Maximin H5 is an antimicrobial peptide derived from toad Bombina maxima[1].
Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity[1][2][3].
(±)-α-Tocopherol acetate ((±)-Vitamin E acetate), is a orally active synthetic form of vitamin E. (±)-α-Tocopherol acetate is the ester of acetic acid and α-tocopherol. (±)-α-Tocopherol acetate can be used for the research of the susceptibility of farmed fish to infectious diseases[1].
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia[1].
Vandetanib is a potent inhibitor of VEGFR2 with an IC50 of 40 nM.
AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood−brain barrier (BBB) penetration[1].
BNM-III-170 TFA salt is a small-molecule CD4-mimetic compound that enhances vaccine efficacy against HIV-1 challenge in vivo; binds the HIV-1 gp120 Env and promotes conformational changes similar to those induced by CD4, exposing conserved Env elements to antibodies; synergizes with antibodies elicited by monomeric HIV-1 gp120 to protect monkeys from multiple high-dose intrarectal challenges with a heterologous simian-human immunodeficiency virus (SHIV).
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
Meloxicam sodium is a non-steroidal anti-inflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].
Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor[1].
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α[1].
HG-7-85-01-NH2 is the ligand of SNIPER(ABL)-033. SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 value of 0.3 μM[1].
EIDD-2801 is an orally bioavailable isopropylester prodrug of the ribonucleoside analog EIDD-1931. EIDD-2801 shows anti-influenza virus and coronaviruses activities. EIDD-2801 has the potential for seasonal and pandemic influenza treatment[1][2].
Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect[1][2].
PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.
Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells[1][2][3][4].
PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]
Bromodichloronitromethane is one of Halonitromethanes, which are a recently identified class of disinfection by-products (DBPs) in drinking water[1].
H-Met-His-OH is a biologically active peptide.
Debilon, a diterpene compound, is a natural product that could be isolated from the roots and rhizomes of Nardostachys chinensis[1].
JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect[1].
Sulfo-NHS-LC-LC-Biotin (Biotin-XX-SSE), a biotin reagent, is used to label the proteins exposed to the external leaflet of intact exosomes and contains a larger spacer arm between the biotin and amine reactive linker. The size of this linker helps to overcome steric hindrance and increases labeling efficiency at the crowded exosome surface[1][2].
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV)[1][2].
Cauloside A (Leontoside A) is a saponin isolated from Dipsacus asper roots. Cauloside A has potent antifungal activity[1][2].
Dodecyl gallate (Lauryl gallate) has been widely used as an antioxidant in food manufacturing, as well as in the pharmaceutical and cosmetic industries. Dodecyl gallate also is active against a highly relevant animal virus such as African swine fever virus (ASFV)[1].
Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function[1].
Trichlormethiazide is a thiazide diuretic with properties similar to those of hydrochlorothiazide.Target: OthersTrichlormethiazide is a diuretic with properties similar to those of hydrochlorothiazide. It is usually administered for the treatment of oedema (including that which is associated with heart failure, hepatic cirrhosis and corticosteroid therapy) and hypertension. In veterinary medicine, trichlormethiazide can be combined with dexamethasone to be used on horses with mild swelling of distal limbs and general bruising. Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle. This results in excretion of sodium, chloride and water, and thus acts as a diuretic [1-3].
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM[1].