25 Jan [MCE]: New Small Molecules for January 2022
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 30,000 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 500 of the newest biochemicals per month
• Data sheet with detailed biological information
• High purity & competitive prices
• Delivery within 24 hours
CAS No.: 2621928-55-8
MRTX1133
Research Area: KRAS G12D Inhibitor/Diverse Cancers
• Inhibits mutant KRAS-dependent signal and selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
• Efficacious in a KRAS G12D mutant xenograft mouse tumor model.
Solubility: DMSO : 50 mg/mL (83.25 mM; Need ultrasonic)
Ivaltinostat formic
Research Area: HDAC Inhibitor/Prostate Cancer/Cholangiocarcinoma
• An orally active, potent hydroxamate-based pan-HDAC inhibitor with antitumor effects.
• Enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-FU, thereby decreasing cell viability and inducing apoptosis.
• Inhibits deacetylation of histone H3 and tubulin in prostate cancer cells and induces clonogenic cell death by modulating acetylation of p53 in cancer cells.
Solubility:
DMSO : 50 mg/mL (105.58 mM; Need ultrasonic)
H2O : 50 mg/mL (105.58 mM; Need ultrasonic)
CAS No.: 1352914-52-3
CR-1-31-B
Research Area: eIF4A Inhibitor/Neuroblastoma/Pancreatic Ductal Adenocarcinoma
• A synthetic Rocaglate and potent eIF4A inhibitor with anticancer and antimalarial activities.
• Exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis.
• Induces apoptosis of neuroblastoma and gallbladder cancer cells.
Solubility: DMSO : 230 mg/mL (453.18 mM; Need ultrasonic)
MRTX9768 hydrochloride
Research Area: PRMT5•MTA Inhibitor/MTAP-del Cancer
• A synthetic lethal-based orally active PRMT5•MTA inhibitor.
• Selectively inhibits symmetric dimethylarginine (SDMA) marks and shows selective antitumor activity in MTAP-del tumor cells while sparing MTAP-WT cells.
Solubility:
DMSO : 90 mg/mL (195.27 mM; Need ultrasonic)
H2O : 40 mg/mL (86.79 mM; Need ultrasonic)
CAS No.: 357425-68-4
CP-601932
Research Area: α3β4 nAChR Agonist/Alcohol Dependence
• High-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~3 μM), has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and can penetrate the CNS.
• Selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure.
Solubility: DMSO : 200 mg/mL (880.17 mM; Need ultrasonic)
CAS No.: 245520-69-8
SCH79797
Research Area: PAR1 Antagonist/Myocardial Ischemia/Reperfusion Injury
• Highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist.
• Inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 (IC50=70 nM; Ki=35 nM) and inhibits thrombin-induced platelet aggregation (IC50=3 μM).
• Limits myocardial ischemia/reperfusion injury in rat hearts.
Solubility: DMSO : 50 mg/mL (134.60 mM; Need ultrasonic)
Kinases are critical in metabolism, cell signalling, protein regulation, cellular transport, secretory processes and many other cellular pathways, which makes them key regulators of cell function. The malfunction of kinases causes a variety of human diseases. Therefore, kinases represent a class of attractive drug targets. However, the highly conserved structure of eukaryotic kinases (especially the catalytic domain) has brought great challenges to the development of highly selective kinase inhibitors. Broad profiling, for many, has become a requirement of new kinase inhibitor programs for better understanding structure/activity relationships. MCE can provide high-quality and comprehensive kinase assay panel. High-quality data on the binding affinity/activity difference between compounds and kinases can evaluate the target selectivity of compounds.
Key Features:
• Flexible and customizable kinase panel: Characteristic TK, CDK kinase profiles, 60/207/302 kinase panels and customized kinase panels.
• Various detection: TR-FRET (LANCE Ultra, LathaScreen, HTRF), fluorescence method (Kinase-Glo, ADP-Glo), Z`-LYTE, binding assay.
• Accurate detection, rapid data.
• 2,400+ compounds included, covering more than 1,000 targets and isoforms.
• 1-3 compounds with high potency and selectivity selected for each target and isoform.
• Detailed bioactive information is available.
• A concise collection of small molecule compounds with comprehensive target coverage.
• A useful tool for phenotypic screening.
Recent Publications Citing Use of MCE Products
Nat Nanotechnol. 2021 Nov;16(11):1260-1270.
Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.
Cell Metab. 2021 Dec 7;33(12):2355-2366.e8.
Cancer Cell. 2021 Nov 8;39(11):1531-1547.e10.
Cell Signaling Pathways
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