N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE
CAS: 133407-82-6
Molecular Formula: C26H41N3O5
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Names and Identifiers
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Physico-chemical Properties
| Molecular Formula | C26H41N3O5 |
| Molar Mass | 475.62 |
| Density | 1.073 |
| Melting Point | 80-84℃ (DEC.) |
| Boling Point | 682.0±55.0 °C(Predicted) |
| Specific Rotation(α) | -61～-67° |
| Flash Point | 366℃ |
| Water Solubility | Soluble in ethanol, chloroform, methanol, water. |
| Solubility | Soluble in DMSO (25 mg/ml), 100% ethanol (25 mg/ml), chloroform:methanol solution (95:5) |
| Appearance | White powder |
| Color | White |
| pKa | 11.14±0.46(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, DMF or ethanol may be stored at -20° for up to 1 week. |
| MDL | MFCD00674886 |
| Use | A proteasome and NF-κB inhibitor. |
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Risk and Safety
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| HS Code | 29242990 |
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Reference
| Reference Show more | 1. [IF=5.778] Yuting Wang et al."Polybrominated diphenyl ethers quinone-induced intracellular protein oxidative damage triggers ubiquitin-proteasome and autophagy-lysosomal system activation in LO2 cells."Chemosphere. 2021 Jul;275:130034 2. [IF=5.34] Xiang Zhou et al.Rosmarinic Acid Decreases the Malignancy of Pancreatic Cancer Through Inhibiting Gli1 Signaling.Phytomedicine. 2021 Nov;:153861 |
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Introduction
MG-132 is a proteasome inhibitor. IC50 is 100 nM and also inhibits calpain. IC50 is 1.2 μM.
Last Update：2022-10-16 17:30:35
N-[(PHENYLMETHOXY)CARBONYL]-L-LEUCYL-N-[(1S)-1-FORMYL-3-METHYLBUTYL]-L-LEUCINAMIDE - Reference Information
| Overview | MG132, a proteasome inhibitor, is a potent, reversible, fine cell permeable 20s protease inhibitor. It inhibits the proteasome chymotrypsin-like peptidase activity with an IC50 value of 24.2 nM. MG-132 inhibited C6 glioma cell proliferation in a time-and dose-dependent manner (IC 50 value of 18.5 μm at 24 hours). MG-132 induces apoptosis by down-regulating the upregulation of anti-apoptotic protein Bcl-2 and XIAP, the pro-apoptotic proteins Bax and caspase-3, and the production of cleaved C- terminal 85kDa PARP. |
| action | MG-132 is a polypeptide aldehyde that is also a potent, reversible, cell-permeable proteasome inhibitor, the IC50 value was 100 nM, effectively blocking the proteolytic activity of the 26S proteasome complex. |
| In Vitro Activity | MG132 inhibits the growth of HeLa cells by inducing cell cycle arrest and initiating apoptosis. MG-132 inhibited C6 glioma cell proliferation in a time-and dose-dependent manner (IC 50 value of 18.5 μm at 24 hours). MG-132(18.5 μm) inhibited proteasome activity by about 70% at 3 hours. MG-132 induces apoptosis by down-regulating the upregulation of anti-apoptotic proteins Bcl-2 and XIAP, pro-apoptotic proteins Bax and caspase-3, and the production of cleaved C- terminal 85kDa PARP. MG-132 will also increase the active oxygen more than 5 times. The IC50 of MG-132 on HeLa,CaSki and C33A cervical cancer cell survival rates after 48 hours of incubation were 2.1,3.2 and 5.2 μM, respectively. |
| in vivo activity | in vivo antitumor activity of MG-132 against cervical cancer was examined using subcutaneous injection. Xenograft model. MG-132 was injected at 1 mg/kg using the following protocol: days 1,4,8,12,15,18,23 and 26 for HeLa Tumor bearing mice. Compared with the control, the growth inhibition rate of MG132 was 49%. MG-132 (inguinal, 0.1 mg/kg/day) by regulating ERK1 / 2 and JNK1 signaling pathway to reduce pressure overload induced cardiac hypertrophy and improve cardiac function in rats with abdominal aortic banding (DAB). |
| biological activity | MG-132 (Z-Leu-Leu-Leu-al) is a potent, reversible proteasome inhibitor, the IC50 was 100 nM. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132 is a peptide aldehyde that is an activator of autophagy. MG-132 also induced apoptosis. |
| Target | IC50: 100 nM (protein), 1.2 μm (Calpain) |
| Cell Line: | C6 glioma cells A549 cells |
| Concentration: | 10, 20, 30, 40 μM 10 μM |
| Incubation Time: | 24 hours 1 hour |
| Result: | Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC 50 of 18.5 μM at 24 hours. Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation. Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice. The growth inhibition rates in HeLa tumors was 49% compared to the control. |
| Animal Model: | 5- to 6-weeks old female athymic nude mice (EC9706 xenograft) Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells) |
| Dosage: | 10 mg/kg 1 mg/kg |
| Administration: | I.p.; daily for 25 days starting 5 days after EC9706 cells injection Intravenous injection; twice a week for 4 weeks |
Last Update：2024-04-09 15:16:52
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QQ: 3008007409
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