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PLD inhibitor
Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM). -
HMG-CoA reductase inhibitor
Pitavastatin Lactone is an HMG-CoA reductase inhibitor. -
Pim-1 inhibitor
Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM. -
11β-hydroxylase inhibitor
Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively. -
tryptophan hydroxylase inhibitor
Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM. -
NAMPT inhibitor
STF 118804 is a highly specific NAMPT inhibitor that reduces the viability of most B-ALL cell lines with high potency IC50 values in the low nanomolar range and improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia. -
TrxR1/CRM1 inhibitor
Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1). -
XOR Inhibitor
Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM. -
metalloendopeptidase inhibitor
Phosphoramidon Disodium Salt is a metalloendopeptidase inhibitor. -
Lp-PLA2 Inhibitor
Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor . -
glucosidase I/II inhibitor
Deoxynojirimycin is a Maltase-glucoamylase (a-glucosidase I and II) inhibitor. It interferes with N-linked glycosylation. -
IDH1 inhibitor
AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. -
IDO inhibitor
Indoximod is a methylated tryptophan with anti-immunosuppressive activity. -
FTase Inhibitor
FTI-277 HCl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. -
IDO1 inhibitor
BMS-986205, also known as Linrodostat, ONO-7701 and F001287, a potent and selective, orally active IDO1 inhibitor with potential immunomodulating and antineoplastic activities. CAS: 1923833-60-6 (free base) 2221034-29-1 (mesylate) -
PDE9 inhibitor
BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor. -
mIDH1 inhibitor
BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). -
human cytochrome P450IA2 inhibitor
Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM. -
COX and lipo-oxygenase inhibitor
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets. -
TLR/SCD inhibitor
E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).
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FAAH inhibitor
BIA10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) . -
alpha-adrenergic receptor agonist / MAO inhibitor
Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release. -
ER stress inhibitor
Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor. -
CYP2C9 inhibitor
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
Metabolism
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