MDL-800

SKU: orb1819232

Description

MDL-800 is a potent and selective SIRT6 activator, enhancing its deacetylase activity to reduce global H3K9ac and H3K56ac levels. It suppresses hepatocellular carcinoma cell proliferation in vitro through SIRT6-mediated cell-cycle arrest and demonstrates efficacy in vivo in xenograft models, supporting its use in oncology and epigenetics research.

Research Area

Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2275619-53-7
• MW: 626.3
• Purity: >98%
• Formula: C₂₁H₁₆BrCl₂FN₂O₆S₂
• SMILES: COC(=O)c1cc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)ccc1S(=O)(=O)Nc1cc(Br)c(F)cc1C
• Target: Protein deacetylase
• Solubility: Soluble in DMSO (up to 10 mg/ml with warming)

Bioactivity

• In Vivo:
  In HCC827 cell-derived xenograft nude mice, intraperitoneal administration of MDL-800 (80 mg · kg-1 · d-1, for 14 days) markedly suppressed the tumor growth, accompanied by enhanced SIRT6-dependent histone H3 deacetylation and decreased p-MEK and p-ERK in tumor tissues.
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• In Vitro:
  MDL-800 increased SIRT6 deacetylase activity with an EC50 value of 11.0 ± 0.3 μM; MDL-800 (10-50 μM) induced dose-dependent deacetylation of histone H3 in 12 NSCLC cell lines. Treatment with MDL-800 dose dependently inhibited the proliferation of 12 NSCLC cell lines with IC50 values ranging from 21.5 to 34.5 μM. The antiproliferation effect of MDL-800 was significantly diminished by SIRT6 knockout. Treatment with MDL-800 induced remarkable cell cycle arrest at the G0/G1 phase in NSCLC HCC827 and PC9 cells. Furthermore, MDL-800 (25, 50 μM) enhanced the antiproliferation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in osimertinib-resistant HCC827 and PC9 cells as well as in patient-derived primary tumor cells, and suppressed mitogen-activated protein kinase (MAPK) pathway.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MDL 800, MDL800, MDL-800, SIRT6

Compound Identifiers

PubChem CID

134717374