| Chemical Properties | Back Directory | [Boiling point ]
632.6±55.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (293.08 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.59±0.70(Predicted) | [color ]
White to off-white | [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) | [InChIKey]
IJHAXMJRQQTBPL-UHFFFAOYSA-N | [SMILES]
N#CC1(CCN(CC1)C2=C(C)C(C(NC3=CC=C(CN)C=C3)=O)=NC=N2)C4=CC=CC=C4 |
| Hazard Information | Back Directory | [Uses]
BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM[1]. | [Biological Activity]
BI8622 is a selective HUWE1 (HECTH9; MULE; ARF-BP1) inhibitor (IC50 = 3.2 μM by HUWE1 HECT-domain auto-ubiquitination assay; IC50 >50 μM against other HECT-domain Ub ligases tested). BI8622 inhibits the degradation of HUWE1 target proteiinsincluding MCL1 (IC50 = 6.8 μM; UV irradiated HeLa MCL1 transfectants)MIZ1 (10 μM; Ls174T)and TopBP1. BI8622 suppresses Ls174T colony formation (IC50 = 8.4 μM in 5 days) and the growth of three colon carcinoma cell lines (20 μM for 5 days; HCT116HT29SW480). | [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. DOI:10.15252/emmm.201403927 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|