[MCE]: New Bioactive Molecules for December 2022

09 Dec [MCE]: New Bioactive Molecules for December 2022

MCE (MedChemExpress) provides a wide range of lifescience biochemicals, including more than 40,000 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 info@bio-etc.com.

CAS No.: 1398695-47-0
GSK2646264
Research Area: SYK Inhibitor/Inflammatory Skin Disease

• A selective and skin permeable spleen tyrosine kinase (Syk) inhibitor with a pIC50 of 7.1, and exhibits >300-fold selectivity over Aurora B.
• Has the potential for chronic spontaneous urticaria, cold urticaria, and cutaneous lupus erythematosus research.

Solubility: DMSO : 50 mg/mL (133.52 mM; ultrasonic and warming and heat to 60°C)

CAS No.: 2406278-81-5
OM-153
Research Area: Tankyrase Inhibitor/Colon Cancer  

• A potent, orally active Tankyrase 1 and Tankyrase 2 (TNKS1/TNKS2) inhibitor with IC50 values of 13 nM and 2 nM, respectively.
• Shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM cells or in COLO 320DM mouse colon carcinoma xenografts.
• Demonstrates antitumor efficacy in COLO 320DM mouse colon carcinoma and B16-F10 mouse melanoma models.

Solubility: DMSO : 100 mg/mL (196.26 mM; Need ultrasonic)

CAS No.: 2102192-68-5
Envafolimab
Research Area: PD-L1 Antibody/Advanced Solid Tumors  

• A fusion protein of a humanized single-domain anti-PD-L1 antibody fused with a human IgG1 Fc fragment.
• Blocks interaction between PD-L1 and PD-1, resulting in T cell-mediated immune response to neoplasms.
• Used in the research of advanced solid tumors, biliary tract carcinoma and sarcoma.

Solubility: Solution: 9.8 mg/mL

CAS No.: 1517965-94-4
Vornorexant
Research Area: OX1R/OX2R Antagonist/Insomnia and Sleep Apnoea Syndrome

• An orally active, dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively.
• Exhibits potent sleep-promoting effects in a rat polysomnogram study, and optimal pharmacokinetic properties with rapid Tmax and short half-lives are observed in rats and dogs.

Solubility: DMSO : ≥ 100 mg/mL (223.48 mM)

CAS No.: 2784577-71-3
RLX-33
Research Area: RXFP3 Antagonist/Metabolic Syndrome

• Selective and CNS-penetrant relaxin family peptide 3 (RXFP3) non-peptide antagonist.
• Inhibits relaxin-3-induced ERK1/2 phosphorylation, and decreases cAMP accumulation.
• Blocks the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats.

Solubility: DMSO : 125 mg/mL (270.04 mM; Need ultrasonic)

In recent years, marine natural products have become an important source for the discovery of new drugs, such as the antiviral drug Vidarabine and the anticancer drug Cytarabine derived from spongothymidine and spongouridine isolated from sponges, and the Eribulin for the treatment of breast cancer and liposarcoma is a derivative of Halichondrin B from Halichondria okadai Kadota.

Product Name	Description	Structure
Didemnin B	Shows activity against miirine B16 melanoma, P388 leukemia, and M5076 sarcoma.
Aaptamine	A competitive antagonist of α-adrenoceptor.
Jasplakinolide	A potent actin polymerization inducer with fungicidal and anti-cancer activities.
Aeroplysinin 1	Exerts anti-HIV-1, anti-inflammatory, anti-angiogenic and anti-tumor activities.
Psammaplin A	A potent inhibitor of HDAC and DNA methyltransferases.

MCE advanced magnetic beads and agarose beads:

Latest Publications Citing Use of MCE Products

Nature. 2022 Nov;611(7936):603-613.
Cell. 2022 Nov 10;185(23):4361-4375.e19.
Nat Genet. 2022 Nov;54(11):1702-1710.
Cancer Discov. 2022 Nov 4:CD-22-0535.

Cell Signaling Pathways