HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level[1].
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].
NG-497 is a selective human adipose triglyceride lipase (ATGL) inhibitor that targets the enzymatically active patatin-like domain of human ATGL. NG-497 has potential value for tumor research[1].
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.Ic50 value:Target: Renin
Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor[1].
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].
2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM[1][2][3].
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].
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
hCAIX-IN-5 (compound 6b) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 130.7, 829.1 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
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].
Z-Leu-Leu-Tyr-COCHO is a potent chymotrypsin-like activity inhibitor with a Ki value of 3.0 nM[1].
ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF[1].
Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2].
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].
LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders[1].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].
Xanthine oxidoreductase-IN-5 is an orally active xanthine oxidoreductase (XOR) inhibitor, with an IC50 of 55 nM. Xanthine oxidoreductase-IN-5 can be used for the research of acute hyperuricemia[1].
4-Phenyl-1H-1,2,3-triazole is an IDO1 inhibitor (IC50: 60 渭M). 4-Phenyl-1H-1,2,3-triazole can be used for cancer research[1].
Naphthol AS-BR is a substrate for the histochemical demonstration of acid and alkaline phosphatase[1].
Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405)[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.
BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.
Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases[1].