NSC 23766 TETRAHYDROCHLORIDE Struktur

NSC 23766 TETRAHYDROCHLORIDE

Bezeichnung:NSC 23766 TETRAHYDROCHLORIDE

CAS-Nr733767-34-5

Englisch Name:NSC 23766 TETRAHYDROCHLORIDE

CBNumberCB6504010

SummenformelC24H35N7

Molgewicht421.58

MOL-Datei733767-34-5.mol

NSC 23766 TETRAHYDROCHLORIDE physikalisch-chemischer Eigenschaften

storage temp.	Desiccate at RT
Löslichkeit	Soluble in DMSO (50 mg/ml); Water (50 mg/ml)
Aggregatzustand	White powder solid.
Farbe	White
Wasserlöslichkeit	Soluble in water.
Sensitive	Light Sensitive & Hygroscopic
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.

NSC 23766 TETRAHYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
NSC-23766 (733767-34-5) is a selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) Trio and Tiam1 (IC50 ca. 50 μM) with no effect on the closely related Cdc42 or RhoA. In cells, it blocks serum or PDGF-induced Rac-1 activation and lamellipodia formation. NSC-23766 suppressed the growth of wild-type NIH 3T3 cells but was inactive in cells expressing the constitutively active Rac1 mutant, L61Rac1.1 It is a useful tool to probe the involvement of Rac1 in cell signalling.2 Off target effect: antagonist at muscarinic acetylcholine receptors.3 Cell permeable.
Verwenden
The compound blocks activation by the guanine nucleotide exchange factors Trio and Tiam1, but does not affect interactions with RhoA or Cdc42. NSC23766 blocks ADP-mediated platelet aggregation. Inhibition of Rac1 by NSC23766 restores sensitivity to trastuzumab by restoring down-regulation of ErbB2. Membrane type 1-matrix metalloproteinases (MT-1MMP) expression in CB CD34+ cells has been reported to decrease in the presence of NSC 23766. Silveta compress investigations indicate that NSC 23766 depolarizes endomembrane cycling, altered polar adhesive secretion, and tip growth.
Definition
ChEBI: NSC 23766 is an aminopyrimidine that is 6-methylpyrimidine-2,4-diamine in which the amino groups at positions 2 and 4 are substituted by 5-(diethylamino)pentan-2-yl and 4-amino-2-methylquinolin-6-yl groups respectively. An inhibitor of the signalling G-protein known as RAC1 (Ras-related C3 botulinum toxin substrate 1). It has a role as an EC 3.6.5.2 (small monomeric GTPase) inhibitor, an antiviral agent, a muscarinic antagonist and an apoptosis inducer. It is an aminoquinoline, an aminopyrimidine, a primary amino compound, a secondary amino compound and a tertiary amino compound.
Biologische Aktivität
Selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC 50 ~ 50 μ M) without affecting Cdc42 or RhoA activation. Inhibits Rac1-mediated cell functions and reported to reverse tumor cell phenotyes in prostate cancer cells.
Einzelnachweise
Gao et al. (2004), Rational design and characterization of a Rac GTPase-specific small molecule inhibitor; Proc. Natl. Acad. Sci. USA, 101 7618 Shankar et al. (2013), Raft endocytosis of AMF regulates mitochondrial dynamics through Rac1 signaling and the Gp78 ubiquitin ligase; J. Cell Sci., 126 3295 Levay et al. (2013), NSC23766, a widely used inhibitor of Rac1 activation, additionally acts as a competitive antagonist at muscarinic acetylcholine receptors; J. Pharmacol. Exp. Ther., 347 69

NSC 23766 TETRAHYDROCHLORIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

733767-34-5, NSC 23766 TETRAHYDROCHLORIDE Verwandte Suche:

Send Inquriy