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Catalog No.
Product Name
Application
Product Information
Product Citation
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Carbonic anhydrase inhbitor
Indisulam (E7070) is a carbonic anhydrase inhbitor, is also a novel synthetic sulfon-amide that targets the G1 phase of the cell cycle. -
FPTase inhibitor
Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.- Stella Liong, .et al. , Mediators Inflamm, 2018, 2018: 3645386 PMID: 30402038
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FTase inhibitor
FTI 276 is an inhibitor that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines. -
GAPDH inhibitor
CGP 3466B maleate is an orally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor. -
dual FAAH/MAGL inhibitor
JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively.- Lakhan S Khara, .et al. , J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. , J Exp Biol, 2021, 21 JUNE
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FAAH inhibitor
JNJ 1661010 is a selective and reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12nM). -
5-LPO inhibitor
ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor. -
DGAT1 inhibitor
Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor. -
squalene synthetase inhibitor
YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents. -
NAMPT inhibitor
CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM. -
FXa Inhibitor
Betrixaban is an anticoagulant drug which acts as a direct factor Xa inhibitor. It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low hERG affinity. -
CYP3A4 inhibitor
PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively). -
PDE 3/4 inhibitor
Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively). -
platelet PDE inhibitor
Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties. -
CRM1 inhibitor
KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.- Youjin Na, .et al. , Oncogene, 2023, Mar;42(13):1038-1047 PMID: 36759572
- Chie Ishikawa, .et al. , Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
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Mitochondrial respiratory chain inhibitor
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. -
DGAT2 inhibitor
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. -
CYP17 inhibitor
CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM. -
PDE5 inhibitor
Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.- Michel R. Corboz, .et al. , Eur J Pharmacol, 2022, 916: 174484 PMID: 34508752
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HSP90 inhibitor
Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents.- Aykut Ozgur, .et al. , Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319
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MAGL Inhibitor
JZL184 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM).- Lakhan S Khara, .et al. , J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. , J Exp Biol, 2021, 21 JUNE
- Toshihiko Tsutsumi, .et al. , Biochim Biophys Acta Mol Cell Biol Lipids, 2020, Sep;1865(9):158761 PMID: 32629025
- Rea Pihlaja, .et al. , Front Neurosci, 2017, 11: 299 PMID: 28611577
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HSF1 activation inhibitor
Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia. -
ACE inhibitor
Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.- Tomas Jasenovec, .et al. , Biomedicines, 2021, Dec 14;9(12):1902 PMID: 34944718
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PDE4 inhibitor?€?
AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines -
Hydroxylase Inhibitor
Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM).- Tianxing Ying, .et al. , Cancers (Basel), 2022, Dec 30;15(1):243 PMID: 36612238
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HSP90 Inhibitor
HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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factor Xa inhibitor
Letaxaban, also known as TAK-442, is a potent, selective, and orally active factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one derivative. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442] and rat (IC(50): 32 nM, TAK-442) plasma. -
IDH1 inhibitor
AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity. -
MAO-A inhibitor
Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A inhibitor. -
HIF inhibitor
BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. -
DHODH inhibitor
Vidofludimus is a novel orally active and potent DHODH inhibitor. -
IDO1 inhibitor
INCB024360 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. -
PDE2A inhibitor
PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. -
squalene synthase inhibitor
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8??0.2 nM. -
FASN inhibitor
Denifanstat (TVB-2640) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.
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Cytochrome P450 inhibitor
Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase. -
alpha-glucosidase I inhibitor
Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection. -
PDE9 inhibitor
PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice.
