cytotoxicit

VK3-OCH3 (2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na) is a selective antitumor agent via heme oxygenase (HO-1) related mechanisms; Vitamine K3 analogue.

ML346 is a novel activator of Hsp70.

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Uric acid is an important antioxidant that scavenges oxygen radicals and reactive oxygen species (such as singlet oxygen and peroxynitrite), inhibits lipid peroxidation, helps maintain stable blood pressure, and is the final product of purine metabolism. It is commonly used to induce hypertension models.

2-Fluoroadenine (NSC-27364) has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for anticancer studies.

Darunavir (TMC114) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

Tempo (2,2,6,6-Tetramethylpiperidinooxy) has a wide range of applications including use as a free radical scavenger, a reagent in organic synthesis and as a structural probe in electron spin resonance spectroscopy.

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.

sCNH240 (2-Fluoro-N-[3-(3-thienyl)-5-isoxazolyl]benzenesulfonamide) is a potential and selective Rv1625c/Cya activator with good cell permeability and oral activity, IC90=1.24 μM in cholesterol-supplemented 7H12 medium against Mycobacterium tuberculosis (Mtb) H37Rv strain, and inhibition of CYP2C19, CYP2C9 and hERG channels.

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

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

Isolongifolene ((-)-Isolongifolene), a tricyclic sesquiterpene isolated from Murraya koenigii, exhibits antioxidant, anti-inflammatory, anticancer, and neuroprotective properties. It mitigates Rotenone-induced oxidative stress, mitochondrial dysfunction, and apoptosis by modulating the PI3K/AKT/GSK-3β signaling pathways.

UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.

C 87 is a small-molecule TNF-α inhibitor. C 87 directly binds to TNFα, potently inhibits TNF-α-induced cytotoxicity (IC50 = 8.73 μM), and effectively blocks TNF-α-triggered signaling activities.

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7/DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

ES 936 is a potent and selective NQO1 inhibitor, inhibiting more than 95% of NQO1 activity within 30 minutes at a concentration of 100 nM, with a cell line-dependent inhibition duration resulting in a small number of DNA strand breaks.

(Z)-Semaxinib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. (Z)-Semaxinib is a quinolone derivative with potential antineoplastic activity.

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

MMAF (MonoMethyl auristatin F), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.

N-acetyltyramine is a metabolite of the biogenic amine tyramine . It enhances cytotoxicity of doxorubicin in resistant P388 murine leukemia cells with an IC50 value of 0.13 μg/ml compared with an IC50 value of 0.48 μg/ml for doxorubicin alone.