16 Feb [MCE]: New Small Molecules for February 2022
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. If you need these products, do not hesitate to contact us via info@bio-etc.com .
CAS No.: 1957234-83-1
dBET23
Research Area: PROTAC BRD4 Degrader
• Highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein.
• Occupies the canonical binding sites on CRBN and BRD4BD1 for Thalidomide and JQ1, respectively.
Solubility: DMSO : 170 mg/mL (192.01 mM; Need ultrasonic)
CAS No.: 1333400-14-8
Sovesudil
Research Area: ROCK Inhibitor/Glaucoma
• Potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively.
• Lowers intraocular pressure (IOP) without inducing hyperemia.
Solubility: DMSO : 100 mg/mL (245.43 mM; Need ultrasonic)
CAS No.: 2294874-49-8
HM43239
Research Area: FLT3 Inhibitor/Acute Myeloid Leukemia
• Orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively.
• Potently inhibits phosphorylation of SYK, STAT3 and STAT5, inhibits the proliferation and induces the apoptosis of leukemic stem cell marker-expressing KG1a cells (CD34+/CD38- cells).
Solubility: DMSO : 125 mg/mL (249.47 mM; Need ultrasonic)
CAS No.: 209394-46-7
Ladostigil hemitartrate
Research Area: Cholinesterase/MAO Inhibitor/Alzheimer’s Disease/Depression
• Orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively.
• A neuroprotective agent used for the research of Alzheimer’s disease and depression.
• Has antioxidant and anti-inflammatory activities and prevents the loss of episodic and spatial memory in aging rats.
Solubility: DMSO : 50 mg/mL (71.97 mM; Need ultrasonic)
Relamorelin TFA
Research Area: GHS-R Agonist/Gastric/Intestinal Dysmobility Disorders
• A pentapeptide ghrelin analog and a potent agonist of ghrelin and growth hormone secretagogue receptor (GHS-R).
• Binds selectively to GHS-1a with a greater affinity (Ki=0.42 nM) than natural ghrelin (1.12 nM).
• Increases growth hormone levels and accelerates gastric emptying.
Solubility: H2O : 100 mg/mL (110.50 mM; Need ultrasonic)
GPCR Bioassay Screening Services
G protein-coupled receptors (GPCRs) play important roles in cellular physiology and they are popular drug targets for various diseases. About 40% of approved drugs on the market belong to this category. Drug candidate screening and profiling is a critical step in GPCR-centered drug discovery. MCE can provide high-quality and comprehensive GPCR Bioassay Services. Through efficient, rapid, and accurate experimental services, MCE can speed up the discovery and development of new drugs for customers and maximize the benefits of customers.
Table 1. Part of MCE GPCR Functional Cell Lines.
• Customized GPCR stable cell line construction
• High-throughput screening platform: FLIPR PENTA (EMC-CD), BMG PHERAstarFSX, BIOTEK multifunctional plate reader
• Multiple assay formats including calcium flux, cAMP determination, and Luciferase reporter gene assays
• Stringent QC standards with competitive prices
GPCR/G Protein Compound Library
Recent Publications Citing Use of MCE Products
Cell. 2022 Jan 6;185(1):158-168.e11.
Adv Mater. 2021 Nov;33(45):e2104594.
Immunity. 2021 Dec 24;S1074-7613(21)00535-5.
J Extracell Vesicles. 2022 Jan;11(1):e12185.
Cell Signaling Pathways
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