antitumor activities

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

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.

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Tiomolibdate diammonium (NSC-286644) is an inhibitor of superoxide dismutase 1 (SOD1) exerting antiangiogenic and antitumor activities. Tiomolibdate diammonium inhibits the activities of cuproenzymes, including SOD1 and COX.

Urolithin M5 (Decarboxyellagic acid) is a neuraminidase inhibitor isolated from olive leaves with antiviral and anticancer and antitumor activities. Urolithin M5 can be used to study influenza A virus infection and SARS-CoV-2 infection.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor. CRA-026440 hydrochloride exhibits Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM, respectively. CRA-026440 hydrochloride exhibits antitumor and antiangiogenic activities.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.

GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors.

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

DRF-1042, an orally active camptothecin analog, exhibits anticancer and insecticidal activities by inhibiting DNA topoisomerase I. It has been studied for its efficacy against solid tumors, including prostate and colon cancers.

CCT 031374 hydrobromide is a TCF β-catenin inhibitor with antitumor activities.

MKI-1 (MASTL Kinase Inhibitor-1) is an inhibitor of MASTL (microtubule-associated serine threonine kinase-like, IC50= 9.9 μM). MKI-1 exerts radiosensitizer and antitumor activities through PP2A activation in breast cancer.

Girinimbine (Girinimbin) is a carbazole alkaloid isolated from the plants M. koenigii, M. koenigii, and Murraya koenigii. Girinimbine exhibits a wide range of biological effects, including apoptosis, antitrypanosomal, antiplatelet, antimicrobial, anti-inflammatory, antioxidant, and antitumor activities.

Cepharanthine (NSC-623442) is a natural alkaloid that inhibits TNF-α-mediated NFκB stimulation, plasma membrane lipid peroxidation, and platelet aggregation, as well as cytokine production. Cepharanthine exhibits anti-inflammatory, antioxidant, and antitumor activities.

2-Methyl-4-nitroimidazole (2-MNI) is a heterocyclic compound with antimicrobial, anti-inflammatory, and antitumor activities.2-MNI has been used in a variety of fields including biochemistry, pharmacology, and biotechnology.

Cyclophosphamide hydrate is a DNA alkylating agent, an inhibitor of DNA synthesis. Cyclophosphamide hydrate has antitumor and immunosuppressive activities.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Catechin (Cianidanol) is a flavan-3-ol, a type of natural phenol and antioxidant.

Clioquinol (Iodochlorhydroxyquin) is an orally bioavailable, lipophilic, copper-binding, halogenated 8-hydroxyquinoline with antifungal, antiparasitic and potential antitumor activities.

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.