- PR-619
- WP1130
- P005091
| LDN 57444UCH-L1 inhibitor,reversible competitve |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.79%
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- HPLC
- NMR (Nuclear Magnetic Resonance)
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- Datasheet
Chemical structure
| Description | LDN 57444 is an inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) with Ki value of 0.4 μM. | |||||
| Targets | UCH-L1 | |||||
| IC50 | 0.4 μM (Ki) | |||||
| Cell experiment [1,2]: | |
Cell lines | Rat insulinoma cell line INS 832/13, SK-N-SH cells |
Preparation method | The solubility of this compound in DMSO is >16.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 30 μM, 24 h |
Applications | In rat insulinoma cell line INS 832/13, LDN 57444 induced cell apoptosis. LDN 57444 (>30 μM) increased the activity of caspase-3. LDN 57444 induced nuclear CHOP, suggesting that the apoptosis induced by the inhibition of Uch-L1. In SK-N-SH cells, LDN 57444 (25-100 μM) induced apoptotic cell death in SK-N-SH cells. LDN 57444 triggered the endoplasmic reticulum stress in SK-N-SH cells. |
| Animal experiment [1]: | |
Animal models | APP/PS1 Mice |
Dosage form | Intraperitoneal injection, 0.4 mg/kg |
Application | LDN 57444 caused dramatic alterations in synaptic protein distribution and spine morphology in vivo. Treatment with LDN 57444 resulted in a rapid fall of Uch-L1 activity. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Gong B, Cao Z, Zheng P, et al. Ubiquitin hydrolase Uch-L1 rescues β-amyloid-induced decreases in synaptic function and contextual memory[J]. Cell, 2006, 126(4): 775-788. [2]. Tan Y Y, Zhou H Y, Wang Z Q, et al. Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor[J]. Molecular and cellular biochemistry, 2008, 318(1-2): 109-115. | |
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| Cas No. | 668467-91-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | [(Z)-[5-chloro-1-[(2,5-dichlorophenyl)methyl]-2-oxoindol-3-ylidene]amino] acetate | ||
| Canonical SMILES | CC(=O)ON=C1C2=C(C=CC(=C2)Cl)N(C1=O)CC3=C(C=CC(=C3)Cl)Cl | ||
| Formula | C17H11Cl3N2O3 | M.Wt | 397.64 |
| Solubility | ≥16.7 mg/mL in DMSO with gentle warming, <2.14 mg/ml="" in="" etoh,=""><2.23 mg/ml="" in="" h2o=""> | Storage | Desiccate at 4°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
LDN 57444 is a reversible competitive inhibitor of ubiquitin C-terminal hydrolase L1 (Uch-L1) with IC50 value of 0.88μM [1].
Besides Uch-L1, LDN 57444 also inhibits Uch-L3 with a higher IC50 value of 25μM. The inhibition of Uch enzymes subsequently causes the reduction of long-term potentiation and basal synaptic transmission, which is similar to the alterations induced by Aβ [1].
In rat insulinoma cell line INS 832/13, treatment of LDN 57444 leads to the cell apoptosis. The increased activity of caspase-3 can be seen when the concentration of LDN 57444 is above 30μM. LDN 57444 also induces nuclear CHOP, suggesting that the apoptosis induced by the inhibition of Uch-L1 is related to ER stress [2].
References:[1] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.[2] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.
