Inauhzin, 98%, a dual SirT1/IMPDH2 inhibitor 2-((5H-[1,2,4]三嗪并[5,6-b]吲哚-3-基)硫基)-1-(10H-吩噻嗪-10-基)丁-1-酮

CAS 309271-94-1 MFCD09271941

化学结构图

309271-94-1
SMILES: CCC(Sc1nnc2c(n1)[nH]c1ccccc12)C(=O)N1c2ccccc2Sc2ccccc21

化学属性

Mol. Weight470
Appearance white solid powder
SolubilitySoluble in DMSO, not in water
Mol. FormulaC25H19N5OS2

别名和识别编码

Chemical Name Translation2-((5H-[1,2,4]三嗪并[5,6-b]吲哚-3-基)硫基)-1-(10H-吩噻嗪-10-基)丁-1-酮
Chemical NameInauhzin, 98%, a dual SirT1/IMPDH2 inhibitor
FormulaC25H19N5OS2
Synonym Inauhzin
IUPAC Name2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one
InChIKeyVHUOXERIKQWIJE-UHFFFAOYSA-N
InChIInChI=1S/C25H19N5OS2/c1-2-19(33-25-27-23-22(28-29-25)15-9-3-4-10-16(15)26-23)24(31)30-17-11-5-7-13-20(17)32-21-14-8-6-12-18(21)30/h3-14,19H,2H2,1H3,(H,26,27,29)
Canonical SMILESCCC(SC1=NN=C2C(NC3=C2C=CC=C3)=N1)C(N4C5=C(C=CC=C5)SC6=CC=CC=C46)=O
MDL NumberN/A
CAS Number309271-94-1
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产品应用

  • Inauhzin is a potent SIRT inhibitor, which effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, Inauhzin stabilizes p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, Inauhzin inhibits cell proliferation, induces senescence and tumour-specific apoptosis, and represses the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice.

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
GHS Symbol

系列性分类

  1. Medical Research Areas
  2. Apoptosis
  3. Mdm2

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