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WDR5-0103

Cat. No. M9004
WDR5-0103 Structure
Synonym:

WD-Repeat Protein 5-0103

Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 383.44
Formula C21H25N3O4
CAS Number 890190-22-4
Purity >97%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction.
Li DD, et al. Bioorg Med Chem. 2016 Nov 15;24(22):6109-6118. PMID: 27720555.

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra G, et al. Biochem J. 2013 Jan 1;449(1):151-9. PMID: 22989411.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WDR5-0103, WD-Repeat Protein 5-0103 supplier, Histone Methyltransferase, inhibitors

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