Bio.etc Pte Ltd | [MCE]: New Small Molecules for December 2021

03 Dec [MCE]: New Small Molecules for December 2021

Posted at 09:14h 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 sales@MedChemExpress.com.

CAS No.: 1595275-62-9
Tesirine
Research Area: Drug-Linker Conjugates for ADC/Small-Cell Lung Cancer

• Antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload.
• Combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics.
• SG3199 is the released warhead component of Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines.

Solubility: DMSO : 200 mg/mL (133.63 mM; Need ultrasonic)

CAS No.: 193012-35-0
FK614
Research Area: PPARγ Agonist/Hyperglycemia/ Hypertriglyceridemia/Type 2 Diabetes

• An orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM) and functions as a PPARγ agonist with potent anti-diabetic activity in vivo.
• Has different effects on the activation of PPARγ at each stage of adipocyte differentiation.
• Used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.

Solubility: DMSO : 100 mg/mL (213.49 mM; Need ultrasonic)

CAS No.: 2172788-92-8
Inarigivir ammonium
Research Area: RIG-I Agonist/HBV Infection

• Orally bioavailable dinucleotide that significantly reduces liver hepatitis B virus (HBV) DNA in transgenic mice expressing HBV.
• Acts as a RIG-I (Retinoic acid-inducible gene-I) agonist, activates the viral sensor proteins RIG-I and NOD2, and triggers the induction of the interferon signaling cascade for antiviral defense.

Solubility: DMSO : 100 mg/mL (165.42 mM; Need ultrasonic)

CAS No.: 680199-06-8
PR-104A
Research Area: DNA Cross-Linking Agent/Cytotoxin/Acute Lymphoblastic Leukemia

• Major metabolite of PR-104, a hypoxia-selective DNA cross-linking agent and cytotoxin. • Can be metabolized to the corresponding hydroxylamine (PR-104H) and amine (PR-104M), resulting in activation of the nitrogen mustard moiety.

Solubility: DMSO : 250 mg/mL (500.71 mM; Need ultrasonic)

CAS No.: 2290608-13-6
VT103
Research Area: TEAD1 Palmitoylation Inhibitor/Malignant Pleural Mesothelioma

• Orally active and selective TEAD1 protein palmitoylation inhibitor.
• Inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD.

Solubility: DMSO : 50 mg/mL (121.83 mM; Need ultrasonic)

CAS No.: 847249-57-4
AES-350
Research Area: HDAC6 Inhibitor/Acute Myeloid Leukemia

• Potent and orally active HDAC6 inhibitor (IC50=24.4 nM; Ki=35 nM).
• Inhibits HDAC3 and HDAC8 with IC50s of 0.187 μM and 0.245 μM, respectively.
• Triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

Solubility: DMSO : 100 mg/mL (320.14 mM; Need ultrasonic)

MCE Instant Powder

MCE provides commonly used biological buffers in the form of instant powders. Using AR/GR grade raw materials, the powders are fully mixed through technological innovation and process upgrading, thus leading to stronger uniformity. The powders can be quickly dissolved into a buffer solution by adding water. Compared with traditional powders, MCE instant powders are simple to operate, eliminating the need for tedious weighing and pH adjustment steps, which can greatly save experimental time and reduce experimental errors.

Natural Products: Xanthones

Phenols are a broad class of natural products with phenolic hydroxyl groups (phenolic acids, flavonoids, xanthones, coumarins, lignans, among others), which have antioxidant and other pharmacological activities. Xanthones are a class of simple tricyclic compounds, which are mainly secondary metabolites from plants (such as mangosteen, lichen) and microorganisms (such as bacteria and fungi). These compounds have a wide range of pharmacological activities, including antihypertensive, antioxidation, antithrombotic, and anticancer activities.

Cat. No.	Drug Name	Structure	Description
HY-N0290	Mangiferin		Activator of Nrf2 that suppresses nuclear translocation of the NF-κB subunits p65 and p50. Exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and anti-inflammatory activities.
HY-N0328	Alpha-Mangostin		Inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Exerts antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects.
HY-N0087	Gambogic Acid		Antagonist of antiapoptotic Bcl-2 family proteins against Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 (IC₅₀s ranging from 0.66 to 2.02 μM). Exerts anti-cancer, anti-inflammatory, antioxidant, anti-bacterial effects.
HY-N6953	Garcinone D		STAT3 activator that increases the protein levels of p-STAT3, Cyclin D1, Nrf2, and HO-1.