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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
IDH1 inhibitor
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H. -
5-lipoxygenase inhibitor
Esculetin, a phenolic compound, acts as a 5-LO (5-lipoxygenase, 5-LOX) inhibitor. -
Factor Xa inhibitor
5-R-Rivaroxaban is (R) enantiomer of Rivaroxaban. Rivaroxaban is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders. -
Hsp90 inhibitor
Alvespimycin is a selective Hsp90 inhibitor with a GI50 of 53 nM. -
CYP3A4 Inhibitor
Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA. -
CYP2C19/CYP2B6 inhibitor
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. -
DGAT-1 inhibitor
DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents. -
Factor Xa inhibitor
Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention. -
PDE Inhibitor
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. -
Liver-targeting SCD Inhibitor
MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. -
lipoxygenase inhibitor
Nordihydroguaiaretic acid is a natural phenolic compound isolated from the creosote bush Larrea divaricata, which has anti-tumor activities both in vitro and in vivo. Its analogs are in clinical development for use in refractory solid tumors. -
PDE5 inhibitor
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. -
PDE3 inhibitor
Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor. -
DHFR inhibitor
Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. -
FAAH inhibitor
PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen. -
Hsp90 inhibitor
Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. -
Human cathepsin L inhibitor
SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
PAK4/NAMPT Inhibitor
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. -
LXRα inhibitor
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects. -
HDAC/ACE inhibitor
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. -
HSP90β Inhibitor
CCT018159 is an ATP-competitive inhibitor of the HSP90β protein, exhibiting an IC50 of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. This compound induces cell cycle arrest and apoptosis in various tumor cell lines while effectively inhibiting processes such as invasion and angiogenesis. CCT018159 is particularly valuable for research applications in cancer biology and therapeutic development. -
Monoamine Oxidase Inhibitor
Harmol is a β-carboline alkaloid functioning as a monoamine oxidase inhibitor and TFEB activator. It has been shown to induce cell mitosis, autophagy, and apoptosis, promoting the degradation of α-synuclein through the autophagy-lysosomal pathway. Harmol exhibits notable anti-tumor, anti-depressant, and anti-aging properties and demonstrates efficacy in improving motor impairments in models of Parkinson's disease. This compound holds significant potential for research in neurodegenerative diseases and cellular autophagy mechanisms. -
HSP Inhibitor
Cucurbitacin D is a potent HSP90 inhibitor that disrupts the interaction between Hsp90 and co-chaperones Cdc37 and p23. This compound exhibits significant biological activities, including the induction of cell cycle arrest and apoptosis, showcasing its potential as an anti-tumor and anti-inflammatory agent. Cucurbitacin D is useful in research applications aimed at understanding the role of heat shock proteins in cancer and inflammation. -
Hsp70 Inhibitor
JG-231 is an allosteric inhibitor targeting heat shock protein 70 (Hsp70). By disrupting the interaction between Hsp70 and BAG family proteins, JG-231 exhibits an inhibition constant (Ki) of 0.11 μM. This compound effectively inhibits tumor cell proliferation and induces apoptosis, demonstrating significant antitumor activity. JG-231 is valuable for research into the roles of Hsp70 in cancer biology and its potential as a therapeutic target. -
IDO Inhibitor
(Rac)-Indoximod is an indoleamine 2,3-dioxygenase (IDO) inhibitor that modulates immune responses. This compound synergizes with interferon-gamma (IFN-γ) to significantly decrease the activity of human cardiac myofibroblasts, characterized by α-SMA expression, and promotes apoptosis by upregulating the genes IRF-1, Fas, and FasL. Its applications include studying immune regulation and apoptosis in cardiac tissue and investigating therapeutic strategies for fibrotic diseases. -
ACE Inhibitor
Benazepril is an orally active angiotensin-converting enzyme (ACE) inhibitor that reduces the production of angiotensin II. This compound exhibits protective effects against oxidative stress and apoptosis through modulation of the PI3K/Akt signaling pathway. Benazepril is commonly utilized in research focusing on hypertension, heart failure, and diabetic nephropathy, demonstrating efficacy in improving diabetic nephropathy and reducing proteinuria. -
PKM2 Inhibitor
PKM2-IN-6 is a potent inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 value of 23 nM. This compound induces apoptosis and facilitates cell cycle arrest at the G2 phase, demonstrating significant anticancer activity. PKM2-IN-6 also decreases the mRNA levels of both PKM1 and PKM2, indicating its effect on metabolic regulation. This reagent is particularly relevant for research applications focused on triple-negative breast cancer. -
PCSK9 Inhibitor
Pinostrobin is a flavonoid that acts as a potent inhibitor of PCSK9, targeting its catalytic activity. This compound demonstrates significant anti-cancer, antioxidant, antiviral, and neuroprotective properties. Pinostrobin is suitable for research applications in diverse areas, including viral infections, cancer therapeutics, cardiovascular and cerebrovascular disorders, cirrhosis, inflammatory diseases, and neurological conditions. -
GLUT4 Inhibitor
GLUT4-IN-2 is a selective inhibitor of the glucose transporter GLUT4, exhibiting IC50 values of 6.8 µM for GLUT4 and 11.4 µM for GLUT1. This compound has been shown to induce cell apoptosis and arrest the cell cycle at the G0/G1 phase, highlighting its potential as an anticancer agent. GLUT4-IN-2 is suitable for research applications aimed at understanding glucose metabolism and evaluating therapeutic strategies in cancer biology. -
Phospholipase A2 Inhibitor
OBAA is a potent inhibitor of phospholipase A2 (PLA2), exhibiting an IC50 of 70 nM. This compound effectively blocks Melittin-induced calcium influx in Trypanosoma brucei, demonstrating an IC50 of 0.4 μM. OBAA is valuable for research applications aimed at understanding the role of PLA2 in various biological processes and cellular responses. -
IDO-1/NS2B-NS3 Inhibitor
Palmatine hydroxide is an irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1) with IC50 values of 3 μM and 157 μM against HEK 293-hIDO-1 and rhIDO-1, respectively. This compound also exhibits uncompetitive inhibition of the West Nile virus NS2B-NS3 protease with an IC50 of 96 μM. Palmatine hydroxide demonstrates a wide range of biological activities, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotective, antibacterial, and antiviral effects, making it a valuable tool for research in cancer therapy, viral infections, and oxidative stress-related studies.
