HIF

Inhibitory Selectivity

Catalog No.	Inhibitor Name	HIF	HIF1	Other
A15530	FG-2216	****	****
A15359	KC7F2	**	**
A11237	Roxadustat
A10012	2-Methoxyestradiol			Microtubule Associated
A14319	PX-478 2HCl
A12978	BAY 87-2243

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Oroxylin A

Catalog No. A14367
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Oroxylin A是一种O-甲基化的黄酮，具有多巴胺再摄取抑制剂的活性，并且是GABAA受体的苯二氮卓部位的负变构调节剂。了解更多

Product Citations (3)

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- Paramesha Bugga, .et al. Sirt3 ameliorates mitochondrial dysfunction and oxidative stress through regulating mitochondrial biogenesis and dynamics in cardiomyoblast, Cell Signal, 2022, Jun;94:110309 PMID: 35304284
- Bugga Paramesha, .et al. Sirt1 and Sirt3 Activation Improved Cardiac Function of Diabetic Rats via Modulation of Mitochondrial Function, Antioxidants (Basel), 2021, Feb 24;10(3):338 PMID: 33668369
- Mai Nagasaka, .et al. Anti-Tumorigenic Activity of Chrysin from Oroxylum indicum via Non-Genotoxic p53 Activation through the ATM-Chk2 Pathway, Molecules, 2018, Jun; 23(6): 1394 PMID: 29890668
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ML 228

Catalog No. A15360
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HIF activator

ML-228是HIF信号通路的激活剂，如HIF反应元件（HRE）报告基因分析，HIF-1α核易位分析和VEGF表达增加所证明。了解更多

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KC7F2

Catalog No. A15359
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HIF 抑制剂

KC7F2是HIF-1α蛋白翻译的抑制剂，但不是转录的抑制剂，可抑制蛋白质合成的两个关键调节子，即真核翻译起始因子4E结合蛋白1（4EBP1）和p70 S6激酶（S6K）的磷酸化。了解更多

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Chetomin

Catalog No. A15358
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HIF 抑制剂

Chetomin是Chaetomium spp的抗生素代谢产物。它对革兰氏阳性细菌具有抑菌作用。了解更多

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SYP-5

Catalog No. A13031
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HIF-1 inhibitor

SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis. 了解更多

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MK-8617

Catalog No. A12618
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pan HIF PHD1-3 inhibitor

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. 了解更多

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ZINC13466751

Catalog No. A12522
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HIF-1α/von Hippel-Lindau interaction inhibitor

ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M. 了解更多

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EL-102

Catalog No. A20925
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HIF1α inhibitor

EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability. 了解更多

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DMOG

Catalog No. A13998
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HIF-PH 抑制剂

DMOG是HIF-PH的细胞渗透性竞争性抑制剂。它可在正常的氧气张力下（0.1至1 mM的浓度）稳定HIF-1α表达。了解更多

Product Citations (1)

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- Hideaki Nakamura, .et al. Differentiated embryo chondrocyte plays a crucial role in DNA damage response via transcriptional regulation under hypoxic conditions, PLoS One, 2018, 13(2): e0192136 PMID: 29466367
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(Rac)-PT2399

Catalog No. A21376
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HIF-2α inhibitor

(Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM. 了解更多

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PT-2385

Catalog No. A21561
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HIF-2α inhibitor

PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM. 了解更多

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IOX 2

Catalog No. A11924
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HIF-PHD 抑制剂

IOX2是一种有效的HIF-1α脯氨酰羟化酶2（PHD2）抑制剂，在无细胞分析中的IC50为21 nM，选择性是JMJD2A，JMJD2C，JMJD2E，JMJD3或2OG加氧酶FIH的100倍以上。了解更多

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- Mun Chiang Chan, etc. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015; 10(7): e0132004.
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FG-4592 (Roxadustat)

Catalog No. A11237
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HIF-PHs 抑制剂

FG-4592 (Roxadustat)是一种用于CKD贫血的新型缺氧诱导因子脯氨酰羟化酶抑制剂。了解更多

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- Singh C, .et al. Serine and 1-carbon metabolism are required for HIF-mediated protection against retinopathy of prematurity, JCI Insight, 2019, Jul 25;4(14) PMID: 31341109
- Hideaki Nakamura, .et al. Differentiated embryo chondrocyte plays a crucial role in DNA damage response via transcriptional regulation under hypoxic conditions, PLoS One, 2018, 13(2): e0192136 PMID: 29466367
- Singh C, .et al. 3-Hydroxypyruvate Destabilizes Hypoxia Inducible Factor and Induces Angiostasis, Invest Ophthalmol Vis Sci, 2018, Jul 2;59(8):3440-3448 PMID: 30025089
- George Hoppe, .et al. Comparative systems pharmacology of HIF stabilization in the prevention of retinopathy of prematurity, Proc Natl Acad Sci U S A, 2016, May 3; 113(18): E2516–E2525 PMID: 27091985
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AFP464

Catalog No. A20978
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HIF-1?? inhibitor

AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator. 了解更多

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PT2977

Catalog No. A18465
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HIF-2alpha inhibitor

PT2977 is HIF-2alpha inhibitor with an IC50 of 9 nM. 了解更多

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Desidustat

Catalog No. A16921
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HIF hydroxylase 抑制剂

Desidustat是抗贫血药物的候选药物。它是从专利WO 2014102818 A1，化合物实施例2中提取的HIF羟化酶的抑制剂。了解更多

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IDF-11774

Catalog No. A16845
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HIF-1 抑制剂

IDF 11774是一种低氧诱导因子-1（HIF-1）抑制剂。它降低了HIFα-1的HRE荧光素酶活性；（IC50＝3.65 μM），并阻断HIF116结肠癌细胞缺氧下的HIFα-1的积累。了解更多

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Vadadustat

Catalog No. A16794
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HIF prolyl-hydroxylase 抑制剂

Vadadustat，也称为AKB-6548和PG-1016548，是一种有效的缺氧诱导因子脯氨酸双加氧酶抑制剂。了解更多

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LW6 (CAY10585)

Catalog No. A12882
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HIF-1 抑制剂

LW6是新型HIF-1抑制剂，IC50为4.4 uM。了解更多

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HIF-2a Translation Inhibitor

Catalog No. A16181
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HIF-2a translation 抑制剂

HIF-2a Translation Inhibitor（IC50值为5 uM）；独立于HIF-2a mRNA表达或HIF-2a蛋白稳定性，并独立于mTOR活性，降低常氧和低氧状态下HIF-2a蛋白和HIF-2a目标基因的表达。此外，翻译抑制剂76增强了IRP1与HIF-2a IRE（铁反应元件）的结合。了解更多

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DASA-58

Catalog No. A15895
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PKM2 Activator

DASA-58是一种有效的丙酮酸激酶M2（PKM2）活化剂。其中AC90和AC50分别为680 nM，38 nM。了解更多

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GSK1278863 (Daprodustat)

Catalog No. A12671
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HIF-prolyl hydroxylase 抑制剂

GSK1278863是新型的HIF-脯氨酰羟化酶抑制剂。了解更多

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JNJ-42041935

Catalog No. A15793
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HIF-PHD 抑制剂 II

JNJ-42041935是有效的(pKi = 7.3-7.9)，2-氧戊二酸竞争性，可逆和选择性PHD酶抑制剂。了解更多

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FG-2216

Catalog No. A15530
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HIF-prolyl hydroxylase 抑制剂

FG-2216是一种有效的HIF-脯氨酰羟化酶抑制剂，对PDH2酶的IC50为3.9 uM；生物利用度并在体内诱导显着且可逆的Epo诱导。了解更多

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Echinomycin

Catalog No. A14021
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HIF-1α 抑制剂

Hypoxia-inducible factor-1 (HIF-1)是一种转录因子，可控制参与糖酵解，血管生成，迁移和侵袭的基因。棘霉素是HIF-1介导的基因转录的细胞可渗透抑制剂了解更多

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Molidustat

Catalog No. A14404
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HIF-PH 抑制剂

Molidustat是一种新型的低氧诱导因子（HIF）脯氨酰羟化酶（PH）抑制剂，可刺激促红细胞生成素（EPO）的产生和红细胞的形成。了解更多

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PX-478 HCl

Catalog No. A14319
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HIF-1alpha 抑制剂

PX-478 HCl是HIF-1alpha抑制剂，也是具有潜在抗肿瘤活性小分子。PX-478对已建立的人类肿瘤异种移植物具有出色的活性，可提供具有HIF-1水平正相关的延长的生长延迟的肿瘤消退。PX-478是高度水溶性的分子，具有良好的i.v.，i.p.和p.o.抗肿瘤活性。了解更多

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BAY 87-2243

Catalog No. A12978
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HIF 抑制剂

BAY 87-2243是低氧诱导基因激活的高效选择性抑制剂，通过抑制线粒体复合体I具有抗肿瘤活性。了解更多

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HIF-C2

Catalog No. A12921
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HIF-2 抑制剂

HIF-C2是一种有效的选择性缺氧诱导因子2（HIF-2）变构抑制剂。了解更多

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FM19G11

Catalog No. A12883
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HIFα 抑制剂

FM19G11是缺氧诱导因子α（HIFα）的抑制剂，缺氧诱导因子α（HIFα）是一种转录因子，可对细胞环境中可用氧的变化做出响应。了解更多

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2-Methoxyestradiol

Catalog No. A10012
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Apoptotic, antiproliferative and antiangiogenic agent

2-Methoxyestradiol是一种凋亡，抗增殖和抗血管生成剂。通过两种途径诱导p53诱导的细胞凋亡：p38和NF-κB的激活；和激活JNK和AP-1导致Bcl-2磷酸化。了解更多

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