| Identification | Back Directory | [Name]
Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- | [CAS]
2682114-39-0 | [Synonyms]
Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- | [Molecular Formula]
C17H14FN3O2 | [MOL File]
2682114-39-0.mol | [Molecular Weight]
311.31 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
15.45±0.50(Predicted) | [color ]
Light yellow to light brown | [Water Solubility ]
Water: Insoluble | [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) | [InChIKey]
MFSSHRCJKRDIOL-UHFFFAOYSA-N | [SMILES]
Fc1c(cccc1)Oc2c(ccc(c2)c3[n](ncc3)C)C(=O)N |
| Hazard Information | Back Directory | [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 formationinhibits RBPJ-mediated Notch intracellular domain (NICD) transcription activity (IC50/Emax = 180 nM/82% and 190 nM/88% using Notch2 ICD or Notch3 ICDrespectively)as well as NICD-independent transcription activity of RBPJ-VP16 (IC50 = 200 nMEmax = 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 |
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