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55

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2423	P7C3-A20	Others	Others
	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。
T2046	Nimorazole Nimorazol,Nitrimidazine,尼莫唑,K-1900,Naxogin,尼莫拉唑	Others; Antibiotic; Parasite	Microbiology/Virology; Others
	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。
T10459	Banoxantrone dihydrochloride AQ4N dihydrochloride,AZD1689 2HCl	NOS	Immunology/Inflammation
	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。
T67963	Teniloxazine
	Teniloxazine 是一种可口服的抗抑郁化合物，具有抗缺氧特性。
T0294	6α-Methylprednisolone 21-hemisuccinate sodium salt Asmacortone,Methylprodnisolone Sodium Succinate,甲强龙琥珀酸钠,Metypresol,Methylprednisolone sodium succinate,Corticel,6-Methylprednisolone succinate sodium	Glucocorticoid Receptor; Glucagon Receptor	Endocrinology/Hormones; GPCR/G Protein
	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。
T11244	Etimizol Ethymisol,Ethimizole,Ethymisole	Others	Others
	Etimizol (Ethimizole) 对缺氧造成的失忆症有效果。
T28607	Rocepafant LAU 8080,LAU8080,BN 50730,LAU-8080,BN50730,BN-50730	Platelet aggregation	Others
	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。
T2020	RGW 611	Others	Others
	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。
TQ0121	VH-298	Others; HIF; Ligand for E3 Ligase	Angiogenesis; Chromatin/Epigenetic; Others; PROTAC
	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。
T3615	Evofosfamide 艾伏磷酰胺,TH-302	Apoptosis; Others	Apoptosis; Others
	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。
T67291	2′,2′-Difluorodeoxyuridine dFdU,2',2'-Difluoro-2'-deoxyuridine	Drug Metabolite	Metabolism
	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。
T4434	Tirapazamine Tirazone,Win59075,SR4233,替拉扎明,SR259075	Others	Others
	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。
T16537	Pimonidazole	Others	Others
	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。
T16536	Pimonidazole hydrochloride
	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。
TP1886L1	NoxA1ds acetate(1435893-78-9 free base)	NADPH-oxidase	Immunology/Inflammation
	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。
T21270	Isometronidazole R.P. 8979,Isometronidazole, Izoklion
	Isometronidazole is a hypoxic cell sensitizer.
T32396	Kih 202 Khi 202,Kih-202
	Kih 202 have hypoxic cytotoxicity to FM3A cells from C3H mice.
T34334	RK 29 RK29,RK-29
	RK 29 has hypoxic cell sensitizer properties.
T34083	PK 130 PK130,PK-130
	PK 130, as a hypoxic cell radiosensitizer, is an L-phenylalanine methyl ester conjugate of 2-nitroimidazol.
T33700	NLP 1 NLP-1,NLP1,2-Nlp-3
	NLP 1 is a DNA intercalating hypoxic cell radiosensitizer and cytotoxin.
T33699	NLCQ-1 HCl NLCQ1,NLCQ-1, NLCQ 1,NSC 709257
	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
T28327	PD 130908 PD130908,PD-130908
	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
T26049	RB 6145 RB6145,RB-6145
	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。
T32427	KU-2285 KU 2285
	KU-2285 is a potent hypoxic cell radiosensitizer. At less than 100 mg/kg, KU-2285 sensitized SCCVII tumors more than MISO and SR-2508 by fractionated irradiation. KU-2285 entered clinical trials in late 1990s.
T21316	Apaziquone EO-9,NSC382459,EO9,NSC 382459,EO 9,NSC-382459
	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
T25943	Phenazoviridin
	Phenazoviridin 是一种新发现的微生物自由基清除剂，从链霉菌 HR04的培养基中分离得到。它是一种抗低氧化合物，对大鼠脑匀浆中的脂质过氧化具有较强的抑制活性，对小鼠具有抗缺氧活性。
T70813	DTP348
	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.
T68675	Porfiromycin
	Porfiromycin is a n N-methyl derivative of the antineoplastic antibiotic mitomycin C isolated from the bacterium Streptomyces ardus and other Streptomyces bacterial species. Bioreduced porfiromycin generates oxygen radicals and alkylates DNA, producing interstrand cross-links and single-strand breaks, thereby inhibiting DNA synthesis. Porfiromycin is preferentially toxic to hypoxic cells.
T35682	2-deoxy-2-fluoro-D-Glucose
	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.
T31566	Doranidazole PR-350,PR350,PR-000350,RP-343,PR000350
	Dornidazole (PR-000350, PR-350, RP-343, PR-69) is an effective radiosensitizer for hypoxic cells with the potential for the treatment of non-small cell lung cancer (NSCLC) and pancreatic cancer.
T34773	TAK-044 TAK044
	TAK-044 is an endotheliin receptor antagonist that prevents and reverses the development of carbon tetrachloride induced cirrhosis in rats. TAK-044 showed a protective effect on neuronal activity in vitro hypoxic glucose deprivation model of stroke.
T21318	Efaproxiral RSR13,Efaproxyn,RSR 13,RSR-13
	Efaproxiral is a synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity, increasing tumor
T61282	hCAI/II-IN-2
	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].
T61832	hCAI/II-IN-3
	hCAI/II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I/II enzymes. It exhibits Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. hCAI/II-IN-3 demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].
T75949	NoxA1ds TFA
	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.
T80963	TPEQM-DMA
	TPEQM-DMA为近红外二区光敏剂，能在癌性线粒体中积累，抑制癌细胞生长。其显著I型光疗效果，有助于克服光动力疗法(PDT)治疗低氧肿瘤的限制。
T69714	Etanidazole
	Etanidazole (SR-2508) is a 2-nitroimidazole drug with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
T38043	Resolvin E4
	Resolvin E4 (RvE4) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acid by 15-lipoxygenase (15-LO)via15(S)-HpEPE and 15S-hydroxy, 5S-HpEPE intermediatesin vitroand by isolated human M2 macrophages or polymorphonuclear (PMN) neutrophils under normoxic or hypoxic conditions. RvE4 synthesis is enhanced in M2 macrophage and neutrophil co-cultures, indicating transcellular biosynthesis by a potential 15-LO and 5-LO mechanism...
TP2046	TAT-cyclo-CLLFVY
	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
TP1886	NoxA1ds
	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
T37608	Riluzole-13C,15N2 Riluzole-13C,15N2
	Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals a...
T36408	Rhein-13C4 Rhein-13C4
	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 i...
T70860	Banoxantrone AQ4N
	Banoxantrone (AQ4N) 作为一种典型的缺氧选择性细胞毒素。Banoxantrone 可被还原为 AQ4，AQ4 是一种有效的拓扑异构酶 II 抑制剂。Banoxantrone 通过iNOS 依赖机制选择性地杀死缺氧细胞。Banoxantrone 显示出强大的细胞毒性和低氧选择性效应，且能被辐射增强。
T74800	HAT-SIL-TG-1&AT
	HAT-SIL-TG-1&AT 是一种 Janus 酪氨酸激酶 (JAK) 抑制剂，具有抗肿瘤作用。HAT-SIL-TG-1&AT 是缺氧激活的前药，可抑制肿瘤组织中的JAK-STAT 信号传导。HAT-SIL-TG-1&AT 在低氧条件下抑制 HEL 细胞增殖并下调磷酸化的STAT3/5。
T79748	hCAIX/XII-IN-7	Carbonic Anhydrase	Metabolism
	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。
T68273	BNC105P
	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, deprivi...
TP2046L	TAT-cyclo-CLLFVY acetate(1446322-66-2 Free base)
	TAT-cyclo-CLLFVY acetate(1446322-66-2 Free base) 是一种选择性 HIF-1 二聚化抑制剂。 TAT-cyclo-CLLFVY acetate 阻断重组 HIF-1α 与 HIF-1β 的蛋白质-蛋白质相互作用，但不阻断 HIF-2α 与 HIF-1β (IC50 = 1.3 μM)。 TAT-cyclo-CLLFVY acetate 在体外抑制缺氧诱导的 HIF-1 活性，并降低骨肉瘤和乳腺癌细胞中 VEGF 和 CAIX 的表达。 TAT-cyclo-CLLFVY acetate 减少缺氧 HUVEC 的管状化。
T71827	AG-205
	(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。
T36404	PRLX-93936
	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...
TP2214	Adrenomedullin (1-12), human	Others	Others
	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

化合物

Cat.No: T2423

Target: Others

Cat.No: T2046

Synonym: Nimorazol,Nitrimidazine,尼莫唑,K-1900,Naxogin,尼莫拉唑

Target: Others, Antibiotic, Parasite

Banoxantrone dihydrochloride

Cat.No: T10459

Synonym: AQ4N dihydrochloride,AZD1689 2HCl

Target: NOS

Cat.No: T67963

6α-Methylprednisolone 21-hemisuccinate sodium salt

Cat.No: T0294

Synonym: Asmacortone,Methylprodnisolone Sodium Succinate,甲强龙琥珀酸钠,Metypresol,Methylprednisolone sodium succinate,Corticel,6-Methylprednisolone succinate sodium

Target: Glucocorticoid Receptor, Glucagon Receptor

Cat.No: T11244

Synonym: Ethymisol,Ethimizole,Ethymisole

Target: Others

Cat.No: T28607

Synonym: LAU 8080,LAU8080,BN 50730,LAU-8080,BN50730,BN-50730

Target: Platelet aggregation

Cat.No: T2020

Target: Others

Cat.No: TQ0121

Target: Others, HIF, Ligand for E3 Ligase

Cat.No: T3615

Synonym: 艾伏磷酰胺,TH-302

Target: Apoptosis, Others

2′,2′-Difluorodeoxyuridine

Cat.No: T67291

Synonym: dFdU,2',2'-Difluoro-2'-deoxyuridine

Target: Drug Metabolite

Cat.No: T4434

Synonym: Tirazone,Win59075,SR4233,替拉扎明,SR259075

Target: Others

Cat.No: T16537

Target: Others

Pimonidazole hydrochloride

Cat.No: T16536

NoxA1ds acetate(1435893-78-9 free base)

Cat.No: TP1886L1

Target: NADPH-oxidase

Isometronidazole

Cat.No: T21270

Synonym: R.P. 8979,Isometronidazole, Izoklion

Cat.No: T32396

Synonym: Khi 202,Kih-202

Cat.No: T34334

Synonym: RK29,RK-29

Cat.No: T34083

Synonym: PK130,PK-130

Cat.No: T33700

Synonym: NLP-1,NLP1,2-Nlp-3

Cat.No: T33699

Synonym: NLCQ1,NLCQ-1, NLCQ 1,NSC 709257

Cat.No: T28327

Synonym: PD130908,PD-130908

Cat.No: T26049

Synonym: RB6145,RB-6145

Cat.No: T32427

Synonym: KU 2285

Cat.No: T21316

Synonym: EO-9,NSC382459,EO9,NSC 382459,EO 9,NSC-382459

Cat.No: T25943

Cat.No: T70813

Cat.No: T68675

2-deoxy-2-fluoro-D-Glucose

Cat.No: T35682

Cat.No: T31566

Synonym: PR-350,PR350,PR-000350,RP-343,PR000350

Cat.No: T34773

Synonym: TAK044

Cat.No: T21318

Synonym: RSR13,Efaproxyn,RSR 13,RSR-13

Cat.No: T61282

Cat.No: T61832

Cat.No: T75949

Cat.No: T80963

Cat.No: T69714

Cat.No: T38043

TAT-cyclo-CLLFVY

Cat.No: TP2046

Cat.No: TP1886

Riluzole-13C,15N2

Cat.No: T37608

Synonym: Riluzole-13C,15N2

Cat.No: T36408

Synonym: Rhein-13C4

Cat.No: T70860

Synonym: AQ4N

HAT-SIL-TG-1&AT

Cat.No: T74800

Cat.No: T79748

Target: Carbonic Anhydrase

Cat.No: T68273

TAT-cyclo-CLLFVY acetate(1446322-66-2 Free base)

Cat.No: TP2046L

Cat.No: T71827

Cat.No: T36404

Adrenomedullin (1-12), human

Cat.No: TP2214

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN1916	Matairesinol 罗汉松树脂酚	ATPase; p38 MAPK; ROS	Immunology/Inflammation; MAPK; Membrane transporter/Ion channel
	Matairesinol has radical and superoxide scavenging activities,; it also has anti-angiogenic activity by suppressing mROS signaling , can decrease hypoxia-inducible factor-1α± in hypoxic HeLa cells.
T21494	Oligomycin	HIF	Angiogenesis; Chromatin/Epigenetic
	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。
T5773	Moslosooflavone 5-羟基-7,8-二甲氧基黄酮,5-hydroxy-7,8-dimethoxyflavone	NF-κB; Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	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。
T2S0843	Negletein 黄芩素-7-甲醚,7-O-Methylbaicalein,Baicalein-7-methylether	IL Receptor; TNF; NOS; Interleukin	Apoptosis; Immunology/Inflammation
	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。
T36749	Herboxidiene
	Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...

天然产物

Cat.No: TN1916

Synonym: 罗汉松树脂酚

Target: ATPase, p38 MAPK, ROS

Cat.No: T21494

Target: HIF

Moslosooflavone

Cat.No: T5773

Synonym: 5-羟基-7,8-二甲氧基黄酮,5-hydroxy-7,8-dimethoxyflavone

Target: NF-κB, Reactive Oxygen Species

Cat.No: T2S0843

Synonym: 黄芩素-7-甲醚,7-O-Methylbaicalein,Baicalein-7-methylether

Target: IL Receptor, TNF, NOS, Interleukin

Cat.No: T36749

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上海市静安区江场三路238号8楼