45
12
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
T39040 |
HIF-PHD-IN-1
|
||
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. | |||
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]. | |||
T61102 |
HIF-1/2α-IN-2
|
||
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] | |||
T7836 |
ML228
|
HIF | Angiogenesis; Chromatin/Epigenetic |
ML228 是一种有效的 HIF 信号通路激活剂,EC50 为 1 μM。ML228 可激活 HIF 以及下游 EGFR。 | |||
T75098 |
HIF-PHD-IN-3
|
Reactive Oxygen Species | Immunology/Inflammation; Metabolism; NF-κB |
HIF-PHD-IN-3 是一种有效的 hiPSC-CM 心脏保护支架,对 HIF-PHD 有潜在的抑制作用,可调节血红素加氧酶-1,可用于研究贫血。 | |||
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。 | |||
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。 | |||
T8973 |
HS-1793
|
Others | Others |
HS-1793 是 resveratrol 类似物,可以诱导细胞凋亡,在多种癌细胞中有抗肿瘤的能力。 | |||
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。 | |||
T0153 |
Oltipraz
吡噻硫酮,NSC 347901,RP 35972 |
HIF/HIF Prolyl-Hydroxylase; HIV Protease; Reverse Transcriptase; Nrf2; HIF | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome |
Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活,IC50为 10 μM,浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。 | |||
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。 | |||
T61367 |
HIF-2α-IN-6
|
||
HIF-2α-IN-6 (117) 是HIF-2α的抑制剂。 | |||
T61614 |
HIF-2α-IN-5
|
||
HIF-2α-IN-5 是一种有效的 HIF-2α的抑制剂,IC50小于 50 nM。 | |||
T27866 |
LXY6090
LXY 6090,LXY-6090 |
||
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 | |||
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。 | |||
T82198 | HIF-1α-IN-6 | 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。 | |||
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 | |||
T61161 |
HIF-1α-IN-3
|
||
HIF-1α-IN-3, also known as Compound (S)-3f, is a hypoxia-selective inhibitor of HIF-1α. It exhibits potent antiestrogenic activity [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。 | |||
TP1546 |
HIF-1 alpha (556-574) TFA (1201633-99-9 free base)
HIF-1 alpha (556-574) TFA |
||
This is a hypoxia-inducible factor-1 (HIF-1 a) 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1 subunit is stabilized in response to a lack of oxygen. This part | |||
T68324 |
KCN1
|
||
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... | |||
T60532 | HIF-1α-IN-5 | ||
HIF-1α-IN-5 是 HIF-1α的抑制剂,在 HEK293T 细胞中的 IC50值为 24 nM,也可抑制 MAO-A 的活性。 在缺氧条件下, HIF-1α-IN-5可下调 VEGF 和 PDK1 mRNA 的表达。HIF-1α-IN-5 具有用于癌症研究的潜力。 | |||
T74027 | 1-Palmitoyl-2-oleoyl-sn-glycerol | ||
1-Palmitoyl-2-oleoyl-sn-glycerol是HIF (藻殖段诱导因子)-1中的主要二酰基甘油,属于内源性代谢产物。 | |||
TP1533 |
HIF-1 alpha (556-574)
HIF-1 alpha 556-574 |
||
HIF-1 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1subunit is stabilized in response to a lack of oxygen. Thi | |||
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。 | |||
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。 | |||
T70903 |
KRH102053
|
||
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。 | |||
T74530 |
GEM-5
|
||
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。 | |||
T61458 |
HIF-PHD-IN-2
|
||
HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor, displaying IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1]. | |||
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。 | |||
T79969 |
Axl-IN-16
|
TAM Receptor | Tyrosine Kinase/Adaptors |
Axl-IN-16为Axl与HIF的双效抑制剂,能激发Flammulina velutipes子实体生成,并抑制HIF活性与受体酪氨酸激酶的表达。 | |||
T74597 |
Zifcasiran
|
||
Zifcasiran为缺氧诱导因子(HIF)合成抑制剂,显示抗肿瘤活性,适用于晚期肾细胞癌研究。 | |||
T74217 | Angiogenesis agent 1 | HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
Angiogenesis agent 1 (compound C-31) 为红景天苷衍生的糖苷类似物,能激活 HIF-1α 通路。该化合物有助于研究糖尿病所致后肢缺血。 | |||
T72997 |
HIF-2α-IN-7
|
||
HIF-2α-IN-7 是一种缺氧诱导因子 2α(HIF-2α)抑制剂。HIF-2α-IN-7 抑制 HIF-2α,EC50值为 6 nM。HIF-2α-IN-7 可用于多种疾病的研究,包括癌症、肝病、炎性疾病、肺病和铁负荷紊乱。 | |||
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... | |||
T68511 |
KRH102140
|
||
KRH102140 is a potent activator of PHD2. KRH102140, which has a structure similar to KRH102053. KRH102140 more efficiently suppressed HIF-1α than KRH102053 in human osteosarcoma cells under hypoxia. Furthermore, KRH102140 decreased the mRNA levels of HIF-regulated downstream target genes associated with angiogenesis and energy metabolism such as vascular endothelial growth factor, adrenomedullin, Glut1, aldolase A, enolase 1 and monocarboxylate transporter 4. KRH102140 also inhibited tube format... | |||
T78834 |
HIV-IN-7
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
Axl-IN-16(Compound 4)为Axl抑制剂,能够抑制Axl表达及抑制HIF活性,并诱导金针菇子实体形成。Axl-IN-16可通过分离红血球菌与猴头菇的“子实体液(FL)”得到。 | |||
T18667 |
(S,R,S)-AHPC-C5-COOH
VH032-C5-COOH |
Others | Others |
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases[1]. | |||
T36492 | CMC2.24 | ||
CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1/2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis throug... | |||
T79560 |
22-(4′-py)-JA
22-(4′-Pyridinecarbonyl) jorunnamycin A |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
22-(4′-py)-JA是久那霉素A的半合成衍生物,源自泰国蓝海绵(Xestospongia sp.)。该化合物显示出抗转移活性,能抑制AKT/mTOR/p70S6K信号通路,并阻断人脐静脉内皮细胞(HUVEC)中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶(MMP-2和MMP-9)、缺氧诱导因子1α(HIF-1α)和血管内皮生长因子(VEGF)来发挥作用。此外,22-(4′-py)-JA对非小细胞肺癌(NSCLC)显示出显著的抗癌效果。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T5429 |
Theaflavin 3,3'-digallate
茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG |
Virus Protease; Antioxidant; HIV Protease; HSV | Microbiology/Virology; oxidation-reduction; Proteases/Proteasome |
Theaflavin 3,3'-digallate (8-Gingerol) 是一种寨卡病毒蛋白酶抑制剂,IC50为 2.3 μM。它直接与 ZIKVpro 结合并抑制 ZIKV 复制,可抑制 gp41 和 NS2B-3 蛋白酶的活性,并具有抗 HSV 和 HIV-1病毒活性。它是红茶中的主要多酚,有抗肿瘤作用。 | |||
T6429 |
Caffeic Acid Phenethyl Ester
Phenylethyl Caffeate,咖啡酸苯乙酯,CAPE |
Apoptosis; NF-κB | Apoptosis; NF-κB |
Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) 是咖啡酸的苯乙醇酯,是蜂巢蜂胶的生物活性成分。它抑制核转录因子 NF-kappa B 的激活,具有抗肿瘤、细胞保护和免疫调节活性。它抑制 PDGF 诱导的血管平滑肌细胞增殖。 | |||
T6S0071 |
Fraxinellone
|
HIF/HIF Prolyl-Hydroxylase; STAT; PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Metabolism; Stem Cells |
Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物,是PD-L1抑制剂,可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1,有用于癌症免疫的潜力。 | |||
T4S1551 |
Cinnamaldehyde
Cinnamic Aldehyde,肉桂醛 |
HIF | Angiogenesis; Chromatin/Epigenetic |
Cinnamaldehyde (Cinnamic Aldehyde) 具有解热作用。 它是镇静剂。它抑制MDA-MB-435S 细胞的侵袭能力与下调miR-27a 的表达有关。它诱导活性氧的产生,发挥血管扩张和抗癌作用。 它似乎是一种有希望的候选药物,可作为与 5-氟尿嘧啶 (5-FU) 和奥沙利铂 (OXA) 这两种用于 CRC 治疗的化疗药物联合治疗的辅助剂。其作用的可能机制可能涉及药物代谢基因的调节。 它在抑制黑色素瘤的发生和发展方面具有一定的作用,其作用机制可能表现为抑制VEGF 和HIF-α的表达,从而使血管模拟和黑色素瘤细胞新生血管的形成,促进肿瘤的生长。 | |||
T3S2344 |
β,β-Dimethylacrylshikonin
β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin |
ERK; HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; MAPK; Metabolism |
β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物,从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达,促进血管生成,具有抗肿瘤活性。 | |||
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。 | |||
TN1952 |
Moracin P
桑辛素 P,桑辛素P |
Others; ROS; HIF | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Others |
Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. | |||
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... | |||
T36439 |
Gramicidin A
|
Antibacterial; HIF; Parasite | Angiogenesis; Chromatin/Epigenetic; Microbiology/Virology |
Gramicidin A 是一种从从 B. brevis 分离出来的多肽类抗生素。Gramicidin A 是一种高度疏水的通道形成离子载体,在人工膜中形成一价阳离子可渗透的通道。Gramicidin A 诱导缺氧诱导因子 1α (HIF-1α) 的降解,并能降低人肾细胞癌小鼠异种移植模型的生长。Gramicidin A 具有抗菌、抗疟活性以及溶血活性。 | |||
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 | |||
TN1951 |
Moracin O
桑辛素 O,桑辛素O |
HIF | Angiogenesis; Chromatin/Epigenetic |
Moracin O shows significant neuroprotective, and analgesic activities, it also has a strong protective influence against doxorubicin-induced cardiomyopathy in H9c2 cells with the EC50 value of 4.5 ± 1.3 μM. Moracin O exhibits potent in vitro inhibitory ac |