HIF/HIF Prolyl-Hydroxylase Inhibitor

GN44028 (Standard) is the analytical standard of GN44028 (HY-110266). This product is intended for research and analytical applications. 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.

PHD2-IN-5 (compound 22) is a potent PHD2 inhibitor with an IC₅₀ of 0.82 μM. PHD2-IN-5 can be used in the study of renal anemia.

PX-478 free base is a multifunctional HIF-1α inhibitor with properties including radiosensitization, autophagy activation, and lipid accumulation inhibition. PX-478 free base also blocks hypoxia-induced VEGF production and regulates β-cell phenotypes under hypoxic conditions. PX-478 free base induces cell cycle arrest and DNA damage, restores autophagic function, reduces foam cell formation, and maintains glucose homeostasis. PX-478 free base is widely used in research on related diseases such as human tumors (e.g., prostate cancer), type 2 diabetes, and atherosclerosis.

VH-298 (Standard) is the analytical standard of VH-298 (HY-100947). This product is intended for research and analytical applications. VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs.

Sapanisertib (INK-128; MLN0128; TAK-228) Standard is the analytical standard of Sapanisertib (HY-13328). This product is intended for research and analytical applications. Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

CLB-016 is a potent Hypoxia-inducible factor (HIF-1) inhibitor with an IC₅₀ of 19.1 μM. CLB-016 significantly suppresses HIF-1-mediated hypoxia response.

Fibrostatin F is a proline hydroxylase inhibitor found in Strptomyces catenulae.

S 4404 is a prolyl-4-hydroxylase inhibitor. S 4404 functions as a non-substrate of hepatobiliary transport systems. S 4404 undergoes metabolic breakdown into fluorescent and red-colored metabolites. S 4404 can be used for the research of liver fibrosis.

MK-8617 (Standard) is the analytical standard of MK-8617 (HY-101023). This product is intended for research and analytical applications. 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.

GW405833 hydrochloride (Standard) is the analytical standard of GW405833 (hydrochloride) (HY-110036A). This product is intended for research and analytical applications. GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC₅₀ and K_i values ​​of 0.65 nM and 3.92 nM for CB2, and EC₅₀ and K_i values ​​of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

PX-478 (Standard) is the analytical standard of PX-478 (HY-10231). This product is intended for research and analytical applications. PX-478 is a multifunctional HIF-1α inhibitor with properties including radiosensitization, autophagy activation, and lipid accumulation inhibition. PX-478 also blocks hypoxia-induced VEGF production and regulates β-cell phenotypes under hypoxic conditions. PX-478 induces cell cycle arrest and DNA damage, restores autophagic function, reduces foam cell formation, and maintains glucose homeostasis. PX-478 is widely used in research on related diseases such as human tumors (e.g., prostate cancer), type 2 diabetes, and atherosclerosis.

Agnuside (Standard) is the analytical standard of Agnuside. This product is intended for research and analytical applications. Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.

Fibrostatin D is a proline hydroxylase inhibitor found in Strptomyces catenulae.

Adaptaquin (Standard) is the analytical standard of Adaptaquin (HY-101449). This product is intended for research and analytical applications. Adaptaquin is a BBB-penetrable HIF-PHDs inhibitor. Adaptaquin has anti-inflammatory and neuroprotective effects. Adaptaquin can effectively inhibit lipid peroxidation, maintain mitochondrial function, and reduce neuronal death. Adaptaquin can be used in the research of nervous system diseases such as Parkinson's disease.

PHD-IN-5 (ISM4808) is an orally active PHD inhibitor that can be used for studying anemia in chronic kidney disease.

Vadadustat-¹³C₆ (PG-1016548-¹³C₆) is ¹³C labeled Vadadustat. Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.

PHD-1-IN-3 is an orally active PHD-1 inhibitor with an IC₅₀ of 0.09 μM. PHD-1-IN-3 acts via monodentate binding interaction with active site Fe²⁺ ion.

Fibrostatin A is a proline hydroxylase inhibitor found in Strptomyces catenulae.

Acanthoic acid (NP1302) is an orally active pimarane-type diterpenoid. Acanthoic acid is isolated from the root bark of Araliaceae family plant Eleutherococcus senticosus (Siberian ginseng). Acanthoic acid activates LXR and FXR. Acanthoic acid activates the AMPK-LKB1, SIRT1, and p38 MAPK signaling pathways and increases the phosphorylation level of ACC. Acanthoic acid downregulates the expression of SREBP-1, CYP2E1, HIF-1α, and PPARγ, and upregulates the expression of PPARα. Acanthoic acid induces Apoptosis by activating Caspase-3, promoting PARP cleavage, and downregulating Bcl-xL. Acanthoic acid exhibits antioxidant, anti-fibrotic, and hepatoprotective effects. It reduces lipid accumulation and lipogenesis. Acanthoic acid is used in studies on non-alcoholic fatty liver disease, alcoholic liver disease, acute promyelocytic leukemia, and Acetaminophen-induced hepatotoxicity.

(Rac)-PT2399 (Standard) is the analytical standard of (Rac)-PT2399 (HY-108697A). This product is intended for research and analytical applications. (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.