SML3865

BAY-805

≥98% (HPLC)

• Synonym(e): BAY 805, BAY805, N-[(1R)-1-[[5-[(4-Cyanophenyl)methyl]-1,3,4-thiadiazol-2-yl]-carbamoyl]-3-methyl-butyl]-1-(trifluoromethyl)-cyclohexanecarboxamide
• Empirische Formel (Hill-System): C₂₄H₂₈F₃N₅O₂S
• CAS-Nummer: 2925481-88-3
• Molekulargewicht: 507.57
• MDL-Nummer: MFCD35067584
• UNSPSC-Code: OTC2302420

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C

Beschreibung

Biochem./physiol. Wirkung

Potent and selective dual USP21 deubiquitinase (DUB) inhibitor with anti-cancer efficacy.

BAY-805 is a higly potent and selective USP21 deubiquitinase (DUBs) inhibitor (IC50 (Emax) = 6 nM (95%) by HTRF assay, 2 nM (87%) by Ub-Rh110 assay; Kd = 2.2 nM by SPR-based competition assay; 50/53% inhibition of USP10/USP22 at 10 µM, <31% inhibition against other DUBs) that effectively upregulates cellular NF-κB activation (7-fold increase at 10 µM 20h post BAY-805 treatment by HEK293T-based reporter assay) with good target engagement (EC50 = 17 nM by USP21 HiBiT CESTA assay).