HIF/HIF Prolyl-Hydroxylase Inhibitor

Fibrostatin C (P-23924C) is an orally active prolyl hydroxylase inhibitor that also inhibits collagen biosynthesis. Fibrostatin C also increases the number of cytoplasmic granules immunoreactive with antibodies to collagen I or III. Fibrostatin C inhibits the secretion of type I collagen in Tenon's capsule fibroblasts. Fibrostatin C is promising for research of the wound fibrotic response in the wound of glaucoma filtering surgery.

HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC₅₀ of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).

KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC₅₀ of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies.

PHD-1-IN-4 is a brain-penetrant PHD-1 inhibitor with an IC₅₀ of 0.074 μM.

PHD-IN-3 (Compound 15) is an orally active PHD inhibitor. PHD-IN-3 can be used in the study of anemia associated with chronic kidney disease.

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC₅₀: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.

TRC160334 sodium is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 sodium can be used for the research of ischemia/reperfusion injury.

HIF-2α-IN-13 (18) is a HIF-2α inhibitor, with an IC₅₀ of 2.7 μM.

HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2 (HY-179424).

CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC₅₀ = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer.

NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.

Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema.

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.

Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression.

HIF-2α-IN-12 (9) is a HIF-2α inhibitor, with an IC₅₀ of 0.9 μM.

PHD2-IN-4 (compound 1) is a PHD2 inhibitor. PHD2-IN-4 inhibits PHD2 with an IC₅₀ of 4 nM. PHD2-IN-4 is potential for chronic kidney disease research.

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal 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.

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC₅₀ of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential.

DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .