Utreloxastat is a compound used for the research of the disorders including α-synucleinopathies, tauopathies, Amyotrophic lateral sclerosis (ALS), traumatic brain injury, and ischemic-reperfusion related injuries (patent WO2020081879A2, example A1)[1].
β-Lactamase-IN-6 is a β-Lactamase inhibitor that shows high antibacetrial activity.
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways[1].
RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and selective inhibitor of RUVBL1/2 ATPase with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1 and RUVBL2 are highly conserved AAA ATPases (ATPases Associated with various cellular Activities) and highly relevant to the progression of cancer. RUVBL1/2 ATPase-IN-1 has the potential for the research of cancer diseases[1].
Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes[1].
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain[1].
BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity[1][2].
Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.
H-Glu(Met-OH)-OH could induce oxidation of hydroxyl radical[1].
Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs[1].
Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
4-Methoxycinnamaldehyde (p-Methoxycinnamaldehyde), an active constituent of Agastache rugosa, exhibits cytoprotective activity against respiratory syncytial virus (RSV) in human larynx carcinoma cell line. 4-Methoxycinnamaldehyde effectively inhibits cytopathic effect of RSV with an estimated IC50 of 0.055 μg/mL[1].
5,6-Epoxyergosterol is a natural product that can be isolated from endophytic fungus Phyllosticta capitalensis[1].
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh)[1]. Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively[2].
Apomorphine is an orally active agonist of Dopamine receptor. Apomorphine can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction,,dystonia, dyspnoea, anismus and belching[1].
SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor extract from WO2015032272A1, compound 2 [1].
6-Benzylaminopurine-d5 (Benzyladenine-d5) is the deuterium labeled 6-Benzylaminopurine. 6-Benzylaminopurine is a cytokinin[1].
Esmolol-d7 hydrochloride is the deuterium labeled Esmolol hydrochloride. Esmolol hydrochloride is a beta adrenergic receptor blocker[1][2].
FASN-IN-2 is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM[1].
A potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM[1].
L-Tyrosine β-naphthylamide is a tyrosine derivative[1].
N3-Gly-Gly-OH is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity[1].
Pachysamine M (Compound 5) is a pregnane alkaloid.Pachysamine M is isolated from naturalPachysandra terminalisSieb. et Zucc[1].
Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75NTR selectively over TRKA[1].
Fluoroquinolonic acid is a bacteriostatic antibiotic. Fluoroquinolonic acid has broad-spectrum activity against Gram-positive and Gram-negative bacteria[1].
MSDC-0602K (Azemiglitazone potassium), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM[1]. MSDC-0602K modulates the mitochondrial pyruvate carrier (MPC). MSDC-0602K can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance[2]. MSDC-0602K, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide[3].
Voclosporin is a calcineurin (CN) inhibitor.