Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2].
Longispinogenin, a oleanane, can be isolated from the nonsaponifiable lipids of the flower extracts of Compositae plants. Longispinogenin exhibits inhibitory effect on TPA (HY-18739)-induced inflammation in mice[1].
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation[1].
Cloprednol is an orally active synthetic glucocorticoid. Cloprednol has anti-inflammatory activity, and can be used in the research of asthma[1].
Ginsenoside Rh1 is isolated from the root of Panax Ginseng. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
SP 4206 is a high-affinity (Kd=70 nM) small molecule that blocks blocks the binding of the IL-2α receptor (IL-2Rα) to IL-2; targets virtually the same critical "hot-spot" residues on IL-2 that drive binding of IL-2Rα.
Linderane, isolated from the root of Lindera strychnifolia, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp[1].
Sulfogaiacol is a antitussive agent. Sulfogaiacol is used for acute respiratory tract infections, cough and other conditions.
RXFP1 receptor agonist-1 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-1 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 300 nM[1].
Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively[1][2].
KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses[1].
Ferrous bisglycinate is an orally active iron fortificants and therapeutic iron supplements. Ferrous bisglycinate can be used for the research of iron deficiency anemia[1][2].
PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1[1].
CCR1 antagonist 8 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist clinical candidate, with an IC50 of 1.8 nM in Ca2+ flux assay[1].
Protease-Activated Receptor-2 Activating Peptide is an agonist of Protease-Activated Receptor-2 (PAR-2).
Keap1-Nrf2-IN-5 (compound 1) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 4.1 µM, Kd of 3.7 µM[1].
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells[1][2].
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids[1][2].
Trachelogenin ((-)-Trachelogenin) is an HCV entry inhibitor without genotype specificity, and with low cytotoxicity. Trachelogenin inhibits HCVcc infection and HCVpp cell entry in a dose-dependent manner with an IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively. Trachelogenin exhibits effective antiviral, anti-inflammatory and analgesic effects[1].
Ethoxyquin dimer is a dimer of Ethoxyquin (HY-B1425). Ethoxyquin dimer is an antioxidant. Ethoxyquin dimer can more readily accumulate in liver and adipose tissue compared with Ethoxyquin. Ethoxyquin above 10?mg/kg shows hepatotoxicity in mice[1].
SH-42 is a potent and selective inhibitor of human Δ24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice[1].
UP202-56 is an adenosine analogue, which is an adenosinergic agonist.
Brp-201 is considered as a promising therapeutic target for the next generation of anti-inflammatory drugs in the treatment of inflammatory diseases. It is a new, effective and selective inhibitor of mPGES-1 with an IC50 value of 0.42 μM.
IK-862 is a selective inhibitor of TACE (ADAM17).
Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight.Target: CYP (cytochrome P-450)Methoxsalen is a drug used to treat psoriasis, eczema, vitiligo, and some cutaneous lymphomas in conjunction with exposing the skin to UVA light from lamps or sunlight. Methoxsalen modifies the way skin cells receive the UVA radiation, allegedly clearing up the disease. The dosage comes in 10 mg tablets, which are taken in the amount of 30 mg 75 minutes before a PUVA (psoralen + UVA) light treatment. Chemically, methoxsalen belongs to a class of organic natural molecules known asfuranocoumarins. They consist of coumarin annulated with furan.Administration of intra peritoneal (ip) methoxsalen significantly increased nicotine's Cmax, prolonged the plasma half-life (fourfold decrease) of nicotine, and increased its area under the curve (AUC) compared with ip vehicle treatment. Methoxsalen pretreatment prolonged the duration of nicotine-induced antinociception and hypothermia (15mg/kg, po) for periods up to 6- and 24-hr postnicotine administration, respectively.
HPK1-IN-17 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-17 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 73)[1].
Cinchophen is an effective method for producing chronic peptic ulcer in dogs.
Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA ligase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity[1][2][3].
Aminophylline is a competitive nonselective phosphodiesterase inhibitor that is used to treat airway obstruction from asthma or COPD.Target: PhosphodiesteraseAminophylline is a compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate. Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD. It is used off-label as a reversal agent during nuclear stress testing. Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor.Adenosine is an endogenous extracellular messenger that can regulate myocardial oxygen needs. It acts through cellular surface receptors which effect intracellular signalling pathways to increase coronary artery blood flow, slow heart rate, block atrioventricular node conduction, suppress cardiac automaticity, and decrease β-adrenergic effects on contractility. Adenosine also antagonizes chronotropic and ionotropic effects of circulating catecholamines. Overall, adenosine decreases the heart's rate and force of contraction, which increases blood supply to the cardiac muscle. Given specific circumstances this mechanism (which is intended to protect the heart) may cause atropine-resistant refractory bradyasystole. Adenosine's effects are concentration-dependent. Adenosine's receptors are competitively antagonized by methylxanthines such as aminophylline. Aminophylline competitively antagonizes the cardiac actions of adenosine at the cell surface receptors. Thus, it increases heart rate and contractility.
TREM-1 inhibitory peptide GF9 (Human TREM-1(213-221)) is a ligand‐independent TREM‐1 inhibitory nonapeptide GF9 that can blunt excessive inflammation caused by rheumatoid arthritis (RA)[1].