with a wide range of EC50 (3.3-3.7 μM). NAMPT activator-1 effectively protects cultured cells from FK866-mediated toxicity and is a potential neuroprotective compound.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

Metacavir (PNA) is a novel nucleoside reverse transcriptase inhibitor, a deoxyguanosine analog, with anti-hepatitis B virus (HBV) activity and mitochondrial toxicity, which can be used to study HBV infection.

Phosphatase-IN-1 (compound II-8), a propranolol derivative, acts as an inhibitor of phosphatidate phosphatase (Pah). It binds to MoPah1 with an affinity constant of 19.8 μM, demonstrating growth inhibition of plant pathogens and anti-fungal properties, while exhibiting no toxicity towards rice seedlings and wheat heads [1].

Tubulin inhibitor 24 is a potent compound that inhibits tubulin polymerization.

Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT was effective in inhibiting viral replication in mice, displayed little toxicity.

PACMA 31 is an irreversible and covalent inhibitor of protein disulfide isomerase (PDI) with an IC50 of 10 μM. PACMA 31 significantly suppresses ovarian tumor growth and exhibits tumor targeting ability.

Mtb-IN-2 is a small molecule compound of Mycobacterium tuberculosis (Mtb) with antimicrobial activity and low toxicity that interferes with methionine metabolism processes and can be used to study tuberculosis.

BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.

FV-100 (Valnivudine HCl) is a potent, selective and orally active anti-vaxx-zoster agent.FV-100 is the API for CF-1743.FV-100 exhibits very low toxicity in vivo.FV-100 is a potent, selective and orally active anti-vaxx-zoster agent.FV-100 is the API for CF-1743.FV-100 exhibits very low toxicity in vivo.

(S)-Carvedilol is a non-selective β α-1 blocker.It exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.