JGB1741

• CAT Number: I011799
• CAS Number: 1256375-38-8
• Molecular Formula: C27H24N2O2S
• Molecular Weight: 440.56
• Purity: ≥95%
• Synonyms: N-benzyl-2-[(E)-(2-hydroxynaphthalen-1-yl)methylideneamino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
• InChI: InChI=1S/C27H24N2O2S/c30-23-15-14-19-10-4-5-11-20(19)22(23)17-29-27-25(21-12-6-7-13-24(21)32-27)26(31)28-16-18-8-2-1-3-9-18/h1-5,8-11,14-15,17,30H,6-7,12-13,16H2,(H,28,31)/b29-17+
• InChIKey: CRTIXRJWHKMWCH-STBIYBPSSA-N
• SMILES: C1CCC2=C(C1)C(=C(S2)N=CC3=C(C=CC4=CC=CC=C43)O)C(=O)NCC5=CC=CC=C5

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research[1].
JGB1741 (ILS-JGB-1741; 1-10000 nM; 24 h) inhibits MDA-MB 231 cell proliferation[1].
JGB1741 (0.01-1 μM; 24 h) induces apoptosis of MDA-MB 231 cells[1].
JGB1741 (0.01-1 μM; 24 h) shows a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase[1].
JGB1741 (0.01-1 μM; 24 h) shows an increase in the global acetylation of H3K9, p53 expression and acetylated p53K382 levels[1].

Reference

[1]. Arunasree M Kalle, et al. Inhibition of SIRT1 by a small molecule induces apoptosis in breast cancer cells. Biochem Biophys Res Commun. 2010 Oct 8;401(1):13-9.
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