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EHT1864

EHT1864 ??? ???
?? ??:
754240-09-0
???:
EHT1864
???(??):
CS-1343;CS-1239;EHT 1864;EHT-1864 2HCl;EHT 1864, >=98%;EHT1864 USP/EP/BP;EHT-1864;EHT-1864;EHT-1864Dihydrochloride;EHT 1864, 10 mM in DMSO;2-(morpholin-4-ylmethyl)-5-[5-[7-(trifluoromethyl)quinolin-4-yl]sulfanylpentoxy]pyran-4-one
CBNumber:
CB12095478
???:
C25H27F3N2O4S2HCl
??? ??:
0
MOL ??:
754240-09-0.mol
MSDS ??:
SDS

EHT1864 ??

???
>195°C (dec.)
?? ??
2-8°C
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H2O: ???10mg/mL, ??
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H2O: 10mg/mL, clear
CAS ??????
754240-09-0
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  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
WGK ?? 3
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
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P261 ??·?·??·???·??·...·????? ??? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
2 0

EHT1864 C??? ??, ??, ??

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EHT 1864 is an inhibitor of the Rac subfamily of Rho GTPases, that binds to Rac1, Rac1b, Rac2, and Rac3 with Kd values of 40, 50, 50, and 250 nM, respectively. It can reverse transformation of NIH 3T3 fibroblasts caused by constitutively activated Rac1, as well as Rac-dependent transformation caused by Tiam1 or Ras. EHT 1864 inhibits APP processing by γ-secretase, reducing Αβ40 and Αβ42 accumulation. It blocks breast cancer cell invasion in a collagen matrix assay and, at 10 μM, increases the size but decreases the density of dendritic spines of hippocampal neurons in culture.

???? ??

Inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (K D values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β -amyloid peptide production in vivo .

Biochem/physiol Actions

EHT 1864 inhibits Rac function. It prevents Aβ40 and Aβ42 production in vitro without direct inhibition of g-secretase.

EHT1864 ?? ?? ? ???

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EHT1864 ?? ??

???( 102)?? ??
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EHT1864 ?? ??:

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