HDAC-IN-57

CAS No. 2716217-79-5

HDAC-IN-57( —— )

Catalog No. M36851 CAS No. 2716217-79-5

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    HDAC-IN-57
  • Note
    Research use only, not for human use.
  • Brief Description
    HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively.
  • Description
    HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ.HDAC-IN-57 induces apoptosis, and has anti-tumor activity.
  • In Vitro
    Western Blot Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.5 μM Incubation Time:48 hours Result:Inhibited cellular LSD1 and HDACs. Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2. Apoptosis Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner.Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM.Cell Migration Assay Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.0 μM, 4 μM Incubation Time:48 hours Result:Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells.Cell Cycle Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    HDAC
  • Recptor
    HDAC | Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2716217-79-5
  • Formula Weight
    377.39
  • Molecular Formula
    C21H19N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    C(NCC1=CC=C(C(NO)=O)C=C1)(=O)C=2C=C(N=CC2)C3=CC=C(OC)C=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.?
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