81428-01-5

Basic information

• Product Name: 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-methylethanesulfonamide
• Synonyms: 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-methylethanesulfonamide;2-(1,3-Dioxoisoindol-2-yl)-N-methylethanesulfonamide
• CAS NO: 81428-01-5
• Molecular Formula: C11H12N2O4S
• Molecular Weight: 268.28898
• Mol File: 81428-01-5.mol
• Article Data: 6

Chemical Properties

• Boiling Point: 446.0±47.0 °C(Predicted)
• Appearance: /
• Density: 1.438±0.06 g/cm3(Predicted)
• PKA: 11.20±0.40(Predicted)
• CAS DataBase Reference: 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-methylethanesulfonamide(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-methylethanesulfonamide(81428-01-5)
• EPA Substance Registry System: 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-methylethanesulfonamide(81428-01-5)

Safety Data

• HazardClass: IRRITANT
• Hazardous Substances Data: 81428-01-5(Hazardous Substances Data)

Usage

Target enzyme

Histone methyltransferase enzyme EZH2 (enhancer of zeste homolog 2).

Function

Inhibitor of EZH2.

Therapeutic potential

Anti-cancer properties, particularly in the treatment of lymphoma and other solid tumors.

Mechanism of action

Inhibits the methylation of histone H3 at lysine 27, leading to changes in gene expression and potentially inhibiting the growth and survival of cancer cells.

Current status

Under research for its potential as a targeted therapy for various types of cancer.

Upstream product

• 4443-24-7 NCS 731 
• 85-44-9 phthalic anhydride 
• 4403-36-5 2-phthalimido-ethanesulfonyl chloride 
• 74-89-5 methylamine 
• 593-51-1 methylamine hydrochloride 

Relevant articles and documents

BICYCLIC JAK INHIBITORS AND USES THEREOF

Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.

Synthesis and QSAR of Quinazoline Sulfonamides As Highly Potent Human Histamine H4 Receptor Inverse Agonists

Hit optimization of the class of quinazoline containing histamine H 4 receptor (H4R) ligands resulted in a sulfonamide substituted analogue with high affinity for the H4R. This moiety leads to improved physicochemical properties and is believed to probe a distinct H4R binding pocket that was previously identified using pharmacophore modeling. By introducing a variety of sulfonamide substituents, the H4R affinity was optimized. The interaction of the new ligands, in combination with a set of previously published quinazoline compounds, was described by a QSAR equation. Pharmacological studies revealed that the sulfonamide analogues have excellent H4R affinity and behave as inverse agonists at the human H4R. In vivo evaluation of the potent 2-(6-chloro-2-(4-methylpiperazin-1-yl)quinazoline4-amino)-N- phenylethanesulfonamide (54) (pki = 8.31 ± 0.10) revealed it to have anti-inflammatory activity in an animal model of acute inflammation.

Synthesis and biological properties of new 1β-methylcarbapenems

The synthesis and biological activity of the novel series of 1β- methylcarbapenems, 1 and 2 were described. Most compounds displayed high potent antibacterial activity. The best compound in this series, 2a (IH201; R2=NH2) showed an excellent and a broad spectrum as well as high renal DHP- I stability. It also possessed good in vivo efficacy and high safety.