474790

MG-132

A cell-permeable, potent, reversible proteasome inhibitor (K_i = 4 nM).

• 동의어(들): Z-Leu-Leu-Leu-al, Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal, Z-LLL-CHO, Proteasome Inhibitor XI, MG-132
• 실험식(Hill 표기법): C₂₆H₄₁N₃O₅
• CAS Number: 133407-82-6
• Molecular Weight: 475.62
• MDL number: MFCD00674886
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze
• 색상: white
• solubility: DMSO: 20 mg/mL; ethanol: 20 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C
• SMILES string: [H]C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1
• InChI: 1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1
• InChI key: TZYWCYJVHRLUCT-VABKMULXSA-N

설명

Amino Acid Sequence

Z-Leu-Leu-Leu-al

일반 설명

A potent, reversible, and cell-permeable proteasome inhibitor (K_i = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. Inhibits NF-κB activation (IC₅₀ = 3 µM). Also reported to increases the survival rate of mesenchymal stem cells following their transplantation. Prevents β-secretase cleavage. A 10 mM (1 mg/210 µl) solution of MG-132 (Cat. No. 474791) in DMSO is also available. This material is ≥98% pure by HPLC. A material with ≥95% purity by HPLC (Cat. No. 474787) is also available.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
proteasome

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 3 µM against NF-κB activation

Target K_i: 4 nM against proteasome

경고

Toxicity: Standard Handling (A)

서열

Z-Leu-Leu-Leu-CHO

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

기타 정보

Li, Z.W. et al. 2011. Sheng Li Xue Bao. 63, 525.
Steinhilb, M.L., et al. 2001. J. Biol. Chem.276, 4476.
Meriin, A.B., et al. 1998. J. Biol. Chem. 273, 6373.
Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.
Klafki, H.W., et al. 1996. J. Biol. Chem.271, 2865.
Lee, D.H., and Goldberg, A.L., 1996. J. Biol. Chem.271, 27280.
Wiertz, E.J., et al. 1996. Cell84, 769.
Jensen, T.J., et al. 1995. Cell 83, 129.
Read, M.A., et al. 1995. Immunity2, 493.
Rock, K.L., et al. 1994. Cell 78, 761.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3