MS436

Bezeichnung:MS436

CAS-Nr1395084-25-9

Englisch Name:MS436

CBNumberCB12677056

SummenformelC18H17N5O3S

Molgewicht383.42

MOL-Datei1395084-25-9.mol

MS436 physikalisch-chemischer Eigenschaften

Siedepunkt	673.7±65.0 °C(Predicted)
Dichte	1.42±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; insoluble in EtOH; ≥19.15 mg/mL in DMSO
Aggregatzustand	solid
pka	9.25±0.36(Predicted)
Farbe	Pink to red

MS436 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM) with preference for the first bromodomain over the second. MS436 effectively blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 ?M, respectively). MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.
Verwenden
MS 436 is a potent bromodomain inhibitor, binding to BRD4 and more tightly to subdomain BD1 than BD2. These domains play a key role in inflammatory gene expression, mitosis and viral/host interaction. Applications involving innhibition of bromodomains include decrease in cell proliferation for leukemia and destruction of tumor cells.
Biologische Aktivität
ms436 is a potent and selective small-molecule inhibitor of brd4 with ki values of ＜0.085μm and 0.34μm, respectively for brd1 and brd2 [1].brd4 plays a role in gene transcription and is a drug target for cancer and inflammation. it has two bromodomains. ms436 is a diazobenzene compound, it is designed from the sar studies to have higher selectivity. in vitro fluorescent anisotropy assay shows ms436 has about 10-fold higher affinity of brd1 over brd2. ms436 binds to brd4 through a set of water-mediated interaction and this is the molecular basis for the binding affinity. ms436 also has activity to cbp brd. in raw264.7 cells, ms436 can block nf-κb-directed no production and block the expression of proinflammatory cytokine interleukin (il)-6 induced by lps [1].
Lager
-20°C
Einzelnachweise
[1] zhang g, plotnikov an, rusinova e, shen t, morohashi k, joshua j, zeng l, mujtaba s, ohlmeyer m, zhou mm. structure-guided design of potent diazobenzene inhibitors for the bet bromodomains. j med chem. 2013 nov 27;56(22):9251-64.

MS436 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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