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| 25mg |
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Purity: ≥98%
EHT 1864 2HCl (EHT-1864; EHT1864), the dihydrochloride salt of EHT-1864, is a potent and novel Rac family GTPase inhibitor with important biological activity. This compound inhibits Rac1, Rac1b, Rac2, and Rac3 at Kd values of 40 nM, 50 nM, 60 nM, and 250 nM, in that order. Pancreatic β-cells' insulin secretion is attenuated by EHT 1864 when glucose is administered. GSIS is specifically inhibited by EHT 1864 when glucose activates Rac1, associates with the membrane, and initiates downstream signaling events.
| Targets |
Rac1 (Kd = 40 nM); Rac1b (Kd = 50 nM); Rac2 (Kd = 60 nM); Rac3 (Kd = 250 nM)
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| ln Vitro |
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| Enzyme Assay |
To conduct inhibitor: GTPase binding analyses, aliquots of small GTPase solution containing a 1 μM inhibitor are titrated into a cuvette containing a 1 μM inhibitor. Fluorescence anisotropy is measured 30 seconds after each addition at λex = 360 nm and λem = 440 nm. Microsoft Excel and QuantumSoft's ProFit for Mac OS X were used for all data analysis and curve fitting.
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| Cell Assay |
In 96-well plates, NIH 3T3 cells that express oncogenic Ras are stably plated. The cells are grown in full growth medium, either on their own or with the addition of 5 μM EHT 1864, for a maximum of 4 days. The next step is to measure cell growth by converting MTT into a formazan product. In summary, the cells are incubated for an additional 4 hours at 37°C after the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml. After that, the medium is taken out, and 100 μl/well of Me2SO is added to stop the reaction. With a microplate reader, the absorbance is measured at 570 nm.
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| Animal Protocol |
Male Hartley albino guinea pigs
40 mg/kg daily i.p. |
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| References |
| Molecular Formula |
C25H29CL2F3N2O4S
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| Molecular Weight |
581.47
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| Elemental Analysis |
C, 51.64; H, 5.03; Cl, 12.19; F, 9.80; N, 4.82; O, 11.01; S, 5.51
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| CAS # |
754240-09-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1COCCN1CC2=CC(=O)C(=CO2)OCCCCCSC3=C4C=CC(=CC4=NC=C3)C(F)(F)F.Cl.Cl
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| InChi Key |
LSECOAJFCKFQJG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27F3N2O4S.2ClH/c26-25(27,28)18-4-5-20-21(14-18)29-7-6-24(20)35-13-3-1-2-10-33-23-17-34-19(15-22(23)31)16-30-8-11-32-12-9-30;;/h4-7,14-15,17H,1-3,8-13,16H2;2*1H
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| Chemical Name |
2-(morpholin-4-ylmethyl)-5-[5-[7-(trifluoromethyl)quinolin-4-yl]sulfanylpentoxy]pyran-4-one;dihydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7198 mL | 8.5989 mL | 17.1978 mL | |
| 5 mM | 0.3440 mL | 1.7198 mL | 3.4396 mL | |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7198 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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