I-BRD9 Struktur

I-BRD9

Bezeichnung:I-BRD9

CAS-Nr1714146-59-4

Englisch Name:I-BRD9

CBNumberCB83122929

SummenformelC22H22F3N3O3S2

Molgewicht497.55

MOL-Datei1714146-59-4.mol

I-BRD9 physikalisch-chemischer Eigenschaften

Siedepunkt	683.9±65.0 °C(Predicted)
Dichte	1.50±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	crystalline solid
pka	9.35±0.40(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

I-BRD9 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 has a pIC50 value of 7.3 for BRD9 inhibitor, with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is also shows a greater than 70-fold selectivity against a panel of 34 bromodomains. I-BRD9 downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells.
Verwenden
I-BRD9 is a bromodomain-containing protein 9 (BRD9) inhibitor which belong to class of (BET) inhibitors that have shown potent anti-inflammatory and anticancer properties.
Biologische Aktivität
pic50: 7.3i-brd9 is a brd9 inhibitor.brd9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. human brd9 has a single bromodomain and contains five isoforms which are produced by alternative splicing.
in vitro
in previous study, the i-brd9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at brd9, over 700-fold selectivity against the bet family as well as more than 70-fold to a panel of 34 bromodomains. in kasumi-1 cells, i-brd9 could downregulate dusp6, clec1, samsn1 and fes genes. moreover, i-brd9 was used to expore genes regulated by brd9 in kasumi-1 cells involved in immune response and oncology pathways. in addition, when brd4 was used as a representative member of the bet family for initial selectivity screening, i-brd9 was found to have a pic50 of 5.3 against this protein. i-brd9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of brd9 bromodomain [1].
Lager
Store at -20°C
Einzelnachweise
[1] theodoulou nh et al. discovery of i-brd9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. j med chem. 2016 feb 25;59(4):1425-39.

I-BRD9 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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