Amicarbazone (also known as BAY-MKH3586 and BAY314666) is a novel, potent inhibitor of photosynthetic electron transport via binding to the Qb domain of photosystem II (PSII); Amicarbazone is a new triazolinone herbicide with a broad spectrum of weed control. The phenotypic responses of sensitive plants exposed to amicarbazone include chlorosis, stunted growth, tissue necrosis, and […]

Protein degrader 1 TFA (trifluoroacetic acid salt) is a novel and potent small molecule ligand for VHL (Von Hippel-Lindau), an E3 ligase which has been targeted in many PROTACs (proteolysis-targeting chimeras). Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use […]

ML-290, a 2-acetamido-N-phenylbenzamide analog, is a novel potent, selective and orally bioactive agonist of the relaxin/insulin-like family peptide receptor (RXFP1) and an activator of anti-fibrotic genes with an EC50 of 94 nM. It was identified from a dose responsive quantitative high throughput screen (qHTS) of >350,000 compounds against a human relaxin/insulin-like family peptide receptor (RXFP1) […]

ML132 (also known as NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM. It contains a nitrile-containing propionic acid moiety as an electrophile for covalent attack by the active-site cysteine residue of caspase 1. The syntheses of several cyanopropanate-containing small molecules based on the optimized peptidic scaffold of […]

LGD-4033 (also known as VK-5211 and Ligandrol) is a novel, potent and selective androgen receptor modulator (SARM) and is being investigated by Ligand Pharmaceuticals for treatment of conditions such as muscle wasting and osteoporosis. LGD-4033 was safe, had favorable pharmacokinetic profile.

GSK-2336805 (also known as GSK-805; GSK2336805; JNJ-56914845) is a novel and potent inhibitor of HCV NS5A. It has the potential for the treatment of HCV infection. Nonstructural protein 5A (NS5A) is an essential component of the HCV replication complex. The NS5a protein interacts with other key viral products (NS4B, NS5B, RNA) and host cell proteins […]

ML-7 (ML7) is a potent Myosin light chain kinase (MLCK) inhibitor with IC50 of 300 nM and IC50>10 μM for MLCK and TRPC6 channel respectively. Myosin light chain kinase (MLCK) plays a pivotal role in regulation of cellular functions, the evidence often relying on the effects of extracelluarly administered drugs such as ML-9. Here we […]

MK-6240 is a novel positron emission tomography (PET) tracer for detecting neurofibrillary tangles (NFTs). It exhibits high specificity and selectivity for binding to NFTs. Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases including Alzheimer’s disease. In vivo detection of NFTs using PET imaging […]

AZD6482 S-isomer, is an isomer of AZD6482 which is a novel, potent, selective and ATP competitive PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and is 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Genetic approaches have shown that the p110β isoform of class Ia phosphatidylinositol-3-kinase (PI3K) is essential […]

NSC77674 (also known as PIH or Pyridoxal isonicotinoyl hydrazone) is is a novel, potent, lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and in vivo in rats and mice. As iron is a crucial component of metabolic pathways involved in DNA synthesis, cancerous cells have a […]