UNC1215

SKU: orb1226333

Description

A potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd of 120 nM; 50-fold more potent toward L3MBTL3 than other members of the MBT family; directly binds to L3MBTL3 via the Kme-binding pocket of the MBT domains.

Key Properties

• CAS Number: 1415800-43-9
• MW: 529.7161
• Purity: >98% (HPLC)
• Formula: C₃₂H₄₃N₅O₂
• SMILES: O=C(C1=CC=C(C(N2CCC(N3CCCC3)CC2)=O)C=C1NC4=CC=CC=C4)N5CCC(N6CCCC6)CC5
• Target: HMTase
• Solubility: DMSO: ≥ 270 mg/mL

Bioactivity

• In Vitro:
  UNC1215 binds L3MBTL3 with a d of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2: 2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UNC 1215 | UNC-1215

Quick Database Links

Gene Symbol

HMTase