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Catalog No.
Product Name
Application
Product Information
Citations
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TPH1/TPH2 inhibitor
Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice. -
FASN inhibitor
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression. -
p32 mitochondrial protein inhibitor
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1. -
ACE inhibitor
H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM. -
CETP inhibitor
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol. Single doses of CKD-519 up to 400 mg were well tolerated and showed potent inhibition of CETP activity. -
HSP27 inhibitor
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof.- Haruka Wakasa, .et al. , J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
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VEGFA inhibitor
PTC299 is a potent, orally bioavailable VEGFA inhibitor, targets dihydroorotate dehydrogenase (DHODH), resulting in cell growth inhibition and differentiation in leukemias, including acute myeloid leukemia, linking DHODH regulation and stress-induced VEGFA and angiogenesis. -
HMG-CoA reductase inhibitor
2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of Atorvastatin calcium salt. Atorvastatin is a potent HMG-CoA reductase inhibitor with an IC50 value of 8 nM. -
COX/LOX inhibitor
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 ?M?? -
TDP1 inhibitor
TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. -
IDH1 inhibitor
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells. -
ETC inhibitor
MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. -
autotaxin inhibitor
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain. -
SCD1 inhibitor
SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor. -
prolyl hydroxylase inhibitor
Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia. -
PFKFB3 inhibitor
KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM . -
PFKFB3 inhibitor
AZ PFKFB3 26 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 23 nM. AZ PFKFB3 26 inhibits PFKFB1 and PFKFB2 with IC50s of 2.06 and 0.384 μM, respectively. -
fungal Cyp51 inhibitor
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes. -
ATX inhibitor
Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM. -
PDE5 inhibitor
Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED). -
MPC inhibitor
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects. -
Cholesterol biosynthesis inhibitor
Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase. -
Cytochrome P450 inhibitor
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD. -
PDE-4 inhibitor
WAY127093B racemate is the racemate of WAY127093B. WAY127093B is a novel, orallyactive phosphodiesterase IV inhibitor in guinea pigs and rats. -
IDO1 inhibitor
LY-3381916 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
