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Á¦¸ñ MCE) New Small Molecules for June 2021
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ÀÛ¼ºÀÏÀÚ 2021-06-09
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InhibitorsAgonists Screening Libraries
MedChemExpress - New Products May 2021
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. If you need these products, please do not hesitate to contact us via sales@MedChemExpress.com.
CAS No.: 69685-22-9
Butaprost

Research Area: GPCR/G Protein/Prostaglandin Receptor/Renal Fibrosis

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

Solubility: Solution in Methyl acetate (12.24 mM)

CAS No.: 853953-65-8

GW604714X

Research Area: Mitochondrial Metabolism/Mitochondrial Pyruvate Carrier

gw604714x structure
Highly specific and potent inhibitor of the mitochondrial pyruvate carrier (Ki<0.1 nM) and inhibits mitochondrial respiration supported by pyruvate but not other substrates.
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

CP-100356 hydrochloride structure
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 ¥ìM).
Has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1 ¥ìM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, 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

cci-007 structure
Selective inhibitor of MLL-rearranged (MLL-r), CALM-AF10 and SET-NUP214 leukemia (IC50=2.5-6.2 ¥ìM 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

acolbifene-hydrochloride structure
Active metabolite of EM800, an orally active, cancer-preventing selective estrogen receptor modulator (SERM).
Inhibits estradiol (E2)-induced transcriptional activity of ER¥á (IC50=2 nM) and ER¥â (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.
Fragment Library
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
Nature. 2021 May;593(7859):418-423.
Nature. 2021 May;593(7859):
418-423.
Science. 2021 Apr 30;372(6541):eaba8490.
Science. 2021 Apr 30;
372(6541):eaba8490.
Nat Nanotechnol. 2021 May 6.
Nat Nanotechnol. 2021 May
6.  
Nat Methods. 2021 May;18(5):528-541.
Nat Methods. 2021 May;
18(5):528-541.
Cell Signaling Pathway
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