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SML3459

Sigma-Aldrich

RBPJ Inhibitor-1

≥98% (HPLC)

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Synonym(s):
2-(2-Fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-benzamide, RIN1
Empirical Formula (Hill Notation):
C17H14FN3O2
CAS Number:
Molecular Weight:
311.31
MDL number:

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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