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WDR5-0103 is a potent and selective small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM). WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5. WD repeat domain 5 (WDR5) plays an important role in various biological functions through the epigenetic regulation of gene transcription.
| Molecular Weight | 383.44 |
| Formula | C21H25N3O4 |
| CAS Number | 890190-22-4 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| BIX 01294 Trihydrochloride
BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
| EPZ-5676
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| EPZ004777
EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. |
| 3-Deazaneplanocin A
3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM. |
| EPZ004777 hydrochloride
EPZ004777 hydrochloride is the hydrochloride salt of EPZ004777, which is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM. |
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