MG115|CAS 133407-86-0|DC Chemicals

Cas No.:	133407-86-0
Chemical Name:	MG-115
Synonyms:	L-Leucinamide,N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formylbutyl]-;(S)-MG115;MG-115;MG-115 (Z-LL-Nva-CHO);Z-Leu-Leu-Norvalinal;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;MG115 Z-LLnV;MG115;Z-LLnV;Z-LL-NVA-CHO;Z-LEU-LEU-NVA-H;Z-LEU-LEU-NVA-CHO;Z-LEU-LEU-NVA-ALDEHYDE;N-CBZ-LEU-LEU-NORVALINAL;MG115, Z-LLnV;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]carbamic acid (phenylmethyl) ester;CHEBI:95100;GTPL11639;Cbz-Leu-Leu-norvalinal;CS-0029136;Q27166869;carbobenzoxy-leucyl-leucyl-norvalinal;Curator_000004;EX-A1500B;Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal;DTXSID00432100;J-006370;AKOS040744889;HY-108552;CHEMBL4518490;SCHEMBL2140161;n-benzyloxycarbonyl-l-leucyl-l-leucyl-l-norvalinal;133407-86-0;NCGC00345815-01;Z-Leu-Leu-Norvalinal, >=90% (HPLC), powder;BDBM476985;QEJRGURBLQWEOU-FKBYEOEOSA-N;DA-55451;DTXCID50382929;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;G12577
SMILES:	O=C([C@H](CC(C)C)NC(=O)OCC1C=CC=CC=1)N[C@H](C(N[C@H](C=O)CCC)=O)CC(C)C
Formula:	C₂₅H₃₉N₃O₅
M.Wt:	461.594267129898
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Rock KL, et, al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71. [2]. Lopes UG, et, al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. [3]. Kim J, et, al. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90.

Target:	Ki: 21 nM (20S proteasome); 35 nM (26 Sproteasome)[1]
In Vitro:	MG-115 (0.1-10 μM; 24 h) dose-dependently decreases the viability of HepG2 cells[3]. MG-115 (0.1-10 μM; 24 h) amplifies the reporter gene expression mediated by CWK18 DNA condensates[3]. Cell Viability Assay[3] Cell Line: HepG2 cells Concentration: 0.1, 1, 2, 5, 10 μM Incubation Time: 24 hours Result: Dose-dependently decreased cell viability. Inhibited the proteasomal activity, with an IC50 of 2 μM.
References:	[1]. Rock KL, et, al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71. [2]. Lopes UG, et, al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. [3]. Kim J, et, al. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90.

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC79609	NCGC00685960	NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.
DC77831	Vicadrostat	Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.
DC77813	Zeltociclib	Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.
DC77714	S3226	S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.
DC77387	AUR1545	AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).
DC77822	JNJ-77242113 (Icotrokinr)	Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
DC77088	T025	T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.