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Catalog No. T11796LCas No. 2079885-05-3
Alias L-45
L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM).
L-Moses
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Catalog No. T11796LAlias L-45Cas No. 2079885-05-3
L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $3,368 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $3,980 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $5,500 | 8-10 weeks | 8-10 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM). |
| Targets&IC50 | BRD:126 nM (kd) |
| In vitro | L-45 binds in the acetylated lysines (KAc) -binding pocket of PfGCN (blue ribbon and sticks) and makes H-bonds (dotted lines) through the triazole to N1436 and the first of a network of four water molecules (red spheres). A structure using highly homologous (64?% identity) Brd from Plasmodium falciparum, PfGCN5, of which L-45 is also a potent ligand (isothermal titration calorimetry (ITC) KD 280 nM), is successfully obtained (PDB: 5TPX). L-45 disrupts PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains [1]. |
| In vivo | In human and mouse liver microsomes, L-45 displays no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability. It also supports its potential for in vivo use[1]. |
| Synonyms | L-45 |
| Molecular Weight | 360.46 |
| Formula | C21H24N6 |
| Cas No. | 2079885-05-3 |
| Smiles | C[C@H](Nc1nn2c(C)nnc2c2ccccc12)[C@@H](N(C)C)c1ccccc1 |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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