Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties[1].
NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.
AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.IC50 value: 3 nM/ 0.6 nM(Ki/IC95)Target: RARγ antagonistMore information can be found in the following patent, Compound 7a.Preparation of disubstituted chalcone oximes having RARγ retinoid receptor antagonist activityBy Tsang, Kwok Yin; Sinha, Santosh; Liu, Xiaoxia; Bhat, Smita; Chandraratna, Roshantha A.From PCT Int. Appl. (2005), WO 2005066115 A2 20050721.
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 µM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation [1][2][3].
Telaprevir is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide.
Palmitic acid-1,2,3,4-13C4 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with an IC50 of ~1-3 μM[1].
Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) (IC50=5 μM). Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema (ED50=50 μg/ear)[1].
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer[1].
Debio 0932 is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
Lovastatin-d3 is deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1)[1][2][3].
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin has antispasmodic activity. Arcapillin also has moderate PTP1B inhibitory activity[1][2].
Ezatiostat hydrochloride is a glutathione analog inhibitor of glutathione S-transferase P1-1 (GSTP1-1).
Pep2-8 is a proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor, with an IC50 of 0.8 μM for PCSK9 binding to LDL receptor.
MDL12330A (RMI12330A) is an adenyl cyclase inhibitor. MDL12330A inhibits the vasopressin action on the short-circuit current (SCC). MDL12330A is also an inhibitor of cAMP phosphodiesterase[1].
Izumerogant is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM[1][2].
Metolazone(Zaroxolyn) is primarily used to treat congestive heart failure and high blood pressure.Target: OthersMetolazone is a thiazide-like diuretic marketed under the brand names Zytanix from Zydus Cadila, Zaroxolyn, and Mykrox. It is primarily used to treat congestive heart failure and high blood pressure. Metolazone indirectly decreases the amount of water reabsorbed into the bloodstream by the kidney, so that blood volume decreases and urine volume increases. This lowers blood pressure and prevents excess fluid accumulation in heart failure. Metolazone is sometimes used together with loop diuretics such as furosemide or bumetanide, but these highly effective combinations can lead to dehydration and electrolyte abnormalities.Metolazone and the other thiazide diuretics inhibit the function of the sodium-chloride symporter, preventing sodium and chloride, and therefore water too, from leaving the lumen to enter the tubule cell. As a result, water remains in the lumen and is excreted as urine, instead of being reabsorbed into the bloodstream. Since most of the sodium in the lumen has already been reabsorbed by the time the filtrate reaches the distal convoluted tubule, thiazide diuretics have limited effects on water balance and on electrolyte levels. Nevertheless, they can be associated with low sodium levels, volume depletion, and low blood pressure, among other adverse effects.
Protizinic acid is an orally active non-steroidal antiinflammatory agent with antiinflammatory and antipyretic activity. Protizinic acid inhibits phospholipase A2 (PLA2) activity, and the IC50 value is 210 μM[1][2].
BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM[1].
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
Zonisamide-d4 (AD 810-d4) is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease[1][2].
MMP2-IN-3 (compound 2) is a potent MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 31 μM. MMP2-IN-3 also shows inhibitory activity against MMP-9 and MMP-8, with IC50 values of 26.6, and 32 μM, respectively[1].
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1][2][3][4].
16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy[1].
HIV-1 integrase inhibitor ((Z)-4-(3-(azidomethyl)phenyl)-2-hydroxy-4-oxobut-2-enoic acid) is uesful for anti-HIV.
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity[1].