L Moses dihydrochloride

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L Moses dihydrochloride | Bromodomain Inhibitors
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Description: High affinity and selective PCAF bromodomain inhibitor

Chemical Name: (1S, 2S)-N1,N1-Dimethyl-N2-(3-methyl-1,2,4-triazolo[3,4-a]phthalazin-6-yl)-1-phenylpropane-1,2-diamine dihydrochloride

Purity: ≥98%

Product Details
Citations (1)

Biological Activity

L Moses dihydrochloride is a high affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM), which exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). L Moses exhibits >4500-fold selectivity for PCAF over BRD4. The compound inhibits Tunicamycin (Cat. No. 3516) -induced neuronal cell death by reversing the transcriptional changes associated with Tunicamycin treatment. L Moses exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC).

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of L-Moses is reviewed on the chemical probes website.

Technical Data

Soluble to 100 mM in water and to 100 mM in DMSO
Desiccate at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the L-Moses probe summary on the SGC website.

Background References

  1. Discovery of a PCAF bromodomain chemical probe.
    Moustakim et al.
    Angew.Chem.Int.Ed., 2017;56:827

Product Datasheets

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Citation for L Moses dihydrochloride

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