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36

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T11561 HIF-2α-IN-2

HIF/HIF Prolyl-Hydroxylase; HIF Angiogenesis; Chromatin/Epigenetic; Metabolism
HIF-2α-IN-2 是低氧诱导因子抑制剂,IC50=16 nM。
T67831 HIF-2α agonist 2

HIF/HIF Prolyl-Hydroxylase; HIF Angiogenesis; Chromatin/Epigenetic; Metabolism
HIF-2α agonist 2 是一种 HIF-2α 激动剂,对HIF-2α的EC50 值为 1.68 μM。HIF-2α agonist 2可以促进HIF-2a-ARNT 复合物3z 结构中ARNT A/B 环的稳定性, 对 786-O-HRE-Luc 细胞无细胞毒性。HIF-2α agonist 2可用于氧代谢研究,与癌症的发生密切相关。
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。
T64336 Izilendustat

HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism
tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate 是一种脯氨酰羟化酶抑制剂。
T3289 Amifostine

氨磷汀,Ethyol,WR2721,Gammaphos

Others; HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism; Others
Amifostine (Ethyol) 是一种广谱细胞保护剂和辐射防护剂,具有清除自由基的作用。它可选择性保护正常组织免受放射线和化学疗法造成的损害。它是有效的 HIF-α1和 p53诱导剂,可降低肾脏毒性并具有抗血管生成作用。
T61349 HIF-1α-IN-2

HIF Angiogenesis; Chromatin/Epigenetic
HIF-1α-IN-2 是一种新型高效的 HIF-1α 抑制剂,具有抗癌抗肿瘤活性,以剂量依赖的方式抑制 HIF-1α 和 VEGF 的表达,抑制细胞迁移。
T6381 Amifostine trihydrate

Ethyol trihydrate,WR2721,三水氨磷汀,Amifostine

Others; HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism; Others
Amifostine trihydrate (WR2721) 是一种广谱细胞保护剂和辐射防护剂。它可选择性保护正常组织免受放射线和化学疗法造成的损害。它是有效的HIF-α1和p53诱导剂。它通过清除氧衍生的自由基来保护细胞免受损伤。它可降低肾脏毒性并具有抗血管生成作用。
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。
T1101 Minocycline hydrochloride

Minocycline HCl,盐酸米诺环素,美满霉素

HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic Chromatin/Epigenetic; Metabolism; Microbiology/Virology
Minocycline hydrochloride (Minocycline HCl) 是四环素抗生素,具有出色的吸收和组织渗透性,可用于多种细菌感染以及痤疮的治疗。米诺环素可导致在开始治疗后 1 至 3 个月内发生的急性肝炎样综合征或通常在长期治疗后具有自身免疫特征的更隐匿的慢性肝炎。
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].
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。
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。
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]
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。
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。
T61367 HIF-2α-IN-6

HIF-2α-IN-6 (117) 是HIF-2α的抑制剂。
T61822 M1002

HIF Angiogenesis; Chromatin/Epigenetic
M1002 是一种缺氧诱导因子-2 (HIF-2) 激动剂,可以增强HIF-2alpha和ARNT对转录激活的亲和力 。M1002能够改变HIF-281alpha PAS-B结构域的Tyr2构象, 与脯氨酰羟化酶结构域 (PHD) 抑制剂可发挥协同作用。
T12675L PT2399

HIF/HIF Prolyl-Hydroxylase; HIF Angiogenesis; Chromatin/Epigenetic; Metabolism
PT2399 是高选择性的HIF-2α拮抗剂,能直接结合 HIF-2α PAS B 结构域,IC50=6 nM,具有显著的体内抗肿瘤特性。
T22022 Adaptaquin

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。
T3180 JNJ-42041935

HIF-PHD Inhibitor II

HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism
JNJ-42041935 (HIF-PHD Inhibitor II) 是一种高效的,竞争性的、选择性的脯氨酰羟化酶PHD 抑制剂,抑制PHD1(pKi= 7.91±0.04),PHD2 (pKi= 7.29 ±0.05) 和 PHD3 (pKi= 7.65±0.09)。
T6961 PX-478

PX-478 2HCl

HIF/HIF Prolyl-Hydroxylase; HIF; Autophagy Angiogenesis; Autophagy; Chromatin/Epigenetic; Metabolism
PX-478 是一种 HIF-1α 抑制剂,具有选择性、口服活性和血脑屏障渗透性。PX-478 具有抗肿瘤活性,还可以保护糖尿病中的胰腺 β 细胞功能,用于 2 型糖尿病的研究。
T67836 AT-533

HSP; HSV Cytoskeletal Signaling; Metabolism; Microbiology/Virology
AT-533 是有效的 HSV 和 Hsp90 抑制剂。AT-533 可以阻断 HIF-1α/VEGF/VEGFR-2 信号通路,从而抑制血管生成和肿瘤生长。AT-533 也抑制下游通路的激活,包括 Erk1/2, FAK, Akt/mTOR/p70S6K。AT-533 抑制人脐静脉内皮细胞 (HUVEC) 的细胞迁移、侵袭和管形成。
T2445 FG-2216

YM-311,FG2216,FG 2216

HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism
FG-2216 (YM-311) 是一种有效的、口服具有活力的HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂,IC50=3.9 nM。它在体内能够诱导促红细胞生成素生成和胎儿血红蛋白的表达。
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。
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。
T27796 Langkamide

Langkamide is a HIF-2 inhibitor with EC₅₀ values of 14.0 uM.
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。
T63035 Izilendustat hydrochloride

Izilendustat (hydrochloride) 是一种脯氨酰羟化酶 (prolyl hydroxylase) 的有效抑制剂,能够稳定缺氧诱导因子-1 α (HIF-1α) 和缺氧诱导因子-2 (HIF-2)。Izilendustat (hydrochloride) 具有潜力进行 HIF-1α 相关疾病的研究(包括外周血管疾病(PVD)、心力衰竭、冠状动脉疾病(CAD)、缺血、贫血、结肠炎和其他炎症性肠病)。
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。
T15234 ENMD-1198

IRC 110160,ENMD-119,ENMD 1198

HIF; STAT Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
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。
T60539 KG-548

KG-548 是一种ARNT/TACC3干扰剂以及HIF-1α抑制剂。KG-548 通过 ARNT 的 PAS-B 结构域与 TACC3 竞争性结合,直接干扰ARNT/TACC3复合物的形成。ARNT 是芳基烃受体核转运蛋白,也称为 HIF-β。
T69966 Roxadustat-d5

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and ...
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。

化合物

HIF-2α-IN-2
Cat.No: T11561
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, HIF
HIF-2α agonist 2
Cat.No: T67831
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, HIF
IOX2
Cat.No: T1823
Synonym: IOX 2,JICL38
Target: HIF/HIF Prolyl-Hydroxylase
Izilendustat
Cat.No: T64336
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase
Amifostine
Cat.No: T3289
Synonym: 氨磷汀,Ethyol,WR2721,Gammaphos
Target: Others, HIF/HIF Prolyl-Hydroxylase
HIF-1α-IN-2
Cat.No: T61349
Synonym:
Target: HIF
Amifostine trihydrate
Cat.No: T6381
Synonym: Ethyol trihydrate,WR2721,三水氨磷汀,Amifostine
Target: Others, HIF/HIF Prolyl-Hydroxylase
HIF-2α-IN-1
Cat.No: T15482
Synonym:
Target: HIF
Minocycline hydrochloride
Cat.No: T1101
Synonym: Minocycline HCl,盐酸米诺环素,美满霉素
Target: HIF/HIF Prolyl-Hydroxylase, Antibacterial, Antibiotic
HIF-PHD-IN-2
Cat.No: T61458
Synonym:
Target:
HIF-2α-IN-7
Cat.No: T72997
Synonym:
Target:
HIF-1α-IN-2 hydrochloride
Cat.No: T78123
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase
HIF-1/2α-IN-2
Cat.No: T61102
Synonym:
Target:
HIF-2α-IN-9
Cat.No: T78937
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase
HIF-2α-IN-5
Cat.No: T61614
Synonym:
Target:
HIF-2α-IN-6
Cat.No: T61367
Synonym:
Target:
M1002
Cat.No: T61822
Synonym:
Target: HIF
PT2399
Cat.No: T12675L
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, HIF
Adaptaquin
Cat.No: T22022
Synonym:
Target: HIF
MK-8617
Cat.No: T4106
Synonym: MK8617
Target: HIF/HIF Prolyl-Hydroxylase
JNJ-42041935
Cat.No: T3180
Synonym: HIF-PHD Inhibitor II
Target: HIF/HIF Prolyl-Hydroxylase
PX-478
Cat.No: T6961
Synonym: PX-478 2HCl
Target: HIF/HIF Prolyl-Hydroxylase, HIF, Autophagy
AT-533
Cat.No: T67836
Synonym:
Target: HSP, HSV
FG-2216
Cat.No: T2445
Synonym: YM-311,FG2216,FG 2216
Target: HIF/HIF Prolyl-Hydroxylase
PX-12
Cat.No: T2283
Synonym: 2-[(1-甲基丙基)二硫代]-1H-咪唑,IV-2,PX12
Target: Thioredoxin
HIF-1α-IN-6
Cat.No: T82198
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase
Langkamide
Cat.No: T27796
Synonym:
Target:
PHD2-IN-1
Cat.No: T79241
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase
Izilendustat hydrochloride
Cat.No: T63035
Synonym:
Target:
1-Palmitoyl-2-oleoyl-sn-glycerol
Cat.No: T74027
Synonym:
Target:
ENMD-1198
Cat.No: T15234
Synonym: IRC 110160,ENMD-119,ENMD 1198
Target: HIF, STAT
Zifcasiran
Cat.No: T74597
Synonym:
Target:
KG-548
Cat.No: T60539
Synonym:
Target:
Roxadustat-d5
Cat.No: T69966
Synonym:
Target:
CMC2.24
Cat.No: T36492
Synonym:
Target:
22-(4′-py)-JA
Cat.No: T79560
Synonym: 22-(4′-Pyridinecarbonyl) jorunnamycin A
Target: Akt
Cat. No. Product Name Target Signaling Pathways
T2941 Glucosamine hydrochloride

Chitosamine hydrochloride,盐酸氨基葡萄糖,2-Amino-2-deoxy-glucose HCl,Chitosamine HCl,D-(+)-Glucosamine hydrochloride

Reactive Oxygen Species; HIF/HIF Prolyl-Hydroxylase; Endogenous Metabolite; Autophagy Autophagy; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; NF-κB
Glucosamine hydrochloride (Chitosamine hydrochloride) 是软骨基质和滑液中糖胺聚糖的天然成分,常用作骨关节炎的治疗方法。它也是一种氨基糖,是糖基化蛋白和脂质生化合成的突出前体,用作膳食补充剂。
T5740 25(R,S)-Ruscogenin

(25RS)鲁斯可皂苷元,(25RS)-Ruscogenin

Others; HIF Angiogenesis; Chromatin/Epigenetic; Others
25(R,S)-Ruscogenin 能够调节 PI3K/Akt/mTOR 信号通路,抑制 MMP-2、MMP-9、uPA、VEGF 和 HIF-1α 的表达,阻碍肝癌转移。 它能够抑制 TLR4信号通路,减轻 LPS 诱导的肺内皮细胞凋亡。
TL0001 dencichine

L-Dencichin,ODAP,Dencichin,三七素

Others; HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism; Others
Dencichine (ODAP) 是抑制从三七中分到的非蛋白氨基酸,可抑制 HIF-prolyl hydroxylase-2 的活性。
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。
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

Glucosamine hydrochloride
Cat.No: T2941
Synonym: Chitosamine hydrochloride,盐酸氨基葡萄糖,2-Amino-2-deoxy-glucose HCl,Chitosamine HCl,D-(+)-Glucosamine hydrochloride
Target: Reactive Oxygen Species, HIF/HIF Prolyl-Hydroxylase, Endogenous Metabolite, Autophagy
25(R,S)-Ruscogenin
Cat.No: T5740
Synonym: (25RS)鲁斯可皂苷元,(25RS)-Ruscogenin
Target: Others, HIF
dencichine
Cat.No: TL0001
Synonym: L-Dencichin,ODAP,Dencichin,三七素
Target: Others, HIF/HIF Prolyl-Hydroxylase
Fraxinellone
Cat.No: T6S0071
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, STAT, PD-1/PD-L1
Cinnamaldehyde
Cat.No: T4S1551
Synonym: Cinnamic Aldehyde,肉桂醛
Target: HIF
β,β-Dimethylacrylshikonin
Cat.No: T3S2344
Synonym: β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin
Target: ERK, HIF/HIF Prolyl-Hydroxylase
Herboxidiene
Cat.No: T36749
Synonym:
Target:
TargetMol Loading
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