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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
PhD-1
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "PhD-1" in MCE Product Catalog:
8
8 Publications Verification
Synonyms: BAY 85-3934
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Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia [1] .
3
3 Cited Publications
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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.
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1 Cited Publications
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TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkey PHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia [1] .
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N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively [1] .
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JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.
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GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) [1].
Cat. No.: HY-170522
CAS No.: 2924181-80-4
Synonyms: ISM012-042
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Garutadustat (ISM012-042) is an orally active, selective inhibitor of PHD1 and PHD2, with IC50 values of 1.9 nM and 2.5 nM, respectively. Garutadustat stabilizes HIF1α protein in intestinal epithelial cells, thereby activating gene transcription programs associated with mucus production, tight junction formation, anti-inflammatory mediator generation and wound healing, which fundamentally promotes mucosal barrier repair and regulates intestinal immunity. Garutadustat can be used for the research of inflammatory bowel disease [1].
Cat. No.: HY-114333
CAS No.: 876150-14-0
Synonyms: 1-Octyl 2-oxopentanedioate
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Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD .
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PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an "Arg367-out" pocket [1].
Cat. No.: HY-183996
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PHD-1 ligand-1 (Compound 1) is a PHD-1 ligand. PHD-1 ligand-1 serves as a target protein ligand for the synthesis of PHD-1 PROTAC degraders, such as SH-26 (HY-183995). PHD-1 ligand-1 is applicable to studies on ischemia/reperfusion injury [1].
Cat. No.: HY-W747868
CAS No.: 1375799-59-9
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Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia [1] .
Cat. No.: HY-153513
CAS No.: 2009343-19-3
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Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
PHD-1-IN-4 is a brain-penetrant PHD-1 inhibitor with an IC50 of 0.074 μM [1].
Cat. No.: HY-153510
CAS No.: 2009344-53-8
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PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC50 of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury [1].
Cat. No.: HY-124133
CAS No.: 1238689-36-5
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JNJ-42905343 is an orally active and highly selective prolyl hydroxylase (PHD1/2/3) inhibitor with pKI values of 8.07, 7.48 and 7.27 for
PHD1, PHD2 and PHD3, respectively. JNJ-42905343 is promising for research of functional iron deficiency (FID) and anemia of chronic disease (ACD) [1].
Cat. No.: HY-139993
CAS No.: 2711720-45-3
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HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively [1].
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N-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively [1] .
Cat. No.: HY-153512
CAS No.: 2009345-20-2
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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 Fe 2+ ion [1].
Cat. No.: HY-12654R
CAS No.: 1154028-82-6
Synonyms: BAY 85-3934 (Standard)
Research Areas:
Molidustat (Standard) is the analytical standard of Molidustat. This product is intended for research and analytical applications. Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia [1] .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
