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Formula | C25H29Cl2F3N2O4S |
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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.) |
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. | ||||||||
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Targets |
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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] |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[2] |
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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.]
Gadd45g insufficiency drives the pathogenesis of myeloproliferative neoplasms [ Nat Commun, 2024, 15(1):2989] | PubMed: 38582902 |
Oct4 controls basement membrane development during human embryogenesis [ Dev Cell, 2024, S1534-5807(24)00175-8] | PubMed: 38579716 |
RAC1 inhibition ameliorates IBSP-induced bone metastasis in lung adenocarcinoma [ Cell Rep, 2024, 43(8):114528] | PubMed: 39052477 |
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 |
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 |
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 |
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.