Migalastat HCl | Galactosidase inhibitor/Pharmacological chaperone
Migalastat (75172-81-5) is a potent, selective, and orally available inhibitor of α-galactosidase A (IC50= 40 nM).1 It binds to mutant misfolded α-GalA shifting the folding behavior
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Migalastat (75172-81-5) is a potent, selective, and orally available inhibitor of α-galactosidase A (IC50= 40 nM).1 It binds to mutant misfolded α-GalA shifting the folding behavior
Lonidamine is an antiglycolytic drug with limited efficacy.1,2 Mito-lonidamine (2361564-49-8) is lonidamine conjugated to a triphenylphosphonium moiety via a decyl-linker which is an effective mitochondria-targeting group.3 Mito-lonidamine was shown
CBR-470-1 (2416095-06-0) is an activator of NRF2 signaling (EC50 ~ 1 µM cellular ARE-LUC assay).1 It inhibits phosphoglycerate kinase 1 leading to a build-up of methylglyoxal which inactivates
5-(3-bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]-phenanthridin-4(1H)-one
UNC7467 (2922283-43-8) is a potent inhibitor of inositol hexakisphosphate kinase (IP6K) – the isoform IP3K1 regulates metabolism, promotes insulin secretion from ß cells, attenuates certain aspects
CBR-470-1 (2416095-06-0) is an activator of NRF2 signaling (EC50 ~ 1 µM cellular ARE-LUC assay).1 It inhibits phosphoglycerate kinase 1 leading to a build-up of methylglyoxal which inactivates
S07-2010 (1223194-71-5) is a pan-aldo-keto reductase 1C (AKR1C) inhibitor (IC50’s for AKR1C isoforms: 1C1 = 470 nM, 1C2 = 730 nM, 1C3 = 190 nM, 1C4
Bempedoic acid (738606-46-7) is an inhibitor of ATP citrate lyase (ACL) and activator of AMPK used in the treatment of hypercholesterolemia.1,2 In vivo, the active molecule is
Visomitin (934826-68-3) is a mitochondria-targeted antioxidant.1,2 A useful tool for studying mitochondrial oxidative stress involvement in many disease states.3-6 In clinical trials for the treatment of various eye
Lonidamine is an antiglycolytic drug with limited efficacy.1,2 Mito-lonidamine (2361564-49-8) is lonidamine conjugated to a triphenylphosphonium moiety via a decyl-linker which is an effective mitochondria-targeting group.3 Mito-lonidamine was shown
IACS-010759 (1570496-34-2) is a potent (IC50 = 1.1 nM isolated mouse complex I) and selective inhibitor of complex I of the mitochondrial electron transport chain (OXPHOS). IACS-010759
STF-118804 (894187-61-2) is a potent and selective next generation inhibitor of nicotinamide phosphoribosyl transferase (NAMPT), inhibiting NAD+ biosynthesis from nicotinamide.1 It reduced the viability of most B-ALL cells
Raltitrexed (112887-68-0) is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2 It is also an inhibitor
Methylbenzoprim (118344-71-1; Compound 19-S), a derivative of the antimalarial drug Pyrimethamine, is a non-classical potent inhibitor of mammalian dihydrofolate reductase (IC50 = 3.2 nM rat liver).1 It inhibited
L-Cycloserine (339-72-0) down-regulates sphingolipid biosynthesis via inhibition of serine palmitoyltransferase (3-ketodihydrosphingosine synthetase).1 The L isomer was shown to be 100-fold more potent than the D isomer at
PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).1 It induced autophagy in head and neck squamous
Mirabegron (223673-61-8) is a potent (EC50 = 22.4 nM CHO cells expressing human ß3-ARs) beta-3 adrenergic receptor (ß3-AR) agonist with high selectivity over the beta-1 and
S07-2010 (1223194-71-5) is a pan-aldo-keto reductase 1C (AKR1C) inhibitor (IC50’s for AKR1C isoforms: 1C1 = 470 nM, 1C2 = 730 nM, 1C3 = 190 nM, 1C4
SM-88 (30625-05-9) is a “dysfunctional” tyrosine mimetic. It is taken up by cancer cells and disrupts tyrosine-mediated metabolic pathways including synthesis of the important protein mucin-1
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