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Submit ReviewL Moses dihydrochloride
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% (HPLC)
Biological Activity for L Moses dihydrochloride
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).
Licensing Information
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.
External Portal Information for L Moses dihydrochloride
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.
Compound Libraries for L Moses dihydrochloride
L Moses dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for L Moses dihydrochloride
| M. Wt | 433.38 |
| Formula | C21H24N6.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 2922480-38-2 |
| PubChem ID | 131698638 |
| InChI Key | MSFPLTWUFWOKBX-IFXJQAMLSA-N |
| Smiles | C[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC2=NN3C(C)=NN=C3C4=CC=CC=C24 |
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.
Solubility Data for L Moses dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 | ||
| DMSO | 100 |
Preparing Stock Solutions for L Moses dihydrochloride
The following data is based on the product molecular weight 433.38. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.31 mL | 11.54 mL | 23.07 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for L Moses dihydrochloride
References for L Moses dihydrochloride
References are publications that support the biological activity of the product.
Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID: 27966810
Pavlou et al (2023) CRISPR-Cas9 genetic screen leads to the discovery of L-Moses, a KAT2B inhibitor that attenuates Tunicamycin-mediated neuronal cell death. Sci Rep 13 3934 PMID: 36894612
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Keywords: L Moses dihydrochloride, L Moses dihydrochloride supplier, PCAF, p300/CBP-associated, factor, GCN5, general, control, non-derepressible, 5, inhibitors, inhibits, high, affinity, selective, cell-permeable, 2079885-05-3, KAT2B, lysine, acetyltransferase, 2B, neuroprotectant, neuroprotection, Bromodomains, 6251, Tocris Bioscience
1 Citation for L Moses dihydrochloride
Citations are publications that use Tocris products. Selected citations for L Moses dihydrochloride include:
Pavlou et al (2023) CRISPR-Cas9 genetic screen leads to the discovery of L-Moses, a KAT2B inhibitor that attenuates Tunicamycin-mediated neuronal cell death. Sci.Rep. 13 3934 PMID: 36894612
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