SML3176

WEHI-539 hydrochloride

≥98% (HPLC)

• Synonym(e): (E)-5-(3-(4-(Aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazono)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid hydrochloride, 5-[3-[4-(Aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-4-thiazolecarboxylic acid hydrochloride, WEHI 539 hydrochloride
• Empirische Formel (Hill-System): C₃₁H₂₉N₅O₃S₂ · xHCl
• Molekulargewicht: 583.72 (free base basis)
• MDL-Nummer: MFCD28044305
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Lagerbedingungen: desiccated
• Farbe: faint yellow to dark orange
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: −20°C

Beschreibung

Biochem./physiol. Wirkung

WEHI-539 is an apoptosis inducer that selectively targets the anti-apoptotic Bcl-2 family member Bcl-XL with high affinity (KD = 0.6 nM; 500-fold over Bcl-2 and 400-fold over Bcl-W, Mcl-1 and A1) in a manner distinct from that of ABT-737. WEHI blocks Bcl-XL from targeting the BH3 domain of the pro-apoptotic family member Bim with high potency (IC50 = 1.1 nM), exhibiting no inhibitory potency against Mcl-1-BimBH3 interaction (IC50 >10 μM). WEHI-539 is shown to induce apoptosis in human and murine cultures by selectively antagonizing Bcl-XL prosurvival activity (EC50 <10 nM/Mcl-1-knockout MEF, <0.5 nM/mouse platelets, and <32 nM/human platelets).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable