I-152

Names

[ CAS No. ]:
311343-11-0

[ Name ]:
I-152

[Synonym ]:
Ethanethioic acid,S-(2-(((2R)-2-(acetylamino)-3-mercapto-1-oxopropyl)amino)ethyl)ester
s-{2-[(n-acetyl-l-cysteinyl)amino]ethyl} ethanethioate
I 152

Biological Activity

[Description]:

I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties[1].

[Related Catalog]:

Signaling Pathways >> NF-κB >> Keap1-Nrf2
Research Areas >> Metabolic Disease

[In Vitro]

I-152 (1 mM;1 h 或 2 h) 降低了 RAW 264.7 细胞中 NRF2 mRNA 的水平[1]。 I-152 (1 mM;0-60 min) 降低了 RAW 264.7 细胞中 NRF2 和 p53 的水平,增加了 ATF4 的表达[1]。 I-152 (0.062、0.125、0.25 或 1 mM) 增加了 RAW 264.7 细胞中 Gclc mRNA (6 h 或 24 h)、Chac1 mRNA (6 h 或 24 h) 和 Chop mRNA (6 h) 的水平[1]。 I-152 (0.062、0.125、0.25 或 1 mM;2 h) 增加了 RAW 264.7 细胞中 GSH 的水平[1]。 I-152 (1 mM;1、2、6 和 24 h) 激活 RAW 264.7 细胞中 ATF4 mRNA 表达[1]。 I-152 (1 mM;24 h 和 48 h) 对 RAW 264.7 细胞显示出细胞杀伤和生长抑制作用[1]。 Western Blot Analysis[1] Cell Line: RAW 264.7 cells. Concentration: 0.062, 0.125, 0.25, 1, 5 or 10 mM. Incubation Time: 2 h or 24 h. Result: Reduced the expression of NRF2/β-ACTIN, increased the expression of GCLM.

[References]

[1]. Crinelli R, et al. Activation of NRF2 and ATF4 Signaling by the Pro-Glutathione Molecule I-152, a Co-Drug of N-Acetyl-Cysteine and Cysteamine. Antioxidants (Basel). 2021 Jan 26;10(2):175.  

Chemical & Physical Properties

[ Molecular Formula ]:
C9H16N2O3S2

[ Molecular Weight ]:
264.36

[ Exact Mass ]:
264.06000

[ PSA ]:
146.35000

[ LogP ]:
1.49740