Bio.etc Pte Ltd | [MCE]: New Small Molecules for October 2021

07 Oct [MCE]: New Small Molecules for October 2021

Posted at 08:50h in News by Editorial Bio.etc

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MCE (MedChemExpress) provides a wide range of lifescience biochemicals, including more than 30,000 bioactive compounds, dye reagents, peptides and natural compounds for laboratory and scientific use.

CAS No.: 2381268-71-7
OP-5244
Research Area: CD73 Inhibitor/Cancer Immunology

• • Potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM.
• Reverses immunosuppression through blocking of adenosine production and has the potential for the cancer research.

Solubility: DMSO : 250 mg/mL (464.78 mM; Need ultrasonic)

CAS No.: 2143542-28-1
2BAct
Research Area: eIF2B Activator/Neurological Defects

• Potent, highly selective, CNS-permeable, and orally active eIF2B (eukaryotic initiation factor 2B) activator (EC50=33 nM).
• Prevents neurological defects caused by a chronic integrated stress response.

Solubility: DMSO : 250 mg/mL (567.15 mM; Need ultrasonic)

CAS No.: 396091-76-2
Pasireotide acetate
Research Area: Somatostatin Agonist/Acromegaly and Cushing’s Disease

• A long-acting cyclohexapeptide somatostatin analogue with high binding affinity for somatostatin receptor subtypes (pKis of 8.2, 9.0, 9.1,
• Potently suppresses GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing’s disease.

Solubility: DMSO : 100 mg/mL (90.31 mM; Need ultrasonic)

Lesogaberan hydrochloride
Research Area: GABAB Receptor Agonist/Gastroesophageal Reflux Disease

• Potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human GABAB receptor.
• Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.
• Inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

Solubility: DMSO : 240 mg/mL (1351.81 mM; Need ultrasonic)

CAS No.: 2421119-60-8
JKE-1674
Research Area: GPX4 Inhibitor/Ferroptosis/Multiple Cancers

• An active metabolite of the GPX4 inhibitor ML-210 and an orally active glutathione peroxidase 4 (GPX4) inhibitor.
• Shows LOX-IMVI cell-killing effects and is completely rescued by ferroptosis inhibitors.

Solubility: DMSO : 100 mg/mL (221.58 mM; Need ultrasonic)

CAS No.: 866933-46-2
Velusetrag
Research Area: 5-HT4 Receptor Agonist/Gastrointestinal Motility Disorders

• Potent, orally active, and selective 5-HT4 receptor agonist (pKi of 7.7) with high intrinsic activity.
• For the research of gastrointestinal motility disorders including gastroparesis.

Solubility: DMSO : 100 mg/mL (198.16 mM; Need ultrasonic)

Anti-Flag Affinity Gel

MedChemExpress (MCE) Anti-Flag Affinity Gel is a purified mouse IgG2b monoclonal antibody covalently attached to agarose Sepharose 4B. With high protein-binding capacity and stability, this product is ideal for high performance purification or immunoprecipitation (IP) of Flag-tagged proteins expressed in E.coli, yeast, insect and mammalian expression systems.

PolyFast Transfection Reagent

MedChemExpress (MCE) PolyFast Transfection Reagent consists of cationic polymers and can introduce nucleic acids (DNA or RNA) into eukaryotic cells. PolyFast Transfection Reagent has high-efficiency, low-toxicity transfection of many cell types, including some hard-to-transfect cells.

PROteolysis TArgeting Chimera (PROTAC)

PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a “three-unit” polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

MedChemExpress (MCE) provides 3,000+ PROTAC products (PROTAC and its building blocks), as well as one-stop services for design, synthesis, activity screening and structural optimization of PROTAC. Each service can also be customized independently.