UNC1999

SKU: orb1304582

Description

UNC1999

Research Area

Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1431612-23-5
• MW: 569.74
• Purity: >98%
• Formula: C₃₃H₄₃N₇O₂
• SMILES: CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccc(nc1)N1CCN(CC1)C(C)C
• Target: Protein methyltransferase
• Solubility: Soluble in DMSO (up to 10 mg/ml).

Bioactivity

• Target IC50:
  EZH2:2 nM|EZH1:45 nM
• In Vivo:
  In animal studies, intraperitoneal injection of UNC1999 (50-150 mg/kg) effectively elevated the concentration levels in animal plasma above the cellular IC50 value.
• In Vitro:
  In the MCF10A cell line, UNC1999 demonstrates relatively low cytotoxicity with an IC50 of 124 nM and reduces H3K27me3 levels in a concentration-dependent manner. It also inhibits cell proliferation concentration-dependently in DLBCL cell lines containing the EZH2Y641N mutation.
• Cell Research:
  DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentrations of compounds (DMSO control, UNC1999, or UNC2400). The medium containing the test compound or control is refreshed every 3 days. The numbers of viable cells from at least three independent experiments are measured using TC20 automated cell counter system. Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 μg of total histones is separated using 15% SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3. (Only for Reference)

Storage & Handling

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

Alternative Names

Autophagy, inhibit, EZH1, EZH2, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase, UNC 1999, UNC1999, UNC-1999

Compound Identifiers

PubChem CID

72551585