cytotoxicity

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.

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.

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.

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.

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.

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.

(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).

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.

Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

L189 is a human DNA ligase inhibitor, inhibits hLigI/III/IV (IC50: 5/9/5 μM).

Lanosterol (3β-Hydroxy-8,24-lanostadiene) is a tetracyclic triterpenoid which is the compound from which all steroids are derived.

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

NU1025 (NSC-696807) is a potent PARP inhibitor with IC50 of 400 nM.