受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H29Cl2F3N2O4S |
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分子量 | 581.47 | CAS No. | 754240-09-0 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL warmed with 50ºC water bath (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. |
製品説明 | 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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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] |
キナーゼアッセイ | Inhibitor:GTPase binding analyses | |
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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. | ||
細胞アッセイ | 細胞株 | NIH 3T3 cells |
濃度 | ~5 μM | |
反応時間 | 4 days | |
実験の流れ | 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. | |
動物実験 | 動物モデル | Male Hartley albino guinea pigs |
投薬量 | 40 mg/kg daily | |
投与方法 | i.p. |
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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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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