SGC0946

SKU: orb1304559

Description

SGC0946 is a potent and selective DOT1L methyltransferase inhibitor with an IC50 of 0.3 nM. It induces selective cell death in MLL-rearranged leukemia cells and is a valuable chemical probe for studying histone methylation in both in vitro and in vivo cancer research models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1561178-17-3
• MW: 618.57
• Purity: 99.82% (May vary between batches)
• Formula: C₂₈H₄₀BrN₇O₄
• SMILES: CC(C)N(CCCNC(=O)Nc1ccc(cc1)C(C)(C)C)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12
• Target: Histone Methyltransferase
• Solubility: Ethanol:93 mg/mL (150.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.33 mM);DMSO:150 mg/mL (242.49 mM)

Bioactivity

• Target IC50:
  DOT1L:0.3 nM
• In Vivo:
  SGC 0946 significantly decreases di-methylation of H3K79 in A431 cells (IC50: 2.6 nM) and MCF10A cells (IC50: 8.8 nM), effectively and selectively killing cells with MLL translocations. Compared to its analogue EPZ004777, SGC 0946 is more potent against DOT1L, making it promising for cancer research. Moreover, SGC 0946 demonstrates over 100-fold higher selectivity for DOT1L than other histone methyltransferases (HMTs).
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Storage & Handling

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

Alternative Names

TOV21G, SGC 0946, SGC0946, SGC-0946, cord blood cells, DOT1L, HistoneMethyltransferase, Histone Methyltransferase, Inhibitor, leukemia, ovarian cancer, Molm13 MLL, MLL-rearrange, inhibit

Compound Identifiers

PubChem CID

56962337