NSC 95397 is an inhibitor for dual-specificity phosphatases, including mitogen-activated protein kinase phosphatase-1 (MKP-1). NSC 95397 suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway[1].
A-908292 is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 38 nM (hACC2), no activity against ACC1 (IC50>30 uM).
Manoalide is a potent Phospholipase A2 (PLA2) and Phospholipase C (PLC) inhibitor. Manoalide, a sesterpenoid compound, displays anti-inflammatory and antibacterial activities[1][2][3].
Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation[1][2].
Indisulam (E 7070) is a carbonic anhydrase inhibitor and a G1-targeting agent. Indisulam causes a blockade in the G1/S transition through inhibition of the activation of both cyclin-dependent kinase 2 (CDK2) and cyclin E. Shows anti-tumor activity in human colon and lung cancer cells[1][2].
Carboxypeptidase C is a carboxypeptidase, is often used in biochemical studies. Carboxypeptidase C removes COOH-terminal lysine, arginine, and proline, as well as all other neutral, aliphatic, aromatic, and the acidic protein amino acids of a peptide chain[1].
ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.3 nM[1].
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively[1].
SBP1 peptide is a chemically synthesized 23-mer peptide fragment of the ACE2 PD α1 helix. SBP1 peptide associates with micromolar affinity to insect-derived SARS-CoV-2-RBD protein [1].
19α-Hydroxyasiatic acid, a natural triterpenoid, possesses anti-elastase activity[1].
Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects[1][2][3][8].
Z-Gly-Pro-Phe-Leu-CHO (Z-GPFL-CHO) is a tetrapeptide aldehyde that acts as a highly selective and potent proteasomal inhibitor (Ki = 1.5 µM for branched chain amino acid preferring, 2.3 µM for small neutral amino acid preferring, and 40.5 µM for chymotrypsin-like activities; IC50 = 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity)[1].
MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis[1][2].
C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1].
PythiDC is a selective collagen prolyl 4-hydroxylase (CP4H1) inhibitor with an IC50 value of 4.0 μM. PythiDC can be used as a CP4H probe and also can be used for the development of a new class of antifibrotic and antimetastatic agents[1].
Sophoraisoflavone A (Allolicoisoflavone B) is a nature product that could be isolated from Glycyrrhiza inflate. Sophoraisoflavone A is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 value of 0.80 μM. Sophoraisoflavone A can be used in research of inflammation[1].
Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1].
Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 10.2 μM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process[1].
Perindopril is a long-acting ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease.Target: ACEPerindopril is a long-acting ACE inhibitor. It is used to treat high blood pressure, heart failure or stable coronary artery disease in form of perindopril arginine (trade names include Coversyl, Coversum) or perindopril erbumine (trade name Aceon). According to the Australian government's Pharmaceutical Benefits Scheme website, based on data provided to the Australian Department of Health and Aging by the manufacturer, perindopril arginine and perindopril erbumine are therapeutically equivalent and may be interchanged without differences in clinical effect. However the dose prescribed to achieve the same effect will differ due to different molecular weights for the two forms. Perindopril is one of the most prescribed inhibitors of angiotensin converting enzyme, has a large evidence base, which allows to use it in patients with hypertension, diabetes mellitus type 2, coronary heart disease and chronic heart failure. In this review, the author focused on the evidence of organoprotecting properties of perindopril that lie outside lowering blood pressure.
Microcystin-RR (Cyanoviridin RR) is a potent and orally active protein phosphatase inhibitor. Microcystin-RR induces Apoptosis and ER stress in mice liver[1][2].
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer[1][2].
Roflumilast N-oxide is a PDE type 4 inhibitor.
LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma[1].
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
NEP-IN-2 is an inhibitor of neutral endopeptidase, used in the research of proliferation in atherosclerosis, restenosis.
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with a Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively, exhibits 10-fold more sensitive than mouse and rat IMPase[1].
Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.