Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
- Product Name
- Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
- CAS No.
- 2682114-39-0
- Chemical Name
- Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
- Synonyms
- RBPJ inhibitor RIN1;RIN1 (RBPJ Inhibitor-1);RBPJ Inhibitor-1 (RIN1) ，S3376;RBPJ Inhibitor-1, 10 mM in DMSO;Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
- CBNumber
- CB610557921
- Molecular Formula
- C17H14FN3O2
- Formula Weight
- 311.31
- MOL File
- 2682114-39-0.mol
Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Property
- Boiling point:
- 454.9±45.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 62 mg/mL (199.16 mM);Ethanol: 62 mg/mL (199.16 mM)
- pka
- 15.45±0.50(Predicted)
- form
- Solid
- color
- Light yellow to light brown
- Water Solubility
- Water: Insoluble
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Chemical Properties,Usage,Production
Uses
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation[1].
Biological Activity
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).
References
[1] Cecilia Hurtado, et al. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci Rep. 2019 Jul 25;9(1):10811. DOI:10.1038/s41598-019-46948-5
Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Preparation Products And Raw materials
Raw materials
Preparation Products
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