NSC23766 trihydrochloride

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    NSC-23766 is a specific inhibitor of Rac with IC50 of 50μM.NSC-23766 blocks the activation of Rac 1 through binding the GEFs including Trio and Tiam 1 [1]. In human dermal microvascular endothelial cells, NSC-23766 decreased trans-endothelial electrical resistance and caused the intercellular gap formation. Inhibition of Rac 1 by NSC-23766 shortly reduced endothelial barrier functions as revealed by measurement of TER and the appearance of intracellular gaps [2]. In the mucous cell of the intestine, inhibition of Rac1 either by NSC-23766 protected cells from TNF-α-induced apoptosis by inhibiting caspase-3, -8 and -9 activities. Inhibition of Rac1 significantly prevented TNF-α-induced activation of JNK1/2, but did not modulate TNF-α-induced ERK1/2, Akt and p38 MAPK activity [3].
    
    [1]. Gao Y, Dickerson JB, Guo F, Zheng J, Zheng Y. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23.
    [2]. Baumer Y, Spindler V, Werthmann RC, Bünemann M, Waschke J. Role of Rac 1 and cAMP in endothelial barrier stabilization and thrombin-induced barrier breakdown. J Cell Physiol. 2009 Sep;220(3):716-26.
    [3]. Jin S1, Ray RM, Johnson LR. Rac1 mediates intestinal epithelial cell apoptosis via JNK. Am J Physiol Gastrointest Liver Physiol. 2006 Dec;291(6):G1137-47.
- Properties
  - Alternative Name
    
    6-N-[2-[5-(diethylamino)pentan-2-ylamino]-6-methylpyrimidin-4-yl]-2-methylquinoline-4,6-diamine
    
    CAS Number
    
    1177865-17-6
    
    Molecular Formula
    
    C24H35N7·3HCl
    
    Molecular Weight
    
    530.96
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥26.55 mg/mL in DMSO; ≥15.33 mg/mL in H2O; ≥3.52 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Amjad Ali, Jasmin Shafarin, et al. "Co-targeting BET bromodomain BRD4 and RAC1 suppresses growth, stemness and tumorigenesis by disrupting the c-MYC-G9a-FTH1axis and downregulating HDAC1 in molecular subtypes of breast cancer." Int J Biol Sci. 2021 Oct 25;17(15):4474-4492. PMID:34803511
    2. Wei Liu, Qian Sun, et al. "Topographic Cues Guiding Cell Polarization via Distinct Cellular Mechanosensing Pathways." Small. 2021 Nov 5;e2104328. PMID:34738726

NSC23766 trihydrochloride

Background

We Also Recommend

Etoposide

Etoposide

SNS-032 (BMS-387032)