E1036

116-9e

≥98% (HPLC), powder

• Synonyme(s) : 116-9e, 4-[1,1′-Biphenyl]-4-yl-3,4-dihydro-6-methyl-2-oxo-5-[(phenylmethoxy)carbonyl]-1(2H)-pyrimidinehexanoic acid
• Formule empirique (notation de Hill) : C₃₁H₃₂N₂O₅
• Numéro CAS: 831217-43-7
• Poids moléculaire : 512.60
• NACRES: NA.77
• PubChem Substance ID: 329798875
• UNSPSC Code: 12352200
• MDL number: MFCD18632539
• Assay: ≥98% (HPLC)
• Form: powder

Propriétés

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to off-white
• solubility: DMSO: >20 mg/mL
• storage temp.: 2-8°C
• SMILES string: CC1=C(C(NC(=O)N1CCCCCC(O)=O)c2ccc(cc2)-c3ccccc3)C(=O)OCc4ccccc4
• InChI: 1S/C31H32N2O5/c1-22-28(30(36)38-21-23-11-5-2-6-12-23)29(32-31(37)33(22)20-10-4-9-15-27(34)35)26-18-16-25(17-19-26)24-13-7-3-8-14-24/h2-3,5-8,11-14,16-19,29H,4,9-10,15,20-21H2,1H3,(H,32,37)(H,34,35)
• InChI key: GHFQWLNXJMUCGC-UHFFFAOYSA-N

Description

Application

116-9e has been used as an inhibitor of heat shock protein 70 (Hsp70) co-chaperone HDJ2 (human Ydj1/DNAJA1) to study the influence of HDJ2 on the regulation of ribonucleotide reductase (RNR) activity in HEK293 cells. It has also been used as an Hsp70 inhibitor to study the effect of Hsp70 chaperone on b5‐ops glycosylation in the side populations (SP) HeLa cells.

Biochem/physiol Actions

116-9e is a dihhydropyrimidine compound.

116-9e is a blocker of Hsp40-Hsp70 binding thereby inhibiting the chaperone activity of Hsp70-Hsp40. The Hsp40 family of co–chaperones binds to Hsp70 through a conserved J–domain. It is believed that 116-9e inhibits chaperone functions by preventing Hsp70–Hsp40 complex assembly.

The same compound by a different name, MAL2-11B, has been found to inhibit the activity of a viral J-domain protein, large tumor antigen (TAg). MAL2-11B inhibited both TAg′s endogenous ATPase activity and the TAg-mediated activation of Hsp70.

116-9e is a blocker of Hsp40-Hsp70 binding.

Informations sur la sécurité

• Pictogrammes: GHS06,GHS09
• Mot-clé: Danger
• Mentions de précaution: P273 - P301 + P310 + P330
• Hazard Classifications: Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1
• Que se passe-t-il ?: WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Codes de danger: H301,H410
• Classe de stockage: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects