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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
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

Fc1c(cccc1)Oc2c(ccc(c2)c3[n](ncc3)C)C(=O)N

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)

InChI key

MFSSHRCJKRDIOL-UHFFFAOYSA-N

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).
Selective transcription factor RBPJ inhibitor that inhibits cancer proliferation and promotes muscle differentiation.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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