hypoxic

Banoxantrone dihydrochloride (AQ4N dihydrochloride) is a novel hypoxic cytotoxin that selectively kills hypoxic cells through an iNOS-dependent mechanism.

Rocepafant (LAU8080) is a platelet-activating factor (PAF) antagonist that attenuates hypoxic-ischemic brain damage in neonatal rats.Rocepafant inhibits tumor necrosis factor-Afa-mediated cytotoxicity in mouse L929 tumor cells.

Teniloxazine is an orally available antidepressant compound with anti-hypoxic properties.

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.

Tirapazamine (Win59075) is a potent cytotoxic agent under hypoxic conditions, can induce apoptosis by inducing breaks in single and double-stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin.

VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.

RGW 611, a morpholine derivative, enhances radiation effects and induces cell death in hypoxic V79-379A cells.

Etimizol (Ethimizole) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). The positive effect of Etimizol on memory is related to its influence on the consolidation stage.

Pimonidazole hydrochloride accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after the reduction of its nitro group. It can be used for qualitative and quantitative assessment of tumor hypoxia. Pimonidazole hydrochloride is a novel hypoxia marker for the complementary study of tumor hypoxia and cell proliferation in tumors.

Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after the reduction of its nitro group. It can be used for qualitative and quantitative assessment of tumor hypoxia. Pimonidazole is a n

hCAIX XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2 M phase cell cycle arrest and increasing apoptosis.

Antiproliferative Agent-58 (compound 8nj) is an effective antiproliferative agent that exhibits activity under both normoxic and hypoxic conditions.

Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor that suppresses VEGF secretion in SiHa cells under hypoxic conditions without inducing cytotoxicity (IC50=0.68 μM). It modulates the PI3K AKT mTOR and MAPK signaling pathways in tumor cells, thereby inhibiting the expression of HIF-1α and VEGF within tumor tissues.

iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.

Protoporphyrin IX disodium, as a radiation sensitizer, enhances the production of ROS and induces DNA damage even under hypoxic conditions. It also acts as a photosensitizer, undergoing direct degradation through photobleaching upon light exposure. This compound accumulates in rat tumor cells following administration of 5-aminolevulinic acid (5-ALA). When activated with a peak wavelength of 405 nm, Protoporphyrin IX disodium selectively improves basal cell carcinoma. It shows promise in pharmacological research of sonodynamic and photodynamic therapy for cancers such as bladder cancer and nodular basal cell carcinoma.

GP-515 HCl is an adenosine kinase inhibitor. In cultured rat myocardial myocytes (RMMs), GP-515 can induce the expression of vascular endothelial growth factor (VEGF). Under severe hypoxia (1% O(2)), GP-515 (20 microM) does not affect VEGF protein expression, but under mild hypoxic conditions, it increases VEGF expression by 27%.

BNC105P is a benzo[b]furan-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and anti-tumor effects. Upon administration, BNC105P, in its disodium phosphate form, rapidly converts to BNC105. In activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may block spindle formation, cause cell cycle arrest, and dismantle the tumor vasculature. This creates a hypoxic environment, depriving tumor cells of nutrients, leading to apoptosis. Apart from its VDA activity, BNC105P also exerts direct cytotoxic effects on tumor cells by inhibiting tubulin polymerization. Notably, BNC105 is not a substrate for the multidrug-resistant P-glycoprotein (Pgp) transporter.

Vincantril is a type of Vinca alkaloid compound known for its anti-hypoxic properties.

Nimorazole (Nimorazol) is a nitroimidazole anti-infective.

TBC-1 is a chlorophyll-a derivative that acts as a photosensitizer for photodynamic therapy (PDT). It efficiently generates type I ROS and targets the endoplasmic reticulum. TBC-1 demonstrates in vitro biocompatibility and PDT effectiveness under both normoxic and hypoxic conditions.

Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.

DOTA-NI-FAPI-04 is an FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention. Through DOTA chelation with metal isotopes (such as 68Ga and 177Lu), it forms radioactive probes ([68Ga]Ga DOTA-NI-FAPI-04 and [177Lu]Lu DOTA-NI-FAPI-04) useful for research in tumor diagnosis and therapeutics. This compound exhibits dual-targeting potential in cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly in scenarios involving the interaction between tumor stroma and hypoxic regions.

Isometronidazole (RO-07-1502) is a chemical compound. The chemical compound is a derivative of the nitroimidazole family. Its molecular formula is C6H9N3O3. Isometronidazole can actually be used in the treatment of radiation therapy. The compound is known as a hypoxic cell sensitizer (radiosensitizer), increasing the efficacy of radiation treatment. Isometronidazole (RO-07-1502), a nitroimidazole derivative with the molecular formula C6H9N3O3, acts as a hypoxic cell sensitizer (radiosensitizer) in radiation therapy, enhancing the efficacy of the treatment.

Apaziquone has potential antineoplastic and radiosensitization activities. It is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA