GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥99%
Moligand™,≥99% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
In Vitro
1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC 50 s of 4 μM and 21 μM, respectively. ?\n1A-116 (1, 10 μM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells. ?\n1A-116 (50, 100 μM; 12 h) blocks Rac1-P-Rex1 interaction. ?\n1A-116 (20 μM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner. ?\n1A-116 (10 μM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS)). ?\n1A-116 (20, 50 μM; 6 h) induces cells apoptosis and in a circadian-dependent manner. ?\n1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: MDA-MB-231, F3II, LN229 cells Concentration: 20 µM Incubation Time: 48 h; 5 h intervals over 25 h. Result: Inhibited cell proliferation in a concentration-dependent and circadian manner. Cell Viability AssayCell Line: Ker-CT human keratinocytes cells with oncogenic Vav2/Rac1 F28L/PAK1 Tyrosine 423 Concentration: 100 nM Incubation Time: Result: Inhibited Rac1 activity at the GEF-Rac1 level. Cell Migration AssayCell Line: LN229 cells Concentration: 10 µM Incubation Time: 16 h Result: Reduced cell migration at 10 HPS which exhibited temporal dependence. Apoptosis AnalysisCell Line: LN229 cells Concentration: 20, 50 µM Incubation Time: 6 h Result: Induced cells apoptosis and in a circadian-dependent manner. Western Blot AnalysisCell Line: F3II cells Concentration: 1, 10 µM Incubation Time: 12 h Result: Blocked Rac1-P-Rex1 interaction. Reduced Rac1-GTP intracellular levels in a concentration-dependent manner.
In Vivo
1A-116 (3 mg/kg; i.v.; once a day for 21 days) demonstrates a high antimetastatic activity with about 60% formation reduction of total metastatic lung colonies in vivo and shows no apparent toxicity . ?\n1A-116 (20 mg/kg; i.p.; once a day, 73 days for ZT12, 68 days for ZT3) increases survival time when treated at ZT12 compare to ZT3 in tumor-bearing mice. (ZT: Zeitgeber time 12 (ZT12) defined as the time of lights off (local time 7 p.m.) and ZT0 defined as lights on (local time 7 a.m.)). ?\n1A-116 shows good oral availability. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c inbred mice (8 to 10-week-old; average 20 g) Dosage: 3 mg/kg Administration: Intravenous injection; once a day for 21 days. Result: Demonstrated a high antimetastatic activity. Animal Model: Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model). Dosage: 20 mg/kg Administration: Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3. Result: Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice.
1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-depend
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
This compound belongs to the class of organic compounds known as trifluoromethylbenzenes. These are organofluorine compounds that contain a benzene ring substituted with one or more trifluoromethyl groups.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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