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.

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.

Butylhydroxyanisole (BHA) is an antioxidant consisting of a mixture of two isomeric organic compounds, 2-tert-butyl-4-hydroxyanisole and 3-tert-butyl-4-hydroxyanisole.

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 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.

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.

ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.

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.

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

Metsulfuron-methyl is a systemic selective wheat field high-efficiency sulfonylurea herbicide, which mainly controls most broadleaf weeds and grass weeds in wheat fields.

ML216 (CID-49852229) is a small molecule inhibitor of BLM helicase with an IC50 of 1.8 μM, demonstrating 28-fold selectivity against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s > 50 μM).

Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.

DCLK1-IN-1 is a selective, in vivo compatible chemical probe of the kinase domain of doublecortin-like kinase 1 (DCLK1) and a highly selective DCLK1/2 inhibitor with IC50 values ​​of 9.5/57.2 nM (DCLK1) and 31/103 nM (DCLK2) by binding and kinase assays, respectively. It has low toxicity and is used to study DCLK1 biology and determine its role in cancer.

UTL-5g (3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-) is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity. It lowers elevated levels of AST, ALT, creatinine, BUN, and TNF-α, increases the reduced platelet count in mice, and acts as a novel chemo- and radioprotective agent.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

Brusatol (NSC-172924) is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

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

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

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.

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.

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

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.