03 Feb [MCE]: New Bioactive Molecules for January 2023
MedChemExpress (MCE) offers a wide range of high quality research chemicals and biochemicals including novel bioactive compounds, dye reagents, peptides and natural compounds for laboratory and scientific use.
• Over 50,000 bioactive molecules in stock
• Target 500+ key proteins in 20+ signaling pathways
• Quality reports (LC/MS, NMR and HPLC) for each product
• Release more than 1,000 newest biochemicals per month
• Data sheet with detailed biological information
• High purity & competitive prices
CAS No.: 2488952-40-3
EEDi-5285
Research Area: EED Inhibitor/Lymphoma
• A potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 of 0.2 nM.
• Efficaciously inhibits Pfeiffer and KARPAS422 lymphoma cancer cells with IC50 values of 20 pM and 0.5 nM, respectively.
• Significantly induces tumor regression in KARPAS422 xenograft mouse models.
Solubility: DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)
CAS No.: 859525-02-3
Cadisegliatin
Research Area: Glucokinase Activator/Type 1 and 2 Diabetes
• An orally active and liver-selective glucokinase (GK) activator.
• Increases glucose metabolism in rat hepatocytes with EC50 values of 2.39 μM and 2.64 μM for lactate and glycogen, respectively.
• Reduces blood glucose, lactate and triglyceride concentrations in ob/ob mouse models with severe diabetes.
Solubility: DMSO : 125 mg/mL (274.35 mM; Need ultrasonic)
CAS No.: 371217-32-2
A-317567
Research Area: ASIC-3 Inhibitor/Depression and Pain
• A potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM.
• Dose-dependently inhibits all ASIC currents (IC50s of 2-30 µM).
• Shows fully analgesic effects in Complete Freund’s adjuvant (CFA)-induced inflammatory thermal hyperalgesia rat models.
Solubility: DMSO : 125 mg/mL (314.42 mM; Need ultrasonic)
CAS No.: 2758364-02-0
CAM833
Research Area: BRCA2-RAD51 Interaction Inhibitor/Cancer
• A selective orthosteric inhibitor of BRCA2-RAD51 interaction with a Kd of 366 nM.
• Dose-dependently decreases RAD51 nuclear foci and inhibits DNA repair.
• Induces cell-cycle arrest and cell apoptosis.
Solubility: DMSO : 125 mg/mL (236.31 mM; Need ultrasonic)
CAS No.: 1375752-78-5
BMS-984923
Research Area: mGluR5 Silent Allosteric Modulator/Alzheimer’s Disease
- An orally active and BBB penetrable mGluR5 silent allosteric modulator (SAM) with a Ki value of 0.6 nM.
- Prevents amyloid-β oligomer (Aβo) mediated toxicity and Aβo-induced signal transduction in brain slices.
Rescues memory deficits and synaptic depletion in Alzheimer’s disease transgenic mouse models.
Solubility: DMSO : 100 mg/mL (266.79 mM; Need ultrasonic)
Targeted protein degradation (TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.
Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.
MCE supplies a unique collection of 30+ molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.
MCE Isotope-labeled Compounds
| Product Name | Cas No. | Structure |
| L-Arginine-13C6, 15N4 hydrochloride |
202468-25-5
|
 |
| L-Glutamine-d5 |
14341-78-7
|
 |
Latest Publications Citing Use of MCE Products
Nature. 2022 Dec;612(7940):555-563.
Science. 2022 Dec 2;378(6623):eabo5503.
Cell. 2022 Nov 10;185(23):4347-4360.e17.
Cell. 2022 Dec 8;185(25):4801-4810.e13.
Cell Signaling Pathways
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