EHT 1864 2HCl

Catalog No.S7482 Batch:S748201

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Technical Data

Formula

C25H29Cl2F3N2O4S
Molecular Weight 581.47 CAS No. 754240-09-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (171.97 mM)
Water 100 mg/mL (171.97 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description EHT 1864 2HCl is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.
Targets
Rac1 [1]
(Cell-free assay)		 Rac1b [1]
(Cell-free assay)		 Rac2 [1]
(Cell-free assay)		 Rac3 [1]
(Cell-free assay)
40 nM(Kd) 50 nM(Kd) 60 nM(Kd) 250 nM(Kd)
In vitro EHT 1864 selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1. EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH 3T3 cells stably expressing H-Ras(61L) protein. [1] EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. [2] In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down. [3]
In vivo EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Inhibitor:GTPase binding analyses

    For inhibitor:GTPase binding analyses, aliquots of small GTPase solution (containing 1 μM inhibitor) are titrated into a solution of 1 μM inhibitor in the cuvette. Changes in fluorescence anisotropy are monitored at λex = 360 nm, λem = 440 nm, 30 s after each addition. All data analysis and curve fitting were performed using Microsoft Excel and QuantumSoft's ProFit for Mac OS X.
Cell Assay:[1]
  • Cell lines

    NIH 3T3 cells

  • Concentrations

    ~5 μM

  • Incubation Time

    4 days

  • Method

    NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, 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, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.
Animal Study:[2]
  • Animal Models

    Male Hartley albino guinea pigs

  • Dosages

    40 mg/kg daily

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , FASEB J, 2018, 32(4):2197-2211]

Data from [Data independently produced by , , Am J Cancer Res, 2018, 8(1):70-80]

Data from [Data independently produced by , , Mol Biol Cell, 2017, 28(13):1745-1753]

Data from [Data independently produced by , , Int J Clin Exp Pathol, 2016, 9(6):5902-5911.]

Selleck's EHT 1864 2HCl has been cited by 21 publications

Allometrically scaling tissue forces drive pathological foreign-body responses to implants via Rac2-activated myeloid cells [ Nat Biomed Eng, 2023, 10.1038/s41551-023-01091-5] PubMed: 37749310
The PMA phorbol ester tumor promoter increases canonical Wnt signaling via macropinocytosis [ Elife, 2023, 12RP89141] PubMed: 37902809
High-Content and High-Throughput Clonogenic Survival Assay Using Fluorescence Barcoding [ Cancers -Basel), 2023, 15(19)4772] PubMed: 37835466
Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749] PubMed: 37100284
Genetics of mirror movements identifies a multifunctional complex required for Netrin-1 guidance and lateralization of motor control [ Sci Adv, 2023, 9(19):eadd5501] PubMed: 37172092
Microphysiological model of PIK3CA-driven vascular malformations reveals a role of dysregulated Rac1 and mTORC1/2 in lesion formation [ Sci Adv, 2023, 9(7):eade8939] PubMed: 36791204
The PMA Phorbol Ester Tumor Promoter Increases Canonical Wnt Signaling Via Macropinocytosis [ bioRxiv, 2023, 2023.06.02.543509] PubMed: 37333286
RSPO2 defines a distinct undifferentiated progenitor in the tendon/ligament and suppresses ectopic ossification [ Sci Adv, 2022, 8(33):eabn2138] PubMed: 35984875
Microbial Lipopeptide Supramolecular Self-Assemblies as a Methuosis-Like Cell Death Inducer with In Vivo Antitumor Activity [ Small, 2021, 10.1002/smll.202104034] PubMed: 34761865
Maduramicin induces cardiotoxicity via Rac1 signaling-independent methuosis in H9c2 cells [ J Appl Toxicol, 2021, 10.1002/jat.4175] PubMed: 33890316

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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