58
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36290 |
HIF-1 inhibitor-1
|
||
HIF-1 inhibitor-1 is an aryl carboxamide compound and a potent hypoxia-inducible factor 1 (HIF-1) inhibitor with an IC50 of 0.32 μM for the cancer metastasi[1]. [1]. Liu M, et al. Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis. J Med Chem. 2019 Oct 24;62(20):9299-9314. | |||
T67767 |
HIF-1 inhibitor-4
HIF-1 inhibitor-4 |
HIF | Angiogenesis; Chromatin/Epigenetic |
HIF-1 inhibitor-4 (HIF-1 inhibitor-4) 是一种 HIF-1 抑制剂 (IC50: 560 nM)。HIF-1 inhibitor-4 减少 HIF-1α 蛋白水平,但不影响 mRNA 水平。 | |||
T9627 |
PHD-1-IN-1
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
PHD-1-IN-1 是口服有效的缺氧诱导因子脯氨酰羟化酶结构域 1抑制剂,IC50为 0.034 μM。它与活性位 Fe2+具有独特的单齿结合相互作用,并诱导形成一个 “Arg367-out” 口袋。 | |||
T29797 |
AKB-6899
AKB6899 |
VEGFR; HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Chromatin/Epigenetic; Metabolism; Tyrosine Kinase/Adaptors |
AKB-6899 是脯氨酰羟化酶结构域 3 (PHD3) 的抑制剂,可增加 GM-CSF 处理的巨噬细胞产生的 VEGF 受体的可溶形式 (sVEGFR-1)。 AKB-6899 能稳定 HIF-2α,从而诱导肿瘤相关巨噬细胞产生 sVEGFR-1 并减少肿瘤生长。 | |||
T6823 |
E3330
|
HIF/HIF Prolyl-Hydroxylase; DNA/RNA Synthesis | Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism |
E3330 是一种口服有效的选择性 AP 内切核酸酶 1 (APE1; REF-1) 抑制剂,可抑制NF-κB DNA 结合活性。它阻断 TNF-α 诱导的肝癌细胞系中 IL-8 的激活,可以抑制癌细胞的生长和迁移,具有抗癌活性。 | |||
T71661 |
HIF-1α inhibitor-1
|
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HIF-1α inhibitor-1 is a HIF-1 alpha inhibitor. | |||
T71659 |
Indacaterol acetate
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Indacaterol acetate is an ultra-long-acting beta-adrenoceptor agonist. | |||
T74804 | HIF-1 inhibitor-5 | ||
HIF-1 inhibitor-5 (Compound 16e) 是一种有效的 HIF-1抑制剂,其 IC50为 2.38 μM。HIF-1 inhibitor-5 具有抗血管生成潜能。 | |||
T3494 |
LW6
HIF-1α inhibitor,CAY10585,LW8 |
Apoptosis; Dehydrogenase; HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Metabolism |
LW6 (HIF-1α inhibitor) 是一种新型 HIF-1抑制剂,IC50值为 4.4 μM。它降低 HIF-1α蛋白表达,但不影响 HIF-1β 表达。 | |||
T15482 |
HIF-2α-IN-1
|
HIF | Angiogenesis; Chromatin/Epigenetic |
HIF-2α-IN-1是一种有效的 HIF-2α 抑制剂, IC50值小于500 nM。 | |||
T60413 |
HIF-IN-1
|
HIF | Angiogenesis; Chromatin/Epigenetic |
HIF-IN-1 是一种有效的缺氧诱导因子 (HIF-1) 抑制剂,与肿瘤和癌细胞的增殖有关,对 HIF-1α 蛋白聚集有抑制作用。 | |||
T3169 |
KC7F2
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HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Chromatin/Epigenetic; Metabolism |
KC7F2 是缺氧诱导因子HIF-1通道抑制剂,在 LN229-HRE-AP 细胞中的IC50=20 μM,可用作抗癌试剂。 | |||
T13050 |
SYP-5
|
HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Chromatin/Epigenetic; Metabolism |
SYP-5 是新型HIF-1抑制剂,阻碍肿瘤细胞侵袭和血管生成。 | |||
T15396 |
GN44028
N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine |
HIF | Angiogenesis; Chromatin/Epigenetic |
GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) 是缺氧诱导因子(HIF)-1的有效抑制剂,其 IC50=14 nM。它可以抑制低氧诱导的 HIF-1α 的转录特性,但不抑制 HIF-1α mRNA 的表达,HIF-1α 蛋白的累积或HIF-1α/HIF-1β 的异缘二聚化。 | |||
T2488 |
BAY 87-2243
|
Ferroptosis; HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Metabolism |
BAY 87-2243 是一种选择性的低氧诱导因子-1 抑制剂。 | |||
T9890 |
HIF1-IN-3
Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]- |
HIF | Angiogenesis; Chromatin/Epigenetic |
HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) 是HIF-1的有效抑制剂(EC50 = 0.9 μM),可用于抗癌的研究。 | |||
T22022 |
Adaptaquin
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HIF | Angiogenesis; Chromatin/Epigenetic |
Adaptaquin 是缺氧诱导因子脯氨酰羟化酶(HIF-PH)的抑制剂。 | |||
T4106 |
MK-8617
MK8617 |
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂,对于PHD2的IC50=1 nM。 | |||
T36953 |
Naphthofluorescein
Naphthafluorescein |
HIF | Angiogenesis; Chromatin/Epigenetic |
Naphthofluorescein (Naphthafluorescein)是一种 Mint3 抑制剂,具有潜在的抗肿瘤和抗炎活性,抑制 HIF-1 和 Mint3 之间的相互作用,抑制 Mint3 依赖性 HIF-1 活性,抑制癌细胞和巨噬细胞的糖酵解活动,同时未显示出明显的体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针,可用于功能性切伦科夫成像。 | |||
T1823 |
IOX2
IOX 2,JICL38 |
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
IOX2 (IOX 2) 是特异性的脯氨酰羟化酶-2 抑制剂,IC50=22 nM。 | |||
T4381 |
Lificiguat
利非西呱,YC-1 |
Others; Guanylate cyclase; HIF | Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein; Others |
Lificiguat (YC-1) 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶激活剂和低氧诱导因子 1α 的抑制剂。 | |||
T2283 |
PX-12
2-[(1-甲基丙基)二硫代]-1H-咪唑,IV-2,PX12 |
Thioredoxin | Metabolism |
PX-12 (PX12) 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂,能够抑制 MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。 | |||
T61367 |
HIF-2α-IN-6
|
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HIF-2α-IN-6 (117) 是HIF-2α的抑制剂。 | |||
T6804 |
Chetomin
Chaetomin,NSC289491,BRN0077366 |
Apoptosis; HSP; HIF | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism |
Chetomin (BRN0077366) 是球毛壳菌的活性成分,是一种无毒的非小细胞肺癌干细胞靶向分子。它是一种热休克蛋白90/缺氧诱导因子1α 途径的抑制剂。 | |||
T61442 | HIF-1/2α-IN-1 | ||
HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1/2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1]. | |||
T23894 |
CLB-016
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CLB-016 is an inhibitor of hypoxia-inducible factor (HIF)-1. | |||
T27866 |
LXY6090
LXY 6090,LXY-6090 |
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LXY6090 is a HIF-1 inhibitor. LXY6090 inhibited the activity of HIF-1 and downregulated the protein level of HIF-1α in breast cancer cells. LXY6090 showed in vivo anticancer efficacy by decreasing the HIF-1α expression in nude mice bearing MX-1 tumor xeno | |||
T61614 |
HIF-2α-IN-5
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HIF-2α-IN-5 是一种有效的 HIF-2α的抑制剂,IC50小于 50 nM。 | |||
TP2046L |
TAT-cyclo-CLLFVY acetate(1446322-66-2 Free base)
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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。 | |||
T82595 |
DEALA-Hyp-YIPD
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DEALA-Hyp-YIPD为HIF-1α抑制剂,阻断VHL/HIF-1α相互作用,显示IC50值为0.91 μM,Kd为180 nM。 | |||
T61102 |
HIF-1/2α-IN-2
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HIF-1/2α-IN-2 is a potent inhibitor of HIF-1/2α, which effectively reduces the levels of HIF-1/2α. This compound elicits an iron starvation response by specifically targeting ISCA2, a key protein involved in Iron Sulfur Cluster Assembly 2. [1] | |||
T61161 |
HIF-1α-IN-3
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HIF-1α-IN-3, also known as Compound (S)-3f, is a hypoxia-selective inhibitor of HIF-1α. It exhibits potent antiestrogenic activity [1]. | |||
TP2046 |
TAT-cyclo-CLLFVY
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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 | |||
T79241 | PHD2-IN-1 | HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
PHD2-IN-1 为一种口服活性强效 HIF-脯氨酰羟化酶2 (PHD2) 抑制剂,具有 22.53 nM 的 IC50 值,适用于贫血病研究。 | |||
T15197 |
Echinomycin
Quinomycin A,NSC-13502 |
Others | Others |
Echinomycin is a cell-permeable hypoxia-inducible factor-1 (HIF-1) DNA-binding activity inhibitor. Echinomycin selectively inhibits the cancer stem cells (CSCs; IC50: 29.4 pM). | |||
T60398 |
Dimethyl-bisphenol A
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Dimethyl-bisphenol A (DMBPA) 是有效的HIF-1α抑制剂,通过从 HIF-1α 解离 Hsp90 促进 HIF-1α 蛋白的降解。Dimethyl-bisphenol A 可降低 Vegfa mRNA 的表达。 | |||
T64310 | KUSC-5001 | ||
KUSC-5001 是一种 HIF-1 的有效抑制剂 (IC50: 18 μM)。HIF-1 在肿瘤生存和恶性肿瘤中具有关键的作用。 | |||
T12547 | Prolyl Hydroxylase inhibitor 1 | Others | Others |
Prolyl Hydroxylase inhibitor 1 is an orally active inhibitor of hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) (IC50 of 62.23 nM). | |||
T82198 |
HIF-1α-IN-6
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HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
HIF-1α-IN-6 (compound 3s) 为HIF-1α抑制剂,MiaPaCa-2 和 MDA-MB-231 细胞中IC50分别为 0.6 nM 和 53.3 nM。它通过减少HIF-1α mRNA水平来抑制HIF-1α表达。 | |||
T36796 |
1,4-DPCA ethyl ester
|
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1,4-DPCA ethyl ester, the ethyl ester derivative of 1,4-DPCA, acts as an inhibitor of the enzyme factor inhibiting HIF (FIH)[1]. | |||
T61458 |
HIF-PHD-IN-2
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HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor, displaying IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1]. | |||
T60524 | HIF-1α-IN-4 | ||
HIF-1α-IN-4 是 HIF-1α抑制剂,在 HEK293T 细胞中的IC50值为 24 nM,具有潜在的抗肿瘤作用。 HIF-1α-IN-4 在缺氧条件下下调 VEGF 和 PDK1 mRNA 的表达。 | |||
T74530 |
GEM-5
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GEM-5为基于吉西他滨且含HIF-1α抑制剂(YC-1)的偶联物,IC50值为30 nM。此化合物能有效降低HIF-1α表达,并提高肿瘤抑制因子p53的表达量。GEM-5可诱导A2780细胞的凋亡(apoptosis),进而抑制肿瘤生长。 | |||
T75943 |
TAT-cyclo-CLLFVY TFA
|
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TAT-cyclo-CLLFVY TFA 是一种 HIF-1异二聚化的环肽抑制剂,可抑制癌细胞中的缺氧信号传导。TAT-cyclo-CLLFVY TFA 破坏 HIF-1α/HIF-1β蛋白相互作用,IC50为 1.3 μM。 | |||
T68324 |
KCN1
|
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KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the grow... | |||
T39040 |
HIF-PHD-IN-1
|
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HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising. | |||
T70903 |
KRH102053
|
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KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells. | |||
T78937 | HIF-2α-IN-9 | HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
HIF-2α-IN-9(compound 35r)为HIF-2α抑制剂,能够抑制VEGF-A(IC50=305 nM),影响肿瘤细胞生长基因表达并促进巨噬细胞介导的肿瘤免疫反应。 | |||
T79720 |
VHL-IN-1
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
VHL-IN-1 (compound 30) 为泛素 E3 连接酶 von Hippel-Lindau (VHL) 的抑制剂,其解离常数 Kd 为 37 nM,能够稳定并激活 HIF-1α 转录功能。此化合物具备作为 HIF-1α 稳定剂以及蛋白水解靶向嵌合体(PROTACs) 降解剂的应用潜力。 | |||
T78123 |
HIF-1α-IN-2 hydrochloride
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
HIF-1α-IN-2 hydrochloride 是一款有效的 HIF-1α 抑制剂,对抗癌活性显著,其在MDA-MB-231细胞和MiaPaCa-2细胞中的IC50值分别为28 nM和15 nM。该化合物主要通过抑制转录和阻碍蛋白质合成来下调HIF-1α的表达。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T1205 |
Chloramphenicol
Chlornitromycin,Levomycetin,Chloromycetin,氯霉素 |
ribosome; HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic | Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Chloramphenicol (Chloromycetin) 是一种广谱抗生素,有效抑制细菌蛋白质生物合成。它主要作用于细菌 70S 核糖体的 50S 亚基,对肽基转移酶有活性,抑制肽键的形成。 | |||
T3404 |
Cucurbitacin B
Cuc B,葫芦素B,DATISCACIN,葫芦素 B,Amarine |
Apoptosis; PTEN; Integrin; Endogenous Metabolite; HIF; STAT; Autophagy | Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
Cucurbitacin B (Cuc B) 是一具有抗癌活性的天然产物。 | |||
T75487 | 7-Hydroxyneolamellarin A | ||
7-Hydroxyneolamellarin A,一种从海绵Dendrilla nigra 提取的天然产物,是高效的缺氧诱导因子 1α (HIF-1α) 抑制剂。该化合物能够减弱HIF-1α蛋白的积累,并抑制血管表皮生长因子 (VEGF) 的转录活性,因而在癌症研究中有应用价值。 | |||
TN4489 | Manassantin A | ERK; cAMP; TNF; NF-κB; MAPK; COX; HIF; Prostaglandin Receptor; JNK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Stem Cells |
Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act |