Bio.etc Pte Ltd | [MCE]: New Small Molecules for April 2022

14 Apr [MCE]: New Small Molecules for April 2022

Posted at 07:16h in News by Editorial Bio.etc

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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 info@bio-etc.com.

CAS No.: 2711006-67-4
ZXH-4-130 TFA
Research Area: PROTAC CRBN Degrader/Multiple Myeloma

• Potent and highly selective PROTAC CRBN degrader which is a CRBN-VHL compound (hetero-PROTAC).
• Induces ~80% CRBN degradation at 10 nM in MM1.S cells.

Solubility: DMSO : 170 mg/mL (172.57 mM; Need ultrasonic)

DSM705 hydrochloride
Research Area: DHODH Inhibitor/Malaria

• Potent antimalarial and orally active, selective Plasmodium DHODHs inhibitor.
• Shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=95 nM), P. vivax DHODH (PvDHODH, IC50=52 nM) and Pf3D7 cells (EC50=12 nM), with no inhibition of the human enzyme.

Solubility: DMSO : 100 mg/mL (226.83 mM; Need ultrasonic)

CAS No.: 1312547-19-5
Samatasvir
Research Area: NS5A Inhibitor/HCV Infection

• Potent and orally active NS5A inhibitor of HCV replication, with EC50s of 2 to 24 pM in genotype 1 through 5 replicons.
• Selective for HCV and is not active against other DNA and RNA viruses.
• Effectively combined with other classes of direct-acting HCV antivirals, as well as IFN-α and Ribavirin.

Solubility: DMSO : 50 mg/mL (56.49 mM; Need ultrasonic)

Hcyb1
Research Area: PDE2 Inhibitor/Depression

• Highly selective, orally active PDE2 inhibitor with an IC50 of 0.57 μM for PDE2A.
• Shows over 250-fold selectivity against other recombinant PDE family members.
• Has neuroprotective and antidepressant‐like effects.

Solubility: DMSO : 62.5 mg/mL (164.28 mM; Need ultrasonic)

CAS No.: 2097117-06-9
Lu AF27139
Research Area: P2X7 Receptor Antagonist/Neuroinflammation and CNS Diseases

• Orally active, rodent-active, and CNS-penetrant P2X7 receptor antagonist (IC50s=12 and 2.4 nM for human and rat P2X7 receptor, respectively; Kis=22, 54, and 13 nM for mouse, human and rat P2X7 receptor, respectively).
• Has the potential for the research of CNS disease.

Solubility: DMSO : 125 mg/mL (251.04 mM; Need ultrasonic)

Apoptosis Detection Kit

Kit	Description
Annexin V-FITC/PI Apoptosis Detection Kit	MCE Annexin V-FITC/PI Apoptosis Detection Kit provides a rapid and convenient method to detect cell apoptosis and necrosis. After staining, live cells show little or no fluorescence (Annexin V-/PI-), early apoptosis cells show green fluorescence (Annexin V+/PI-), late apoptosis cells and necrosis cells show red and green fluorescence (Annexin V+/PI+).
Cell Cycle and Apoptosis Analysis Kit (PI staining)	MCE Cell Cycle and Apoptosis Analysis Kit (PI staining) provides a convenient method to detect cell cycle and cell apoptosis. The content of DNA is changed with the process of cell cycle. DNA can be stained by fluorescent dye, such as Propidium Iodide (PI), to measure its intensity by flow cytometry to monitor the cell cycle distribution in G1/S/G2/M phase as well as apoptosis cells with signals at sub-G1 region.

Flavonoids

Flavonoids refer to a series of compounds synthesized by connecting two benzene rings (often referred to as A ring and B ring) with three central carbons. They are called flavonoids because their structure contains ketone groups, and their color is often yellow. Flavonoids widely exists in nature. Most of them combine with saccharides to form flavonoid glycosides in plants, and few of these exist as aglycones. Generally, flavonoids can be divided into several subgroups such as flavones, dihydroflavones, chalcone and isoflavones.

Flavonoids have a wide range of activities. For example, Rutin, a common flavonoid in nature, has antioxidant, anti-inflammatory, and antiviral activities, and Silymarin derived from Silybum marianum has antiviral and anti-tumor effects.

Cat. No.	Drug Name	Structure	Description
HY-N1860	3-O-Methylquercetin		Inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. Exhibits IC₅₀s ranging from 1.6-86.9 μM for PDE isozymes (PDE1-5).
HY-N6896	Isoviolanthin		Markedly inhibits TGF-β1-mediated migration and invasion by deactivating epithelial-mesenchymal transition (EMT) via the TGF-β/Smad and PI3K/Akt/mTOR pathways in HCC cells. Exhibits no cytotoxic effects on normal liver LO2 cells.
HY-N7012	7,3′,4′-Tri-O-methylluteolin		Possesses potent anti-inflammatory effects in LPS-induced macrophage cell line mediated by inhibition of release of inflammatory mediators, NO, PGE2, and pro-inflammatory cytokines. Significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2.
HY-N2412	Irisolidone		Shows the high efficacy for volume-regulated anion channels (VRAC) blockade (IC₅₀=9.8 μM). Hepatoprotective activity.