Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-

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