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제목 [MedChemExpress ; MCE] New Small Molecules for February 2022
작성자 abbabio
작성일자 2022-02-11
조회수 307
MedChemExpress - Master of Bioactive Molecules (Inhibitors. Screening Libraries. Proteins)
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, please do not hesitate to contact us via sales@MedChemExpress.com.
CAS No.: 1957234-83-1
dBET23

Research Area: PROTAC BRD4 Degrader

dBET23 structure
•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

Sovesudil structure
•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

HM43239 structure
•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

Ladostigil hemitartrate structure
•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

Relamorelin TFA structure
•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.
Receptor FamilyReceptorCouple to G proteinSpecies
AdenosineA1Gihuman
A2AGs & Gqhuman
A2BGshuman
AdrenoceptorAlpha 1A/1B/1DGqhuman
Alpha 2A/2B/2CGihuman
Beta 1/2Gshuman
CannabinoidCB1/2Gihuman
ChemokineCCR1/2/5/7/8;
CXCR2/4		Gihuman
CholecystokininCCK1/2Gqhuman
DopamineD1/D5Gshuman
D2L/D2S/D3/D4Gihuman
Key Features:
•100+ different 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
MCE GPCR/G Protein Compound Library
MCE provides a unique collection of 1,500+ GPCRs-targeted small molecules, targeting various GPCRs such as 5-HT Receptor, Dopamine Receptor, Opioid Receptor, Adrenergic Receptors, Cannabinoid Receptor, and mGluR. MCE GPCR/G Protein Compound Library can be used in the screening for various GPCRs-related research and drug development projects.
Recent Publications Citing Use of MCE Products
Covers of Recent PublicationsCell.
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 Pathway
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