Lyciumin A, a cyclic octapeptide, exhibits inhibitory activity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension[1][2].
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM[1][2].
DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM in a time-resolved FRET assay). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM[1].
AN3199 is a PDE4 inhibitor with IC50 of 94.5 nM.IC50 value: 94.5 nM [1]Target: PDE4The detailed information please refer to Compound 11 in the reference.
Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans[1].
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus[1].
HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity[1].
Cyclotheonamide A is a serine protease inhibitor (cyclic polypeptide), which can be obtained from marine sponges of the genus Theonella. Cyclotheonamide A shows potent inhibitory activity against trypsin (Ki=0.023 µM) and streptokinase (Ki=0.035 µM) and moderate inhibitory activity against human α-thrombin (Ki=0.18 µM). Cyclotheonamide A can be used in study of antithrombotic[1].
11C-MK-3168 is a potent, reversible and blood/brain barrier penetrated fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, respectively.
FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells; selectively and irreversibly inhibits the growth of mesenchymally transformed breast cancer cells ( FOXC2-HMLER cells IC50=234 nM) and soft tissue sarcomas of diverse histological subtypes.
2-Bromo-4'-hydroxyacetophenone a PTP1B inhibitor, with a Ki of 42 μM[1].
(3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane is a homoisoflavonoid. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane increases the level of alkaline phosphatase (ALP) activity. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane promotes mesenchymal stem cells (MSCs) osteogenesis, but cannot enhance MSCs proliferation. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane can be used for osteoporosis research[1].
Anticancer agent 142 (compound 235) is a PTPN inhibitor, with the potential to study cancer[1].
HSP90-IN-27 (compound 19) is an HSP90 inhibitor[1].
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein tyrosine phosphatase 1B (PTB-1B), with an IC50 of 1 μM, 200-fold preference over TC-PTP (IC50 of 224 μM).
Carbazeran, a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran can be used for the research of metabolic disease[1].
Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.
EMT inhibitor-2 (Compound 1) 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[1].
ALDH2 modulator 1 is a potent and orally active aldehyde dehydrogenase-2 (ALDH2) modulator. ALDH2 modulator 1 reduces blood alcohol levels in mice[1].
PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro[1].
VP3.15 dihydrobromide 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 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS)[1].
BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 μM.
IDO-IN-15 is an IDO1 inhibitor (IC50 < 0.51 nM).
IGUANA-1 is a potent inhibitor of ALDH1B1, which is a mitochondrial enzyme that promotes colorectal and pancreatic cancer. IGUANA-1 has significant inhibition against cancer cells[1].
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) [1].
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[1][2].
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity[1].
Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor.
(rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1].