MMP-2 Inhibitor II (compound 2) is a selective MMP-2 inhibitor. The Kinetic parameters for MMP inhibition are 2.4 μM (MMP-2), 45 μM (MMP-1), and 379 μM (MMP-7), respectively[1].
BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM. IC50 value: 0.24± 0.0019 uM (SC1.5) [1]Target: Glucokinase activatorThe R stereoisomer Ro 28-1675 activated GK with a SC1.5 of 0.24 uM, while the S isomer did not activated GK up to 10 uM. Oral administration of Ro 28-1675 (50 mg/Kg) to male C57B1/6J mice caused a statistically significant reduction in fasting glucose levels and improvement in glucose tolerance relative to the vehicle treated animals [1]. Comparison of rat PK parameters indicated that Ro 28-1675 displayed lower clearance and higher oral bioavailability compared to 9a. Following a single oral dose, Ro 28-1675 reduced fasting and postprandial glucose levels following an OGTT, was well tolerated, and displayed no adverse effects related to drug administration other than hypoglycemia at the maximum dose (400 mg). [1]
ALDH1A3-IN-1 (Compound 14) is a potent ALDH1A3 inhibitor, with an IC50 of 0.63 µM and a Ki of 0.46 µM. ALDH1A3-IN-1 can be studied in prostate cancer[1].
SU 10603 is a specific inhibitor of P45017α (P450c17; CYP17A1)[1].
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research[1][2].
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis[1].
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ[1].
BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis[1].
Naphthol AS-BR is a substrate for the histochemical demonstration of acid and alkaline phosphatase[1].
Isovalerylcarnitine chloride, a product of the catabolism of L-leucine, is a potent activator of the Ca2+-dependent proteinase (calpain) of human neutrophils[1].
Handle region peptide, rat is a prorenin receptor antagonist, suppresses the progression of diabetic nephropathy and has anti-inflammatory in the eye.
Nedosiran sodium is a GalNAc-dsRNA conjugate designed to inhibit production of the hepatic lactate dehydrogenase (LDH) enzyme.
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.
Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[1].
CDC25B-IN-2 is a potent cdc25B inhibitor[1].
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis[1].
Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor[1].
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
NQ301 is an antithrombotic agent; inhibits collagen-challenged rabbit platelet aggregation with an IC50 of 10 mg/mL.
Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities[1].
Win-62005 is a cyclic AMP phosphodiesterase III (PDE III) inhibitor with Kis of 25 and 26 nM for rat heart and canine aorta, respectively.
Proteasome-IN-5 (compound 5) is a proteasome inhibitor[1].
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice[1][2].
Hy-146215 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.
Bempedoic acid-d5 is the deuterium labeled Bempedoic acid[1]. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2].
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1][2].
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation.
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases[1].