RIP1/RIP3/MLKL activator 1

• CAT Number: I043874
• CAS Number: 2682850-41-3
• Molecular Formula: C43H56N4O3
• Molecular Weight: 676.93
• Purity: ≥95%
• Synonyms: (2R,4aS,6aR,6aS,14aS)-N-[[1-[(4-tert-butylphenyl)methyl]triazol-4-yl]methyl]-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxamide
• InChI: InChI=1S/C43H56N4O3/c1-27-31-14-15-34-41(7,32(31)22-33(48)36(27)49)19-21-43(9)35-23-40(6,17-16-39(35,5)18-20-42(34,43)8)37(50)44-24-30-26-47(46-45-30)25-28-10-12-29(13-11-28)38(2,3)4/h10-15,22,26,35,49H,16-21,23-25H2,1-9H3,(H,44,50)/t35?,39-,40-,41+,42-,43+/m1/s1
• InChIKey: QLFCJGYFBTYJGC-RSWNTZNOSA-N
• SMILES: CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)NCC6=CN(N=N6)CC7=CC=C(C=C7)C(C)(C)C)C)C)C)C)O

RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability[1].
RIP1/RIP3/MLKL activator 1 (Compound 6i) (96 h) shows antiproliferative activities in human glioma cell lines[1].
RIP1/RIP3/MLKL activator 1 (0-4 µM, 0-72 h) exhibits remarkable antiproliferative activity for U251 cells in a time- and concentration-dependent manner[1].
RIP1/RIP3/MLKL activator 1 (10 µM, 0-72 h) shows acceptable stability[1].
RIP1/RIP3/MLKL activator 1 (0-2 µM, 24 h) effectively inhibits the migration of U251 cells[1].
RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway, and induces mitochondrial depolarization in U251 cells[1].
RIP1/RIP3/MLKL activator 1 could not induce apoptosis in U251 cells[1].
RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability[1].

Reference

[1]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070.
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