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1mg |
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5mg |
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10mg |
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Other Sizes |
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Purity: ≥98%
BI-8622 is a novel, potent and specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARF-BP1, MULE) associates with both MYC and the MYC-associated protein MIZ1.
ln Vitro |
BI8622 has an IC50 value of 6.8 μM and causes ectopic production of HUWE1 in HeLa cells, which eliminates ubiquitination of MCL1 [1]. With an approximate IC50 value of 8.4 μM, BI8622 suppresses the development of Ls174T cell colonies[1]. All phases of the cell cycle are delayed in Ls174T cells when treated with BI8622 (10 μM; 1-4 days), with the greatest effect occurring in G1 [1]. BI8622 (0-50 μM; 16 hours) inhibits HUWE1 in HeLa cells, delaying MCL1 degradation in response to UV exposure [1]. Colorectal cancer cells' MYC-dependent transactivation is inhibited by BI8622 [1].
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Cell Assay |
Cell Cycle Analysis[1]
Cell Types: Ls174T Cell Tested Concentrations: 0 μM, 5 μM, 10 μM, 15 μM, 20 μM Incubation Duration: 0-4 Days Experimental Results: Passaging of Ls174T cells was delayed in all phases of the cell cycle, G1 has the strongest effect. Western Blot Analysis [1] Cell Types: HeLa cells Tested Concentrations: 0 μM, 10 μM, 20 μM Incubation Duration: 16 hrs (hours) Experimental Results: Delaying the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells. |
References |
[1]. Peter S, et al. Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase. EMBO Mol Med. 2014 Dec;6(12):1525-41.
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Molecular Formula |
C25H26N6O
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Molecular Weight |
426.513544559479
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CAS # |
1875036-74-0
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SMILES |
O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4
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InChi Key |
IJHAXMJRQQTBPL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C25H26N6O/c1-18-22(24(32)30-21-9-7-19(15-26)8-10-21)28-17-29-23(18)31-13-11-25(16-27,12-14-31)20-5-3-2-4-6-20/h2-10,17H,11-15,26H2,1H3,(H,30,32)
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Chemical Name |
N-(4-(Aminomethyl)phenyl)-6-(4-cyano-4-phenylpiperidin-1-yl)-5-methylpyrimidine-4-carboxamide
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Synonyms |
BI8622; BI 8622; BI-8622
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~125 mg/mL (~293.08 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3446 mL | 11.7231 mL | 23.4461 mL | |
5 mM | 0.4689 mL | 2.3446 mL | 4.6892 mL | |
10 mM | 0.2345 mL | 1.1723 mL | 2.3446 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.