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Catalog No.
Product Name
Application
Product Information
Product Citation
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SGK1 inhibitor
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
SGK1 inhibitor
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
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. -
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. -
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. -
15-LO inhibitor
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis. -
Hsp90 inhibitor
Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. -
PDE-5 inhibitor
Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction. -
IDH1 inhibitor
DH1 Inhibitor 2 is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM. -
dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). -
IDO/TDO dual inhibitor
IDO/TDO-IN-1 is a highly potent and orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50s of 9.7 and 47 nM, respectively . -
EMT inhibitor
EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. -
PDE12 inhibitor
PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity. -
5-Lipoxygenase (5-LO) inhibitor
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation. -
FXIa inhibitor
BMS-962212 is a reversible, direct, and highly selective inhibitor of FXIa. -
Hsp70 inhibitor
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.- Siu Hong Dexter Wong, .et al. , Sci Adv, 2023, Jul 7;9(27):eadg9593 PMID: 37418519
- Shivani Patel, .et al. , iScience, 2022, Apr 22;25(5):104282 PMID: 35573186
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cell motility and cell invasion inhibitor
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life. -
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. -
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. -
TDP1 inhibitor
TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. -
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.
