E235

• CAT Number: I012666
• CAS Number: 891894-69-2
• Molecular Formula: C28H25FN4OS
• Molecular Weight: 484.59
• Purity: ≥95%
• Synonyms: N-(1-benzylpiperidin-4-yl)-2-(4-fluorophenyl)imidazo[2,1-b][1,3]benzothiazole-6-carboxamide
• InChI: InChI=1S/C28H25FN4OS/c29-22-9-6-20(7-10-22)24-18-33-25-11-8-21(16-26(25)35-28(33)31-24)27(34)30-23-12-14-32(15-13-23)17-19-4-2-1-3-5-19/h1-11,16,18,23H,12-15,17H2,(H,30,34)
• InChIKey: SNVVZJBHCSPRGY-UHFFFAOYSA-N
• SMILES: C1CN(CCC1NC(=O)C2=CC3=C(C=C2)N4C=C(N=C4S3)C5=CC=C(C=C5)F)CC6=CC=CC=C6

E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research[1].
E235 (1 µM; 2, 4, 8, 16 or 24 h) down-regulates the level of XBP-1s mRNA in HT1080 cells with time dependent manner[1].
E235 (0.1-10 µM; 4 d or 5 d) has anti-proliferative activity on HT1080, RPMI-8226, B16F10, 4T1, HT1080 shNT and HT1080 shATF4 cells[1].
E235 (0, 1, 5 and 10 µM; 4 h) increases the expression of p53 with dose-dependent manner in AG1522 cells[1].
E235 (1 µM; 2 h) increases the expression of p-Chk2 in AG1522 cells[1].
E235 (0, 1, 5 and 10 µM; 2 h) increases the expression of p-p53 in AG1522 and HT1080 cells[1].
E235 (0, 0.5, 1, 5 and 10 µM; 0.5 h) increases the expression of γ-H2AX with dose-dependent manner in HT1080 cells[1].

Reference

[1]. Sayers CM, et al. Identification and characterization of a potent activator of p53-independent cellular senescence via a small-molecule screen for modifiers of the integrated stress response. Mol Pharmacol. 2013 Mar;83(3):594-604.
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