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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 .
PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia .
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research .
PHD-IN-1 (compound 80) is a potent inhibitor of PHD2，with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells，respectively .
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI) .
PHD-IN-2 (Compound 91) is a PHD antagonist (IC50: < 5 nM). PHD-IN-2 induces erythropoietin synthesis in HEP3B cells (EC50: <2.5 μM). PHD-IN-2 can be used for research of cardiovascular disorders, metabolic disorders, hematological disorders, pulmonary disorders, kidney disorders, liver disorders, wound healing disorders, and cancer .
HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia .
Octyl-α-ketoglutarate is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional TCA cycle, stimulating PHD activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD .
M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors .
JBC117 is a novel anticancer lead compound targeting Pygo2 PHD. JBC117 can effectively antagonize the cell effect of β-catenin-dependent activity and inhibit the migration and invasion of cancer cells. JBC117 can induce apoptosis .
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM .
(S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
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.
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) .
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 .
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 .
(Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity .
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM forPHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM . Antianemia agent .
Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin .
Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. Adaptaquin can inhibit lipid peroxidation and maintain mitochondrial function .
DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation .
DC-BPi-11 hydrochloride is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 hydrochloride shows remarkable inhibition against leukemia cell proliferation .
DS44470011 is a hypoxia-inducing factor prolyl hydroxylase (HIF-PHD) inhibitor. DS44470011 has oral activity. DS44470011 promotes cell release of erythropoietin (EPO). DS44470011 can be used in the research of renal anemia .
FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo .
DS-1093a is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitor, with an EC50 of 0.49 μM in Hep3B cell EPO production. DS-1093a can be used in the research of renal anemia .
Roxadustat (Standard) is the analytical standard of Roxadustat. This product is intended for research and analytical applications. Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin .
NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity .
TM6008 is a potent and orally active prolyl hydroxylase (PHD) inhibitor. TM6008 chelats transition metal (copper) and inhibits the autoxidation of ascorbic acid with an IC50 value is 0.57 μM. TM6008 exerts organ protection against ischemia in vivo and can be used for cerebrovascular disease research .
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 .
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 .
TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector .
AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects .
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
ZG-2305 is a potent, orally active and selective factor inhibiting hypoxia-inducible factor (FIH) inhibitor with Ki values of 79.6, 2786 nM for FIH, PHD2, respectively. ZG-2305 increases the expression of EGLN3 gene. ZG-2305 decreases the cellular triglycerides levels and reduces lipid accumulation. ZG-2305 has the potential for the research of obesity and fatty liver disease .
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research .
(Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity .
The BRPF3 protein is a scaffold in various HAT complexes such as MOZ/MORF and HBO1 and is critical for histone H3 acetylation, especially in directing the specificity of KAT7/HBO1 for H3K14ac. In the HBO1 complex, BRPF3 promotes DNA replication initiation and activates replication origins. BRPF3 Protein, Human is the recombinant human-derived BRPF3 protein, expressed by E. coli , with tag free. The total length of BRPF3 Protein, Human is 140 a.a., .
The BRPF3 protein is a scaffold in various HAT complexes such as MOZ/MORF and HBO1 and is critical for histone H3 acetylation, especially in directing the specificity of KAT7/HBO1 for H3K14ac. In the HBO1 complex, BRPF3 promotes DNA replication initiation and activates replication origins. BRPF3 Protein, Human (His) is the recombinant human-derived BRPF3 protein, expressed by E. coli , with N-6*His labeled tag. The total length of BRPF3 Protein, Human (His) is 140 a.a., .
The BRPF1 protein is a key scaffold in HAT complexes such as MOZ/MORF and HBO1, and has histone H3 acetyltransferase activity. In the HBO1 complex, BRPF1 directs the specificity of KAT7/HBO1 for H3K14ac. BRPF1 Protein, Human is the recombinant human-derived BRPF1 protein, expressed by E. coli , with tag free. The total length of BRPF1 Protein, Human is 129 a.a., .
The BRPF1 protein is a key scaffold in HAT complexes such as MOZ/MORF and HBO1, and has histone H3 acetyltransferase activity. In the HBO1 complex, BRPF1 directs the specificity of KAT7/HBO1 for H3K14ac. BRPF1 Protein, Human (His) is the recombinant human-derived BRPF1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of BRPF1 Protein, Human (His) is 129 a.a., .
BPTF proteins are regulatory subunits in the NURF-1 and NURF-5 ISWI chromatin remodeling complexes that assemble ordered nucleosome arrays to access DNA during replication, transcription, and repair. The NURF-1 complex is critical for brain development and actively regulates the expression of En1 and En2. BPTF Protein, Human is the recombinant human-derived BPTF protein, expressed by E. coli , with tag free. The total length of BPTF Protein, Human is 169 a.a., .
BPTF proteins are regulatory subunits in the NURF-1 and NURF-5 ISWI chromatin remodeling complexes that assemble ordered nucleosome arrays to access DNA during replication, transcription, and repair. The NURF-1 complex is critical for brain development and actively regulates the expression of En1 and En2. BPTF Protein, Human (His) is the recombinant human-derived BPTF protein, expressed by E. coli , with N-6*His labeled tag. The total length of BPTF Protein, Human (His) is 169 a.a., .
UHRF2; E3 ubiquitin-protein ligase UHRF2; Np95/ICBP90-like RING finger protein; Np95-like RING finger protein; Nuclear protein 97; Nuclear zinc finger protein Np97; RING finger protein 107; RING-type E3 ubiquitin transferase UHRF2; Ubiquitin-like PHD and RING finger domain-containing protein 2; Ubiquitin-like-containing PHD and RING finger domains protein 2
UHRF2 protein is an E3 ubiquitin ligase involved in DNA methylation, histone modification, cell cycle regulation and DNA repair. UHRF2 Protein, Human (His, SUMO) is the recombinant human-derived UHRF2 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of UHRF2 Protein, Human (His, SUMO) is 230 a.a., .
The PHF8 protein is a histone lysine demethylase that plays a key role in cell cycle progression, rDNA transcription, and brain development. It selectively demethylates H3 'Lys-9' (H3K9Me1 and H3K9Me2), H3 'Lys-27' (H3K27Me2) and H4 'Lys-20' (H4K20Me1). PHF8 Protein, Human is the recombinant human-derived PHF8 protein, expressed by E. coli , with tag free. The total length of PHF8 Protein, Human is 446 a.a., .
The PHF8 protein is a histone lysine demethylase that plays a key role in cell cycle progression, rDNA transcription, and brain development. It selectively demethylates H3 'Lys-9' (H3K9Me1 and H3K9Me2), H3 'Lys-27' (H3K27Me2) and H4 'Lys-20' (H4K20Me1). PHF8 Protein, Human (His) is the recombinant human-derived PHF8 protein, expressed by E. coli , with N-6*His labeled tag. The total length of PHF8 Protein, Human (His) is 446 a.a., .
EGLN1 Protein, Human (His) is the recombinant human-derived EGLN1, expressed by E. coli , with His labeled tag. The total length of EGLN1 Protein, Human (His) is 246 a.a.,
PHD3 Antibody (YA1612) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1612), targeting PHD3, with a predicted molecular weight of 27 kDa (observed band size: 27 kDa). PHD3 Antibody (YA1612) can be used for WB, IHC-P, IP experiment in human, mouse, rat background.
PHD1 Antibody (YA3325) is a biotin-conjugated non-conjugated IgG antibody, targeting PHD1, with a predicted molecular weight of 44 kDa (observed band size: 44 kDa). PHD1 Antibody (YA3325) can be used for WB experiment in human, rat background.
PHD2 Antibody (YA2431) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2431), targeting PHD2, with a predicted molecular weight of 46 kDa (observed band size: 46 kDa). PHD2 Antibody (YA2431) can be used for WB, IP experiment in human background.
PHF8 Antibody (YA2324) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2324), targeting PHF8, with a predicted molecular weight of 118 kDa (observed band size: 140 kDa). PHF8 Antibody (YA2324) can be used for WB, ICC/IF, IP experiment in human, mouse, rat background.
HIF Prolyl Hydroxylases Antibody (YA2975) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2975), targeting HIF Prolyl Hydroxylases, with a predicted molecular weight of 57 kDa (observed band size: 43 kDa). HIF Prolyl Hydroxylases Antibody (YA2975) can be used for WB, IHC-P, IP experiment in human background.
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