SML3459
RBPJ Inhibitor-1
≥98% (HPLC)
Synonym(s):
2-(2-Fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-benzamide, RIN1
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About This Item
Empirical Formula (Hill Notation):
C17H14FN3O2
CAS Number:
Molecular Weight:
311.31
MDL number:
UNSPSC Code:
12352200
Recommended Products
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
Certificates of Analysis (COA)
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Rani Ojha et al.
Developmental cell, 57(2), 260-276 (2022-01-26)
Metabolic flexibility is a hallmark of many cancers where mitochondrial respiration is critically involved, but the molecular underpinning of mitochondrial control of cancer metabolic reprogramming is poorly understood. Here, we show that reverse electron transfer (RET) through respiratory chain complex
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