MG-115
MG-115 (Z-Leu-Leu-Nva-H) is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis. Blockade of proteasomal degradation by MG115 can activate autophagy.
Treatment with proteasome inhibitors Z-Leu-Leu-Nva-H (MG-115) or Z-Leu-Leu-Leu-H (MG-132) prevented the accelerated degradation of these mutant receptors, resulting in increased amounts of the mutant receptors in the COS-7 cells [1].
A potent, reversible proteasome inhibitor with Ki of 21 nM for 20S proteasome and 35 nM for 26S proteasome. The inhibition of proteasome was through specific inhibition of chymotrypsin-like activity of the proteasome. Also shown to induce apoptosis in Rat-1 and PC12 cells via a p3-independent pathway.
References:
1. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. Imamura, T., Haruta, T., Takata, Y., Usui, I., Iwata, M., Ishihara, H., Ishiki, M., Ishibashi, O., Ueno, E., Sasaoka, T., Kobayashi, M. J. Biol. Chem. (1998)
- 1. Abhishesh Bajracharya, Jing Xi, et al. "PHYTOCHROME-INTERACTING FACTOR 4/HEMERA-mediated thermosensory growth requires the Mediator subunit MED14." Plant Physiol. 2022 Nov 28;190(4):2706-2721. PMID: 36063057
- 2. Wang Y, Lu S, et al. "Sonic hedgehog induces GLT-1 degradation via PKC delta to suppress its transporter activities." Neuroscience. 2017 Oct 6;365:217-225. PMID: 28993237
| Physical Appearance | A solid |
| Storage | Store at -20°CThe product is not stable in solution, please dissolve it immediately before use. |
| M.Wt | 461.59 |
| Cas No. | 133407-86-0 |
| Formula | C25H39N3O5 |
| Synonyms | Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115 |
| Solubility | ≥23.08 mg/mL in DMSO; insoluble in H2O; ≥26.5 mg/mL in EtOH |
| Chemical Name | benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate |
| SDF | Download SDF |
| Canonical SMILES | CCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Transfected COS-7 cells expressing mutant or wild-type insulin receptors |
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Preparation method |
Soluble in DMSO. 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. |
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Reaction Conditions |
50 μM; 2 hrs |
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Applications |
In the Leu1193 and Asp1179 mutant cell lines, MG-115 increased the intensities of the bands of the insulin proreceptors and the mature β-subunits to 3- and 4.2-fold, respectively. However, in the wild-type cell lines, there was no change in the intensities of these bands. The results suggested that both Leu1193 and Asp1179 mutant insulin proreceptors were degraded by the proteasome in the cytosol. |
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References: [1]. Imamura T, Haruta T, Takata Y, et al. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. J Biol Chem, 1998, 273(18): 11183-11188. |
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