Bio.etc Pte Ltd | [MCE]: NEW SMALL MOLECULES FOR JUNE 2021

10 Jun [MCE]: NEW SMALL MOLECULES FOR JUNE 2021

Posted at 04:27h in News by Editorial Bio.etc

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MCE (MedChemExpress) provides a wide range of lifescience biochemicals, including more than 25,000 bioactive compounds, dye reagents, peptides and natural compounds for laboratory and scientific use.

CAS No.: 69685-22-9
Butaprost
Research Area: GPCR/G Protein/Prostaglandin Receptor/Renal Fibrosis

• Selective prostanoid EP2 receptor agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor.
• Attenuates fibrosis by hampering TGF‐β/Smad2 signalling and can be used for the research of renal fibrosis

Solubility: DMSO : 100 mg/mL (214.32 mM; Need ultrasonic)

CAS No.: 344900-92-1
GW604714X
Research Area: Mitochondrial Metabolism/Mitochondrial Pyruvate Carrier

• Highly specific and potent inhibitor of the mitochondrial pyruvate carrier (K_i
• Inhibits L-lactate transport by the plasma membrane monocarboxylate transporter MCT1.

Solubility: DMF : 5.26 mg/mL (11.16 mM; Need ultrasonic and warming)

CAS No.: 1031496-06-6
CIM0216
Research Area: TRP Channel/TRPM3/Neurogenic Inflammation

• A synthetic TRPM3 ligand and acts as a potent and selective agonist of TRPM3.
• Acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro.
• Powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research.

Solubility: DMSO : 35 mg/mL (100.75 mM; Need ultrasonic and warming)

CAS No.: 1207660-00-1
Indophagolin
Research Area: Autophagy/P2X Receptor/Breast Cancer

• Potent inhibitor of autophagy (IC₅₀=140 nM) that antagonizes the P₂X₄, P₂X₁, P₂X₃ as well as the Gq-protein-coupled P₂Y₄, P₂Y₆, and P₂Y₁₁ receptors (IC₅₀ ranging from 2.4 to 15.4 μM).
• Has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1 μM) and a moderate effect on receptors 5-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇.

Solubility: DMSO : 250 mg/mL (477.33 mM; Need ultrasonic and warming)

CAS No.: 939228-52-1
CCI-007
Research Area: Mitochondrial Dysfunction/Leukemia

• Selective inhibitor of MLL-rearranged (MLL-r), CALM-AF10 and SET-NUP214 leukemia (IC₅₀=2.5-6.2 μM in sensitive cells).
• Induces a caspase-dependent apoptosis with mitochondrial depolarization. Alters the characteristic MLL-r gene expression signature in sensitive cells with downregulation of the expression of HOXA9, MEIS1, CMYC and BCL2.

Solubility: DMSO : 83.33 mg/mL (247.74 mM; Need ultrasonic)

CAS No.: 252555-01-4
Acolbifene hydrochloride
Research Area: Estrogen Receptor/ERR/Breast Cancer

• Active metabolite of EM800, an orally active, cancer-preventing selective estrogen receptor modulator (SERM).
• Inhibits estradiol (E₂)-induced transcriptional activity of ERα (IC₅₀=2 nM) and ERβ (IC₅₀=0.4 nM).
• Exerts a potent and pure antiestrogenic action in the mammary gland and uterus.

Solubility: DMSO : 180 mg/mL (364.36 mM; Need ultrasonic)

MCE Ion Channel Screening Service

Patch clamp electrophysiology is the gold standard for ion channel studies. High-throughput identification of compound ion channel efficacy, potency, specificity, or potential for off-target effects is a critical step in early drug discovery. MCE offers high-throughput fluorescence-based assays, automated patch clamp electrophysiology assays as well as manual patch assays to identify the most promising candidates.

Kinase and Phosphatase Inhibitor Library

Protein phosphorylation is a key post-translational modification that involves the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc. Kinases and phosphatases contribute to the regulation of protein phosphorylation homeostasis in the cell.

MCE kinase inhibitor library contains 1800+ kinase inhibitors and phosphatase inhibitor library contains 80+ phosphatase inhibitors. These two libraries are important tools for protein phosphorylation research and drug discovery used to target a variety of diseases.

Recent Publications Citing Use of MCE Products