MtTMPK-IN-4 (compound 2), a para-piperidine, is a potent mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 of 6.1 μM. MtTMPK-IN-4 is a potent tyrosinase inhibitor. MtTMPK-IN-4 is a potent antibacterial agent[1][2].
Theodrenaline hydrochloride is a cardiac stimulant, also acts as an anti-hypotensive agent together with Cafedrine.
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties[1][2].
NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells[1].
8-Prenylluteone is a HIV-1 protease inhibitor, with an IC50 of 4 μM[1].
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1].
IDH1 Inhibitor 8 (91) is isocitrate dehydrogenase 1 (IDH1) inhibitor. IDH1 Inhibitor 8 can be used for the research of cancer[1].
Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models[1][2][3].
JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii[1]. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase[2][3].
R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor. The fuction is similar to R 80122 (HY-100615, Revizinone).In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) is 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increases global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [3]
Aureusidin is an aurone with high antioxidant and lipoxygenase inhibitory activity. Aureusidin also shows anti-inflammatory effects[1].
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
6-Hydroxyluteolin (Compound 17) is a flavonoid compound. 6-Hydroxyluteolin has an inhibitory effect on aldose reductase (AR) [1].
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production[1].
Opevesostat is a cholesterol side-chain cleavage enzyme (CYP11A1) inhibitor[1].
Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity[1].
Mvt-101 is a hexapeptide-based inhibitor of HIV-1 protease. Mvt-101 is also reduced-peptide-bond inhibitor. Mvt-101 inhibits reproduction of the HIV virus by blocking protease action[1].
Fosinopril (SQ28555) is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value of 0.18 μM[1]. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with a Ki value of 1.675 μM[2].
SKF107457 is an HIV-1 protease inhibitor that can be used in AIDS research[1][2].
MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
Lovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM[1].
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC50s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC50s of 60.2 and 38.6 μM, respectively[1].
KZR-504 is a highly selective and orally active inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively.
Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs)[1].
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE[1][2].
Samatasvir (IDX719) is a highly potent, selective inhibitor of HCV NS5A that effectively inhibits HCV genotype 1-5 replicons with EC50 of 2-24 pM; also retains full activity in the presence of HIV and hepatitis B virus (HBV) antivirals; demonstrates an overall additive effect when combined with IFN-α, ribavirin, representative HCV protease, and nonnucleoside polymerase inhibitors or the nucleotide prodrug IDX184. HCV Infection Phase 2 Clinical
FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells[1].
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy[1].
Lys-Ala-pNA is hydrolytic substrate the of dipeptidyl peptidase (DPP) II with Km of 0.42 mM[1].
Alirocumab (REGN 727) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia[1].