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SML2825

Sigma-Aldrich

I-BET469

≥98% (HPLC)

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Synonym(s):
5-(1-(1,3-Dimethoxypropan-2-yl)-5-morpholino-1H-benzo[d]imidazol-2-yl)-1,3-dimethylpyridin-2(1H)-one, 5-[1-[2-Methoxy-1-(methoxymethyl)ethyl]-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-1,3-dimethyl-2(1H)-pyridinone
Empirical Formula (Hill Notation):
C23H30N4O4
CAS Number:
2003197-53-1
Molecular Weight:
426.51

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (Kd in nM: BRD4 BrD1/2 = 1.5/2.9, BRD3 BrD1/2 = 2/2.3, BRD2 BrD1/2 = 2.3/2.8, BRDT BrD1/2 = 12/100, CREBBP = 37, EP300 = 49; Kd ≥4.8 μM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pKd = 8.3 or Kd = 5.0 nM by NanoBRET) and shows in vivo efficacy in a murine acute endotoxic shock model (1, 3, 10 mg/kg po. 30 min prior to LPS) and a chronic T cell-dependent immunization model (IgG suppression on day 14 = 24% and 65%, respectively, with 0.3 mg/kg or 3 mg/kg daily po.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Christopher R Wellaway et al.
Journal of medicinal chemistry, 63(2), 714-746 (2020-01-07)
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption

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