SGC-iMLLT, MLLT1/3 YEATS domain inhibitor (TBI4046)

Description

Product Details

Formal Name: (S)-1-Methyl-N-(2-((2-methylpyrrolidin-1-yl)methyl)-1H-benzo[d]imidazole-5-yl)-1H-indazole-5-carboxamide

Molecular Formula: C₂₂H₂₄N₆O

Formula Weight: 388.50

CAS Number: 2255338-25-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 50 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

MLLT1/3 YEATS domain inhibitor

Functions

Potent (IC50 = 260 nM) inhibitor of the YEATS domain of MLLT1/3. YEATS domain containing proteins bind acetyl and crotonyl marks on histone tails. Selective against the two other human YEATS domains YEATS2/4 and 48 bromodomains. YEATS containing MLL-ENL leukemic cells display increased sensitivity to SGC-iMLLT versus control AML cells.

Application Procedures

First dissolved in DMSO (up to 50 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.