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SML2335

Sigma-Aldrich

IACS-9571 trifluoroacetate salt

≥98% (HPLC)

Sinonimo/i:

IACS 009571-001-4 trifluoroacetate, N-(6-(3-(4-(Dimethylamino)butoxy)-5-propoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-3,4-dimethoxybenzenesulfonamide trifluoroacetate, N-[6-[3-[4-(Dimethylamino)butoxy]-5-propoxyphenoxy]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide trifluoroacetate

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About This Item

Formula empirica (notazione di Hill):
C32H42N4O8S · CF3CO2H
Numero CAS:
1883598-69-3
Peso molecolare:
756.79
Codice UNSPSC:
12352200

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=S(C1=CC=C(C(OC)=C1)OC)(NC2=C(C=C(C3=C2)N(C(N3C)=O)C)OC4=CC(OCCC)=CC(OCCCCN(C)C)=C4)=O.FC(F)(C(O)=O)F

Azioni biochim/fisiol

IACS-9571 is a dimethylamine analogue.
IACS-9571 is a high-affinity, potent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nM, BAZ2B/TAF1 BrD2/BRD4 BrD1,2 Kd = 0.4/1.8/>10 μM by DiscoveRx; ≤63% binding inhibition of 25 other BrDs at 1 μM). IACS-9571 potently blocks H3K23Ac peptide from TRIM24 BrD binding (IC50 = 7.6 nM) and displaces ectopically expressed TRIM24 PHD-BrD from endogenous histone H3 in 2-hr 5 μM SAHA-stimulated HeLa cells (IC50 = 50 nM). When adiministered in mice, IACS-9571 exhibits good pharmacokinetics and oral availability in vivo (F = 29%, 10 mg/kg p.o.).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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Wylie S Palmer et al.
Journal of medicinal chemistry, 59(4), 1440-1454 (2015-06-11)
The bromodomain containing proteins TRIM24 (tripartite motif containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are involved in the epigenetic regulation of gene expression and have been implicated in human cancer. Overexpression of TRIM24 correlates with
Structure-guided design of IACS-9571, a selective high-affinity dual TRIM24-BRPF1 bromodomain inhibitor
Palmer WS, et al.
Journal of medicinal chemistry, 59(4), 1440-1454 (2015)
Lara N Gechijian et al.
Nature chemical biology, 14(4), 405-412 (2018-03-07)
The addressable pocket of a protein is often not functionally relevant in disease. This is true for the multidomain, bromodomain-containing transcriptional regulator TRIM24. TRIM24 has been posited as a dependency in numerous cancers, yet potent and selective ligands for the
Yanai Zhan et al.
Epigenetics & chromatin, 8, 37-37 (2015-09-24)
Proteins that 'read' the histone code are central elements in epigenetic control and bromodomains, which bind acetyl-lysine motifs, are increasingly recognized as potential mediators of disease states. Notably, the first BET bromodomain-based therapies have entered clinical trials and there is

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