NSC 23766 TETRAHYDROCHLORIDE manufacturers
- NSC 23766
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- $49.00 / 2mg
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2026-05-11
- CAS:733767-34-5
- Min. Order:
- Purity: 99.49%
- Supply Ability: 10g
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| | NSC 23766 TETRAHYDROCHLORIDE Basic information |
| | NSC 23766 TETRAHYDROCHLORIDE Chemical Properties |
| storage temp. | Desiccate at RT | | solubility | Soluble in DMSO (50 mg/ml); Water (50 mg/ml) | | form | White powder solid. | | color | White | | Water Solubility | Soluble in water. | | Sensitive | Light Sensitive & Hygroscopic | | Stability: | 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 Usage And Synthesis |
| Description | 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. | | Uses | 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. | | Biological Activity | 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. | | in vivo | NSC23766 (2.5 mg/kg/day, i.p.) significantly attenuates the onset of spontaneous diabetes in NOD mice, without significant effects on the growth (body weights) of the mice. NSC23766 significantly increases the expression of Rac1 and CHOP, a marker for ER-stress, in islets from NOD mice[1]. | | References | [1] YUAN GAO. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2004, 101 20: 7618-7623. DOI:10.1073/pnas.0307512101
[2] JAY SHANKAR. Raft endocytosis of AMF regulates mitochondrial dynamics through Rac1 signaling and the Gp78 ubiquitin ligase.[J]. Journal of cell science, 2013: 3295-3304. DOI:10.1242/jcs.120162
[3] MAGDOLNA LEVAY. NSC23766, a widely used inhibitor of Rac1 activation, additionally acts as a competitive antagonist at muscarinic acetylcholine receptors.[J]. Journal of Pharmacology and Experimental Therapeutics, 2013, 347 1: 69-79. DOI:10.1124/jpet.113.207266 |
| | NSC 23766 TETRAHYDROCHLORIDE Preparation Products And Raw materials |
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