hypoxic

P7C3-A20 是促神经原性和神经保护活性的 P7C3 衍生物。它具有抗抑郁活性，能够透过血脑屏障，并可用于研究脑损伤。

Nimorazole (Nimorazol) 是一种 2-硝基咪唑，是一种低氧细胞辐射敏化剂。它具有抗感染，抗滴虫等原生动物的作用。它有头颈癌的研究潜力。

Teniloxazine 是一种可口服的抗抑郁化合物，具有抗缺氧特性。

Rocepafant (LAU8080) 是一种血小板活化因子(PAF)拮抗剂，可减轻新生大鼠缺氧缺血性脑损伤。Rocepafant 抑制肿瘤坏死因子-Afa 介导的小鼠 L929 肿瘤细胞的细胞毒性。

Banoxantrone dihydrochloride (AQ4N dihydrochloride) 是一种新型缺氧细胞毒素，通过 iNOS 依赖机制选择性地杀死缺氧细胞。

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone) 是一种糖皮质激素，是一种有效的抗炎剂，半衰期比 Prednisolone 长。

VH-298 是一种高效的 VHL:HIF-α 相互作用抑制剂(Kd:80-90 nM)。它可用于PROTAC 技术中。

Oligomycin 是一种抗真菌抗生素，是 H+-ATP 合成酶的抑制剂。Oligomycin 能够阻断氧化磷酸化和电子传递链。Oligomycin 对缺氧性肿瘤细胞 HIF-1alpha 表达具有抑制作用。

Tirapazamine (Win59075) 是抗癌剂，对实体瘤中的缺氧细胞具有选择性细胞毒性，促使 DNA 中的单链和双链断裂，碱基损伤和细胞死亡。

RGW 611 是一种能够增强辐射且诱导缺氧 V79-379A 细胞死亡的吗啉衍生物。

Pimonidazole hydrochloride 通过与大分子共价结合或在其硝基还原后形成还原性代谢物在缺氧细胞中积累。 可用于肿瘤缺氧的定性和定量评估。 它是一种新型的缺氧标志物，用于肿瘤缺氧和肿瘤细胞增殖的互补研究。

NoxA1ds acetate(1435893-78-9 free base) 是一种有效的选择性 NADPH 氧化酶 1 (NOX1) 抑制剂 (IC50 : 20 nM)。对 NOX1 的选择性优于对 NOX2、NOX4、NOX5 和黄嘌呤氧化酶的选择性。它抑制 HT-29 人结肠癌细胞中 NOX1 衍生的 O2 产生。在体外缺氧条件下减弱 VEGF 诱导的人肺动脉内皮细胞迁移。

Negletein (7-O-Methylbaicalein) 一种神经保护剂，可增强神经生长因子的作用并诱导 PC12 细胞中的神经突生长。它通过抑制TNF-α和IL-1β表现出抗炎活性，其 IC50值分别为 16.4 和 10.8 μM。它还具有抗菌、抗缺氧和抗阿尔茨海默病活性。

Etimizol (Ethimizole) 对缺氧造成的失忆症有效果。

Moslosooflavone (5-hydroxy-7,8-dimethoxyflavone) 是一种从雪莲中分离出来的类黄酮，具有抗缺氧和抗炎作用。

Evofosfamide (TH-302) 是一种缺氧激活前药，在缺氧 (N2) 和常氧 (21% O2) 环境下，IC50分别为 10 μM 和 1000 μM。

2′,2′-Difluorodeoxyuridine (dFdU) 是 Gemcitabine 的主要代谢产物。2′,2′-Difluorodeoxyuridine 具有抗癌和抗肿瘤活性，在低氧条件下的显示出放射增敏作用，可用于研究胰腺癌。

Pimonidazole 是缺氧标记物，能够与大分子的共价结合或被还原形成还原性代谢物后在缺氧细胞中积累，可用于定性和定量评估肿瘤缺氧。它可用于瘤内缺氧和细胞增殖的补充性研究。

iNOs-IN-5（Compound BN-4）作为一种iNOS抑制剂，其IC50值为0.1707 μM，能有效降低LPS (HT-D1056) 刺激下RAW264.7细胞中的NO表达。此外，iNOs-IN-5还能减少缺氧损伤激发的ROS与乳酸脱氢酶的表达，显示其抗坏死及抗凋亡的效果。在SD大鼠的脑缺血模型中，iNOs-IN-5展现了显著的神经保护和抗脑缺血性能，且能透过血脑屏障。

PK 130, as a hypoxic cell radiosensitizer, is an L-phenylalanine methyl ester conjugate of 2-nitroimidazol.

RK 29 has hypoxic cell sensitizer properties.

PD 130908 is an analogue of RSU 1069 with effective hypoxic cytotoxin, but less potent than RSU 1069. Toxicity toward hypoxic tumor cells in vivo is demonstrated by clamping tumors (for 60 min) following administration of PD 130908. Systemic toxicity is s

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg ml.4,5In vivo, 2-deoxy-D-glucose (500 mg kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

Protoporphyrin IX disodium 作为辐射敏化剂，在缺氧环境下能有效增强 ROS 的生成并诱导 DNA 损伤。作为光敏剂，该化合物在光照射下可经历光漂白反应直接降解。此外，Protoporphyrin IX disodium 能在大鼠肿瘤细胞中通过给药 5-aminolevulinic acid (5-ALA) 形成并积累。在 405 nm 波长的红色荧光激活下，它可有效改善基底细胞癌的病情。Protoporphyrin IX disodium 在声动力和光动力疗法中对治疗膀胱癌和结节性基底细胞癌具有研究潜力。

2-deoxy-2-fluoro-D-Glucose (2-FG) is a derivative of glucose with anticancer activity.1It inhibits the growth of 143B osteosarcoma cells grown under normoxic and hypoxic conditions when used at concentrations of 6 and 24 mM.

Potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50 = 20 nM). Exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. Inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. Attenuates VEGF-induced human pulmonary

BNC105P is a benzofuran-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and antineoplastic activities. Upon administration vascular disrupting agent BNC105P, the disodium phosphate ester of BNC105, is rapidly converted to BNC105; in activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may result in a blockage of mitotic spindle formation, cell cycle arrest, and disruption of the tumor vasculature. Hypoxic conditions ensue, depriving tumor cells of nutrients and resulting in tumor cell apoptosis. In addition to its VDA activity, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization. BNC105 is not a substrate for the multidrug-resistance P-glycoprotein (Pgp) transporter.

The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility to reduction by oxygen-depleted mitochondria. More recently, Cu-ATSM has been reported to improve locomotor function and survival in a transgenic ALS mouse model by delivering copper specifically to cells in the spinal cords of mice producing misfolded SOD1 proteins. Copper chaperone for SOD (CCS) is presumed to utilize the copper from Cu-ATSM to prevent misfolding of the SOD1 protein.

RB 6145是一种双功能硝基咪唑，低氧细胞放射增敏剂RSU 1069的前药，它的毒性较RSU 1069降低。它具有缺氧细胞优先细胞毒性和抗肿瘤治疗活性。

PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM. PRLX-93936 inhibits tumor growth in PANC-1 and HT-1080 xenograft models when administered at a dose of 50 mg/kg and induces tumor regression when administered at a dose of 100 mg/kg.

Adrenomedullin (AM) (1-12), human, is a peptide with the sequence Tyr-Arg-Gln-Ser-Met-Asn-Asn-Phe-Gln-Gly-Leu-Arg. Adrenomedullin (AM) (1-12), human, was initially identified as a vasodilator, and as such, it has the ability to relax vascular tone. Other

(rac)-AG-205 是一种对孕激素受体膜组分1 (Pgrmc1) 的有效抑制剂，并能诱导参与甾醇合成的基因表达，这些基因涉及 INSIG1 蛋白与 PGRMC1 形成复合物的过程。(rac)-AG-205 能够抑制 NF-kB 信号及 BDNF PI3K AKT 通路的活化，从而防止神经元对缺氧缺血状况的抵抗。

hCAIX XII-IN-7（compound 3e）为高效的hCA IX与XII抑制剂，对hCA I、II、IX与XII的Ki值分别为3.2 nM、9.2 nM、503.7 nM及59 nM，显示其在缺氧肿瘤研究中的应用潜力。

NoxA1ds TFA is a potent and selective inhibitor of NADPH oxidase 1 (NOX1), with an inhibition concentration (IC50) of 20 nM, demonstrating selectivity over NOX2, NOX4, NOX5, and xanthine oxidase. It effectively inhibits NOX1-derived O2- production in HT-29 human colon cancer cells and attenuates VEGF-induced migration of human pulmonary artery endothelial cells under hypoxic conditions in vitro.

Antiproliferative agent-34 (Compound A14) 是一种多激酶抑制剂，能有效抑制包括EGFRL858R T790M在内的特定EGFR基因变异形式，IC50为177 nM，对EGFRWT则为1567 nM。它还能抑制JAK2、ROS1、FLT3、FLT4和PDGFRα的活性，其IC50分别为30.93、106.90、108.00、226.60和42.53 nM。在正常氧气环境中，Antiproliferative agent-34对H1975和HCC827细胞株的抑制IC50值低于40 nM，而在低氧环境下，其抑制效能增强4至6倍，IC50值降至低于10 nM。

hCAIX XII-IN-13是一种针对人类碳酸酐酶 (hCA) IX和XII亚型的抑制剂，展现出高效的抑制效果，其Ki值分别达到0.08 µM 和 0.06 µM。此外，hCAIX XII-IN-13能在缺氧条件下增强Doxorubicin对MCF-7细胞的细胞毒作用，通过促进G2 M期的细胞周期阻滞和细胞凋亡 (apoptosis) 来发挥作用。

Kih 202 have hypoxic cytotoxicity to FM3A cells from C3H mice.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cance

Isometronidazole is a hypoxic cell sensitizer.

NLCQ-1 is a novel weak DNA-intercalative bioreductive compound. NLCQ-1 exhibited a C50 of 44 microM. NLCQ-1 demonstrated significant hypoxic selectivity in several rodent (V79, EMT6, SCCVII) or human (A549, OVCAR-3) tumor cell lines. Its potency as a hypo

hCAI II-IN-2 (compound 2b) is a highly effective dual inhibitor of human carbonic anhydrase I and II (hCA I II), with Ki values of 40.97 nM, 15.15 nM, and 61.88 nM for hCA I, hCA II, and hCA IX, respectively. With its anti-hypoxic properties, hCAI II-IN-2 demonstrates activity against acute mountain sickness (AMS). Furthermore, this compound exhibits low cellular activity [1].

DTP348 is an oral dual CAIX inhibitor radiosensitizer. DTP 348 is an oral dual drug with two mechanisms of action: (1). carbonic anhydrase IX inhibitor which acidifies the intracellular pH through the sulfamide components; (2). radio sensitizer of hypoxic cells through its 5-nitroimidazole moiety.

Antiproliferative agent-58 (compound 8nj) 在常氧与缺氧环境中均具显著抗增殖效果，表明其作为抗增殖剂的潜力。

Vincantril属于长春花生物碱类化合物，具有抗缺氧作用。

SR 4330是一种对缺氧细胞显示细胞毒性的化学药剂。其在小鼠与人类血浆中的最低定量限分别为40 ng mL和20 ng mL。

GP-515 HCl 是一种腺苷激酶抑制剂。在培养的大鼠心肌肌母细胞（RMMs）中，GP-515能够诱导血管内皮生长因子（VEGF）的表达。在严重缺氧（1% O(2)）条件下，GP-515（20 microM）对VEGF蛋白表达无影响，但在轻度缺氧环境中，可使VEGF表达增加27%。

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5