Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease. Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 can be used to test HIV-1 protease activity[1].
H-Tyr-Tyr-OH (L-Tyrosyl-L-tyrosine) is an antihypertensive peptide. H-Tyr-Tyr-OH inhibits angiotensin I-converting enzyme (ACE) with an IC50 value of 0.028 mg/mL. H-Tyr-Tyr-OH can be used for the research of high blood pressure[1][2].
6BrCaQ is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity. 6BrCaQ can be used in the synthesis of 6BrCaQ-TPP conjugates[1].
Arg-Arg-AMC is a highly selective substrate of Cathepsin B. Arg-Arg-AMC can be used to cathepsin B activity assay in cancer cells, while cathepsin B is assocaited with cell invasive and metastatic phenotype in numerous types of cancer[1].
CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM[1].
VU0155069 (CAY10593), compound 69, is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro[1]. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays[2].
WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. WNK1-IN-1 inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for the research of blood pressure regulation and cancer[1].
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice[1][2].
h-NTPDase-IN-5 (compound 3b) is a pan-inhibitor of NTPDase with IC50s of 1.10 μM (h-NTPDase1), 44.73 μM (h-NTPDase2), 26.14 μM (h-NTPDase3), 0.32 μM (h- NTPDase8).
SQ 32602 is a cathepsin E inhibitor.
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator[1][2].
KGP-94 is a potent, selective cathepsin L inhibitor with IC50 of 189 nM, shows no significant inhibitory effect on cathepsin B (IC50>10 uM); significantly decreases the activity of cathepsin L toward human type I collagen, and impeds both migration and invasion of MDA-MB-231 human breast cancer cells; shows tumor growth retardation in a C3H mouse mammary carcinoma model.
Ro 41-0960 is a selective catechol-O-methyltransferase(COMT) inhibitor[1].
Chlorogenic acid butyl ester, a caffeoylquinic acid, is a potent melanogenesis inhibitor. Chlorogenic acid butyl ester inhibits the expression of microphtalmia-associated transcription factor (MITF), tyrosinase, tyrosinerelated protein 1 (TRP-1), and TRP-2. Chlorogenic acid butyl ester also shows antioxidant activity[1].
IHVR-11029 is a small molecule inhibitor of ER α-glucosidases, with an EC50 of 0.09 μM[1].
Phosphoramidon disodium is a metalloprotease inhibitor. Phosphoramidon inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively.
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 inhibits the formation of invasive pseudopodia and increases the level of PAI-2 in vitro. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC)[1][2].
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation[1][2][3].
Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent[1][2].
Coptisine Sulfate is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM[1].
Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi[1][2][3].
VM4-037 can be used for the synthesis of VM4-037(18F). VM4-037(18F) is a fluorinated PET imaging agent for carbonic anhydrase IX[1].
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).IC50 value: 2 nM(Ki)Target: RARα antagonistAGN 196996 shows no activity in transactivation assays, but instead block the gene transcriptional activity induced by ATRA and other RAR agonists.
BMS-767778, a DPP-4 inhibitor, is used potentially for the treatment of type 2 diabetes.
H-Ile-Pro-Pro-OH hydrochloride, a milk-derived peptide[1], inhibits angiotensin-converting enzyme (ACE)[1] with an IC50 of 5 μM[2]. Antihypertensive tripeptides[1].
20(21)-Dehydrolucidenic acid A is a triterpenoid isolated from the fruiting body of the fungus Ganoderma sinense. 20(21)-Dehydrolucidenic acid A has weak anti-HIV-1 protease activity[1].
Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.IC50 value: 0.1 nM(Ki) [1]Target: 15-PGDHin vitro: SW033291 inhibition of 15-PGDH was noncompetitive versus PGE2 over concentrations up to 40 μM PGE2. SW033291 also demonstrated selective high-affinity interaction with 15-PGDH in thermal denaturation assays. Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with 50% of maximal stimulation (EC50) at ~75 nM [1].in vivo: mice injected with SW033291 closely phenocopied 15-PGDH knockout mice, with 10 mg per kg of weight (mg/kg) SW033291 inducing a twofold increase in PGE2 levels in bone marrow, colon, lung, and liver. Mice injected with SW033291 at 20 mg/kg daily for 7 days showed equivalent daily weights and activity as mice injected with vehicle-control and showed no adverse changes in blood counts or serum chemistry [1].
Enpp-1-IN-8 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-8 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51)[1].