Imirestat (AL 1576) is an aldose reductase inhibitor, used for the treatment of diabetes.
Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1][2].
Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor[1].
GSK3739936 (BMS-986180) is a potent, allosteric HIV-1 integrase (ALLINI), shows excellent potency in vitro against majority of the 124/125 variants (EC50=1.7 nM).
Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator[1][2].
Z-Arg-Arg-4MβNA triacetate is a cathepsin B-specific substrate and can produce fluorescent end product 4MβNA (λex = 355 nm, λem = 430 nm)[1][2].
Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively[1].
NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression[1].
Cilomilast(SB 207499; Ariflo) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.IC50 value: 110 nMTarget: PDE 4Cilomilast (SB-207499) inhibits HPDE4 and LPDE4 catalytic activity with equal potency (Ki ≈100 nM). SB-207499 and rolipram are equipotent against LPDE4, but Cilomilast (Ariflo, SB-207499) is 100-fold less potent against HPDE4. This profile suggests that Cilomilast (Ariflo, SB-207499) retain the anti-inflammatory activity of rolipram yet have a decreased tendency to produce side effects.
Napsagatran hydrate is a novel and specific thrombin inhibitor.
Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
Phosphatase-IN-1 (compound II-8), a propranolol (HY-B0573B) derivative, is a phosphatidate phosphatase (Pah) inhibitor. Phosphatase-IN-1 can binds to MoPah1, with an affinity constant of 19.8 μM. Phosphatase-IN-1 inhibits growth of plant pathogens and shows anti-fungal ability. Phosphatase-IN-1 is not toxic to rice seedlings and wheat heads[1].
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions[1][2].
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively[1][2].
FX-11 is a potent LDH-A inhibitor with an IC50 of 23.3 μM for HeLa cell，a Ki value of 8 μM.
Nitrefazole is a 4-nitroimidazole derivative with strong and long lasting inhibition of aldehyde dehydrogenase (ALDH), an enzyme involved in the metabolism of alcohol.
TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
MMP-9-IN-3 is a MMP-9 inhibitor (IC50: 5.56 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-3 also inhibits AKT activity (IC50: 2.11 nM). MMP-9-IN-3 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-3 can be used in the research of cancers[1].
Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral drugs (ARVs)[1].
IDO1-IN-11 is an IDO1 inhibitor with an IC50 value of 0.6 nM.
hTYR/AbTYR-IN-1 (Compound 7) is a hTYR/AbTYR dual inhibitor, with IC50s of 5.4 μM and 3.52 μM for hTYR and AbTYR respectively[1].
ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion[1].
5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsin K activity[1][2].
Urokinase peptidolytic (Urokinase-type plasminogen activator) is a serine protease, an inactive form (zymogen) of the serine protease plasminogen. Activation of plasmin triggers a proteolytic cascade reaction, which in turn participates in thrombolysis or extracellular matrix degradation, implicated in vascular disease and cancer-related research[1].