5-Chloro-1-[(2,5-dichlorophenyl)methyl]-1H-indole-2,3-dione3-(O-acetyloxime)

Name	LDN 57444
Synonyms	LDN-57444 LDN 57444 UCH-L1 Inhibitor (Z)-3-(Acetoxyimino)-5-chloro-1-(2,5-dichlorobenzyl)indolin-2-one 5-Chloro-1-[(2,5-dichlorophenyl)methyl]-1H-indole-2,3-dione3-(O-acetyloxime) 3-(O-acetyloxime), 5-chloro-1-[(2,5-dichlorophenyl)methyl]-1H-Indole-2,3-dione 1H-Indole-2,3-dione, 5-chloro-1-[(2,5-dichlorophenyl)methyl]-, 3-(O-acetyloxime) 5-Chloro-1-[(2,5-dichlorophenyl)methyl]-1H-indole-2,3-dione 3-(O-acetyloxime) LDN 57444
CAS	668467-91-2

Molecular Formula	C17H11Cl3N2O3
Molar Mass	397.64
Density	1.50±0.1 g/cm3(Predicted)
Boling Point	534.4±60.0 °C(Predicted)
Solubility	DMSO: soluble16mg/mL
Appearance	solid
Color	Yellow
pKa	-2.57±0.20(Predicted)
Storage Condition	2-8°C
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
In vitro study	50 μm LDN-57444 treatment for 24 hours inhibited 70% of the protease activity. LDN-57444 above 25 μm significantly reduced the cell survival rate, which was concentration dependent, and the cell survival rate was reduced to 61.81% at 50 μm. LDN-57444 can lead to cell death through the apoptotic pathway, by reducing the activity of the ubiquitin-proteasome system and increasing the level of highly ubiquitinated proteins, both of these can activate the unfolded protein response. LDN-57444-induced apoptosis can be triggered by activation of endoplasmic reticulum stress (ERS).
In vivo study	LDN-57444, the distribution of synaptophysin in the body and the morphology of the spine were significantly changed. LDN treatment resulted in a rapid decrease in UCH-L1 activity, but treatment for several hours had no effect on protease inhibition of cAMP levels.

Hazard Symbols	N - Dangerous for the environment
Risk Codes	50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment.
Safety Description	S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets.
UN IDs	UN 3077 9 / PGIII
WGK Germany	3

Last Update：2024-01-02 23:10:35

biological activity	LDN-57444 is a reversible and competitive proteasome inhibitor. when inhibiting UCch-L1, IC50 is 0.88 μM, which is 30 times higher than the selectivity of subtype Uch-L3.
in vitro study	50 μM LDN-57444 treatment for 24 hours inhibited 70% protease activity. LDN-57444 above 25 μM significantly reduced the cell survival rate, which was concentration-dependent. At 50 μM, the cell survival rate decreased to 61.81%. LDN-57444 can lead to cell death through the apoptosis pathway, by reducing the activity of the ubiquitin proteasome system and increasing the level of highly ubiquitinated proteins, both of which can activate unfolded protein reactions. LDN-57444-induced apoptosis can be triggered by activating endoplasmic reticulum stress (ERS).
in vivo studies	LDN-57444 significantly change the distribution of synaptic proteins and spine morphology in vivo. LDN treatment resulted in a rapid decline in UCH-L1 activity, but treatment for several hours had no effect on protease inhibition at cAMP level.
target	IC50: 0.88 μM (UCH-L1), 25 μM (UCH-L3) Ki: 0.40 μM (UCH-L1)

Last Update：2024-04-09 21:11:58

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CAS: 668467-91-2
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Spot supply

Product Name: LDN 57444 Visit Supplier Webpage Request for quotation
CAS: 668467-91-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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5-Chloro-1-[(2,5-dichlorophenyl)methyl]-1H-indole-2,3-dione3-(O-acetyloxime) Request for Quotation