hif-1

HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM. HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.

Acetylarenobufagin is a steroidal hypoxia-inducible factor-1 (HIF-1) modulator.

GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.

Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.

Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in anticancer studies.

Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.

PROTAC HIF-1α degrader-1 (compound V2) is an effective proteolysis-targeting chimeric (PROTAC) degrader of hypoxia-inducible factor-1α (HIF-1α), with an IC50 value of 7.54 µM. This compound exhibits anti-proliferative activity, reduces HIF-1α protein expression, and induces apoptosis.

NF-κB/HIF-1α-IN-1 (compound 9c) effectively inhibits the NF-κB activation pathway and demonstrates selective antifibrotic activity. This compound exhibits no significant cytotoxicity in NCI tumor cell lines. In rat models, NF-κB/HIF-1α-IN-1 successfully ameliorates liver fibrosis, suppresses the expression levels of NF-κB and HIF-1α, and induces Nrf2.

HIF-1/2α-IN-2 is a potent inhibitor of HIF-1/2α that effectively reduces HIF-1/2α levels and elicits an iron starvation response by specifically targeting ISCA2, a key protein in Iron-Sulfur Cluster Assembly 2. [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].

HIF-1α inhibitor-1 is a HIF-1 alpha inhibitor.

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 value of 2.38 μM, demonstrating significant anti-angiogenic potential [1].

HIF-1 alpha (556-574) TFA is a 19-residue fragment of hypoxia-inducible factor-1 (HIF-1), the master regulator of oxygen homeostasis [1].

HIF-1 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as a master regulator of oxygen homeostasis by initiating hypoxia-induced gene expression when the HIF-1 subunit is stabilized due to lack of oxygen. This fragment binds to the von Hippel-Lindau factor (VHL), an E3 ubiquitin ligase, with proline 564 being essential to the binding process.

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

HIF-2α-IN-1 is a potent inhibitor of HIF-2α, with IC50 values below 500 nM.

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.

HIF-IN-1 is a potent inhibitor of hypoxia-inducible factor (HIF-1), which is associated with tumor and cancer cell proliferation and inhibits HIF-1α protein aggregation.

HIF-1α-IN-4 is an inhibitor of HIF-1α with IC50 of 24 nM in HEK293T cells which has potential antitumor effects. HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia [1].

HIF-1α-IN-5 is an inhibitor of HIF-1α with an IC 50 value of 24 nM in HEK293T cells that also inhibits the activity of MAO-A. HIF-1α-IN-5 downregulates the mRNA expressions of VEGF and PDK1 under hypoxia. HIF-1α-IN-5 has the potential to be used in the cancer research[1].

HIF-1α-IN-3, also known as Compound (S)-3f, is a hypoxia-selective inhibitor of HIF-1α. It exhibits potent antiestrogenic activity [1].

HIF-1α-IN-2 hydrochloride is a potent HIF-1α inhibitor exhibiting anticancer activity, with IC50 values of 28 nM in MDA-MB-231 cells and 15 nM in MiaPaCa-2 cells, effectively suppressing HIF-1α expression by inhibiting transcription and protein translation [1].