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HIF-1α Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIF/HIF Prolyl-Hydroxylase (67) ADC Cytotoxin (2) Akt (4) Amyloid-β (2) Antibiotic (10) AP-1 (1) Apoptosis (18) ATP Synthase (1) Autophagy (6) Bacterial (6) Calcium Channel (4) Cholinesterase (ChE) (2) DNA/RNA Synthesis (1) E3 Ligase Ligand-Linker Conjugates (2) Endogenous Metabolite (2) Epigenetic Reader Domain (1) ERK (1) FAK (1) Fungal (3) Histone Acetyltransferase (2) Histone Methyltransferase (2) HSP (4) HSV (1) Influenza Virus (2) Isotope-Labeled Compounds (3) Keap1-Nrf2 (1) Ligands for E3 Ligase (3) MDM-2/p53 (7) MicroRNA (3) Microtubule/Tubulin (3) Mitochondrial Metabolism (1) Monoamine Oxidase (1) mTOR (3) NF-κB (3) NOD-like Receptor (NLR) (1) Oxidative Phosphorylation (2) p38 MAPK (1) Parasite (2) PD-1/PD-L1 (4) PI3K (1) Potassium Channel (4) PPAR (2) PROTACs (1) Proton Pump (1) Pyroptosis (1) Ras (1) Reactive Oxygen Species (3) STAT (5) Topoisomerase (2) Trk Receptor (1) VEGFR (7) Xanthine Oxidase (3)
By Research Areas:	Cancer (83) Cardiovascular Disease (9) Infection (15) Inflammation/Immunology (15) Metabolic Disease (7) Neurological Disease (10)
Oligonucleotides:	Antisense Oligonucleotides (2)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: HIF/HIF Prolyl-Hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13671

LW6 25+ Cited Publications HIF-1α Inhibitor; LW8	HIF/HIF Prolyl-Hydroxylase Apoptosis	Cancer
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC₅₀ value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases *HIF-1α* protein expression without affecting HIF-1β expression.

HY-16031B

AFP464 dihydrochloride NSC710464 dihydrochloride	HIF/HIF Prolyl-Hydroxylase	Cancer
AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent *HIF-1α* inhibitor with an IC₅₀ value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).

HY-N2425

Rhodiosin	Cholinesterase (ChE)	Metabolic Disease
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the K_i is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-110266

GN44028 5 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC₅₀ of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .

HY-N0234

Bavachinin 3 Publications Verification 7-O-Methylbavachin; Bavachinin A	Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology Cancer
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of *HIF-1α*. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .

HY-115903A

HIF-1α-IN-2 hydrochloride 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-2 hydrochloride is an effective *HIF-1α* inhibitor with anticancer potencies (IC₅₀s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .

HY-149635

HIF-1α-IN-6	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-6 (compound 3s) is a *HIF-1α* inhibitor with IC₅₀ values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA .

HY-163370

HIF-1α-IN-7	HIF/HIF Prolyl-Hydroxylase	Neurological Disease
HIF-1α-IN-7 (Compound D13) is a potent *HIF-1α* inhibitor. HIF-1α-IN-7 has neuroprotective activity. HIF-1α-IN-7 can be used in Alzheimer's disease research .

HY-N2425R

Rhodiosin (Standard)	Cholinesterase (ChE)	Metabolic Disease
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-D2360

O-Carboranylphenoxyacetanilide	HIF/HIF Prolyl-Hydroxylase HSP	Cancer
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .

HY-N0234R

Bavachinin (Standard)	Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .

HY-115903

HIF-1α-IN-2 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-2 is an effective *HIF-1α* inhibitor with anticancer potencies (IC₅₀s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .

HY-146144

HIF-IN-1	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity .

HY-N0242

Fraxinellone 3 Publications Verification	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Inflammation/Immunology Cancer
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits *HIF-1α* protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .

HY-156106

VHL-IN-1	Ligands for E3 Ligase HIF/HIF Prolyl-Hydroxylase	Cancer
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .

HY-139804

CTK7A	Epigenetic Reader Domain Histone Acetyltransferase HIF/HIF Prolyl-Hydroxylase	Cancer
CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with *HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α* accumulation and activity, which can be used for cancer treatment research .

HY-115746

Dimethyl-bisphenol A DMBPA	HIF/HIF Prolyl-Hydroxylase	Cancer
Dimethyl-bisphenol A (DMBPA) is a potent *HIF-1α* inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression .

HY-P10223

Cyclo(CRVIIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 65 and 123 μM, respectively .

HY-146540

GEM-5	HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53	Cancer
GEM-5 is a gemcitabine-based conjugate containing a *HIF-1α* inhibitor (YC-1) (IC₅₀=30 nM). GEM-5 can significantly down-regulate the expression of *HIF-1α* and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth .

HY-147813

HIF-1α-IN-3	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective *HIF-1α* inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency .

HY-P10221A

Cyclo(CKLIIF) TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 2.6 and 2.2 μM, respectively .

HY-P10222

Cyclo(CRLLIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 14.5 and 10.2 μM, respectively .

HY-158826

EZN-2968 RO 707179	HIF/HIF Prolyl-Hydroxylase	Cancer
EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.

HY-158826A

EZN-2968 sodium	HIF/HIF Prolyl-Hydroxylase	Cancer
EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.

HY-N0242R

Fraxinellone (Standard)	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Inflammation/Immunology Cancer
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .

HY-15672

FM19G11	HIF/HIF Prolyl-Hydroxylase	Neurological Disease Cancer
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC₅₀ of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions .

HY-164259

AJM 290	HIF/HIF Prolyl-Hydroxylase	Cancer
AJM 290 is a Trx-1 inhibitor. AJM 290 is an inhibitor of the HIF-1α COOH-terminal transactivation domain, and blocks HIF-1 binding to DNA .

HY-N10330

7-Hydroxyneolamellarin A	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .

HY-10231

PX-478 45+ Cited Publications	HIF/HIF Prolyl-Hydroxylase Autophagy	Cancer
PX-478 is an orally active *HIF-1α* inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier .

HY-17412S

Minocycline-d6 hydrochloride	Isotope-Labeled Compounds Antibiotic	Others
Minocycline-d₆ hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and *HIF-1α* inhibitor .

HY-151465

HIF-1α-IN-4	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-4 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .

HY-151466

HIF-1α-IN-5	HIF/HIF Prolyl-Hydroxylase Monoamine Oxidase	Cancer
HIF-1α-IN-5 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .

HY-16031

AFP464 free base NSC710464 free base	HIF/HIF Prolyl-Hydroxylase	Cancer
AFP464 free base (NSC710464 free base), is an active *HIF-1α* inhibitor with an IC₅₀ of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.

HY-153017

HIF-1 inhibitor-4	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC₅₀: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level .

HY-119264A

PRLX-93936 dihydrochloride	HIF/HIF Prolyl-Hydroxylase Ras	Cancer
PRLX-93936 dihydrochloride (Compound 16) is a *HIF-1α* inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .

HY-122094

Steppogenin	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
Steppogenin is a potent inhibitor of *HIF-1α* and DLL4, with IC₅₀ values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors .

HY-158341

IOX5	HIF/HIF Prolyl-Hydroxylase Apoptosis	Cancer
IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC₅₀ of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .

HY-15468

IOX2 5+ Cited Publications	HIF/HIF Prolyl-Hydroxylase	Cancer
IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC₅₀ of 22 nM. IOX2 regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 can be used in the study of thrombotic diseases .

HY-15468A

IOX2 sodium	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC₅₀ of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases .

HY-N0596

Panaxadiol 20(R)-Panaxadiol	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Cancer
Panaxadiol (20(R)-Panaxadiol) is an orally active *HIF-1α/STAT3* inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .

HY-18259

103D5R	HIF/HIF Prolyl-Hydroxylase	Cancer
103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC₅₀ of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC₅₀ of 26 µM .

HY-17412S1

Minocycline-d6 sulfate	Isotope-Labeled Compounds	Infection Neurological Disease Inflammation/Immunology Cancer
Minocycline-d₆ sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.

HY-19731

SID 3712249 MiR-544 Inhibitor 1	MicroRNA Apoptosis	Cancer
SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer .

HY-107553

Chetomin	HSP Apoptosis	Cancer
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .

HY-N0596R

Panaxadiol (Standard)	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Cancer
Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .

HY-15205

Ganetespib 30+ Cited Publications STA-9090	HSP Apoptosis	Cancer
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .

HY-120087

KG-548	HIF/HIF Prolyl-Hydroxylase	Cancer
KG-548 is an ARNT/TACC3 disruptor and a *HIF-1α* inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β .

HY-B0223

Albendazole 3 Publications Verification SKF-62979	Parasite Microtubule/Tubulin Autophagy Apoptosis Reactive Oxygen Species VEGFR HIF/HIF Prolyl-Hydroxylase Antibiotic Bacterial	Infection Cancer
Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and *HIF-1α, VEGF* expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells .

HY-124722

OHM1	HIF/HIF Prolyl-Hydroxylase	Cancer
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .

HY-121172

1,4-DPCA 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC₅₀ of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits *factor inhibiting* HIF (FIH) with an IC₅₀** of 60 μM .

Cat. No.	Product Name	Type

HY-D2360

O-Carboranylphenoxyacetanilide	Fluorescent Dyes/Probes
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .

Cat. No.	Product Name	Target	Research Area

HY-P10221A

Cyclo(CKLIIF) TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 2.6 and 2.2 μM, respectively .

HY-P2657

Verucopeptin	HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite	Cancer
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.

HY-P1420

TAT-cyclo-CLLFVY 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts *HIF-1α/HIF-1β* protein-protein interaction with an IC₅₀ of 1.3 μM .

HY-P5908

DEALA-Hyp-YIPD	Peptides	Cardiovascular Disease
DEALA-Hyp-YIPD is an HIF-1α peptide that inhibits *VHL/HIF-1α* interaction with an IC₅₀ of 0.91 μM and a K_d** of 180 nM .

HY-P10223

Cyclo(CRVIIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 65 and 123 μM, respectively .

HY-P10222

Cyclo(CRLLIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 14.5 and 10.2 μM, respectively .

HY-P10426

cyclo(CLLFVY)	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .

HY-P1420A

TAT-cyclo-CLLFVY TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts *HIF-1α/HIF-1β* protein-protein interaction with an IC₅₀ of 1.3 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2425

Rhodiosin	Flavonols Structural Classification Classification of Application Fields Crassulaceae Source classification Metabolic Disease Plants Rhodiola crenulata (HK. f. et.Thoms) H. Ohba Flavonoids Rhodiola rosea Linn. Phenols Polyphenols Disease Research Fields	Cholinesterase (ChE)
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the K_i is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-N0234

Bavachinin 3 Publications Verification 7-O-Methylbavachin; Bavachinin A	Structural Classification Monophenols Flavonoids Classification of Application Fields Leguminosae Flavonones Source classification Phenols Psoralea corylifolia L. Plants Inflammation/Immunology Disease Research Fields	Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of *HIF-1α*. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .

HY-N0242

Fraxinellone 3 Publications Verification	Structural Classification Classification of Application Fields Terpenoids Dictamnus dasycarpus Turcz. Sesquiterpenes Source classification Rutaceae Plants Inflammation/Immunology Disease Research Fields	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits *HIF-1α* protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .

HY-122094

Steppogenin	Structural Classification Flavonoids Flavones Source classification Maclura tricuspidata Carriere Plants Moraceae	HIF/HIF Prolyl-Hydroxylase
Steppogenin is a potent inhibitor of *HIF-1α* and DLL4, with IC₅₀ values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors .

HY-N0596

Panaxadiol 20(R)-Panaxadiol	Panax ginseng C. A. Meyer Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Araliaceae Cancer	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
Panaxadiol (20(R)-Panaxadiol) is an orally active *HIF-1α/STAT3* inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .

HY-N2425R

Rhodiosin (Standard)	Flavonols Structural Classification Flavonoids Rhodiola rosea Linn. Crassulaceae Source classification Phenols Polyphenols Plants Rhodiola crenulata (HK. f. et.Thoms) H. Ohba	Cholinesterase (ChE)
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-N0234R

Bavachinin (Standard)	Structural Classification Monophenols Flavonoids Leguminosae Flavonones Source classification Phenols Psoralea corylifolia L. Plants	Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase
Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .

HY-N0242R

Fraxinellone (Standard)	Structural Classification Terpenoids Dictamnus dasycarpus Turcz. Sesquiterpenes Source classification Rutaceae Plants	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .

HY-N10330

7-Hydroxyneolamellarin A	Structural Classification Animals Source classification Phenols	HIF/HIF Prolyl-Hydroxylase VEGFR
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .

HY-N0596R

Panaxadiol (Standard)	Panax ginseng C. A. Meyer Triterpenes Structural Classification Terpenoids Source classification Plants Araliaceae	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .

HY-16560

Camptothecin 35+ Cited Publications Campathecin; (S)-(+)-Camptothecin; CPT	Infection Structural Classification Alkaloids Classification of Application Fields Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields	Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .

HY-N2199

Sotetsuflavone	Structural Classification Flavonoids Classification of Application Fields Source classification Phenols Polyphenols Selaginellaceae Plants Biflavones Selaginella tamariscina (P. Beauv.) Spring Disease Research Fields Cancer	Apoptosis Autophagy
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .

HY-N0787

Cryptochlorogenic acid 1 Publications Verification 4-Caffeoylquinic acid; 4-O-Caffeoylquinic acid	Structural Classification Classification of Application Fields Source classification Plants Moraceae Endogenous metabolite Simple Phenylpropanols Other Diseases Phenols Polyphenols Phenylpropanoids Disease Research Fields Morus alba Linn.	Endogenous Metabolite NF-κB Keap1-Nrf2 mTOR HIF/HIF Prolyl-Hydroxylase
Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / *HIF-1α* signaling pathway Induced physiological stress response .

HY-N3005

Britannin 1 Publications Verification	Phyllodium pulchellum (L.) Desv. Structural Classification Classification of Application Fields Terpenoids Sesquiterpenes Source classification Plants Compositae Inflammation/Immunology Disease Research Fields	Apoptosis Autophagy NOD-like Receptor (NLR) Pyroptosis
Britannin is an NLRP3 inhibitor with an IC₅₀ of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .

HY-N6782

Oligomycin Maximum Cited Publications 50 Publications Verification	Infection Structural Classification Microorganisms Antifungal Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Disease Research Fields	Oxidative Phosphorylation ATP Synthase Fungal Antibiotic
Oligomycin, an antifungal antibiotic, is an inhibitor of H ⁺-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells .

Cat. No.	Product Name	Chemical Structure

HY-17412S1

Minocycline-d6 sulfate
Minocycline-d₆ sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.

HY-16560S

Camptothecin-d5

Camptothecin-d₅ is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].

HY-17412S

Minocycline-d6 hydrochloride
Minocycline-d₆ hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and *HIF-1α* inhibitor .

HY-W654013

Minocycline-d7

Minocycline-d₇ is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .

Cat. No.	Product Name		Classification