SML3459

RBPJ Inhibitor-1

≥98% (HPLC)

• Synonym(e): 2-(2-Fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-benzamide, RIN1
• Empirische Formel (Hill-System): C₁₇H₁₄FN₃O₂
• CAS-Nummer: 2682114-39-0
• Molekulargewicht: 311.31
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD32856863
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C
• SMILES string: Fc1c(cccc1)Oc2c(ccc(c2)c3[n](ncc3)C)C(=O)N
• InChI: 1S/C17H14FN3O2/c1-21-14(8-9-20-21)11-6-7-12(17(19)22)16(10-11)23-15-5-3-2-4-13(15)18/h2-10H,1H3,(H2,19,22)
• InChI key: MFSSHRCJKRDIOL-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

RBPJ Inhibitor-1 (RIN1) is a selective inhibitor against the transcription factor RBPJ. RIN1 blocks RBPJ-SHARP transcriptional repressor complex formation, inhibits RBPJ-mediated Notch intracellular domain (NICD) transcription activity (IC50/Emax = 180 nM/82% and 190 nM/88% using Notch2 ICD or Notch3 ICD, respectively), as well as NICD-independent transcription activity of RBPJ-VP16 (IC50 = 200 nM, Emax = 81%). RIN1 inhibits Notch-driven cancer proliferation (by ~70% post 4-day 10 μM RIN1 treatment; Jurkat) and promotes muscle differentiation (0.6 μM for 4 days; C2C12 myoblasts).

Selective transcription factor RBPJ inhibitor that inhibits cancer proliferation and promotes muscle differentiation.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable