Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene is primarily isolated from plants in the Rutaceae family, such as citrus fruits. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5)[1].
Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 is a melanotropin, a melanocyte-stimulating hormone. Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 stimulates tyrosinase and exhibits thermoregulatory effect in rats model[1][2].
Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3].
Navoximod is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
Cbl-b-IN-10 (Compound 463) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.0 nM and 3.5 nM, respectively[1].
FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
RID-F is an inhibitor of the nonpeptidic proteasome.
Plasma kallikrein-IN-4 (Example 153) is a plasma kallikrein inhibitor with an IC50 of 0.016 μM against human plasma kallikrein[1].
Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
Oxybenzone-d5 is the deuterium labeled Oxybenzone[1]. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells[2][3][4].
ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders[1].
Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
hCAIX-IN-7 (compound 6c) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 43.0, 410.6 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects[1][2][3].
Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM[1].
IDH2R140Q-IN-2 (compound 36) is an an orally active IDH2R140Q inhibitor (IC50: 29 nM). IDH2R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2R140Q (IC50: 10 nM). IDH2R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2R140Q-IN-2 can be used for research of acute myeloid leukemia (AML)[1].
Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
LAS-31180 is an inhibitor of phosphodiesterase 3, with positive inotropic and vasodilator properties.
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 nM.
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1].
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1 (PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer[1].
Suc-Ala-Ala-Ala-AMC is a peptide substrate of elastase or elastase-like[1].
TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 can be used for the research of ischemia/reperfusion injury[1].