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Purity: ≥98%
UNC669 (UNC-669) is a novel, potent and selective inhibitor of malignant brain tumor (MBT) with anticancer activity. It inhibits L3MBTL1/3 with IC50 of 4.2 and 3.1 μM, respectively, and shows 11-fold selectivity over L3MBTL4.
| ln Vitro |
L3MBTL1, a paralogue of Drosophila tumor suppressor lethal(3)malignant brain tumor (l(3)mbt), binds histones in a methylation state-dependent way and contributes to higher order chromatin structure and transcriptional repression. Similar to L3MBTL1, the closely related protein, L3MBTL3, also includes three MBT repeats and has been demonstrated to play a function in meduloblastoma production and normal hematopoiesis in humans[1][2].
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| References |
[1]. James LI, et al. Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem. 2013 Sep 26;56(18):7358-71.
[2]. Trojer P, et al. L3MBTL1, a histone-methylation-dependent chromatin lock. Cell. 2007;129(5):915-928. [3]. Baughman BM, et al. The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer [retracted in: ACS Chem Biol. 2018 Jan 19;13(1):281]. ACS Chem Biol. 2016;11(3):722-728. |
| Molecular Formula |
C15H20BRN3O
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| Molecular Weight |
338.24
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| CAS # |
1314241-44-5
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| SMILES |
BrC1=C([H])N=C([H])C(=C1[H])C(N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9565 mL | 14.7824 mL | 29.5648 mL | |
| 5 mM | 0.5913 mL | 2.9565 mL | 5.9130 mL | |
| 10 mM | 0.2956 mL | 1.4782 mL | 2.9565 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.
A) ITC binding curve of 14 (UNC669) to wt L3MBTL1 overlayed with the titration using the D355A mutant of L3MBTL1. B) Co-crystal structure of 14 with L3MBTL1. C) Binding curve for 14 in a FP displacement assay with FAM-H3K9Me1. J Med Chem. 2011 Apr 14; 54(7): 2504–2511.
Structures of monobasic MBT domain inhibitors.J Med Chem. 2013 Sep 26;56(18):7358-71. |
Mero76-1co-localizes with GFP-L3MBTL3 in the nucleus in HEK293 cells (row 1), and compounds1,2, and56(1 equivalent relative to mero76-1; rows 2 – 4) all displace mero76-1from GFP-L3MBTL3 (red is mero76-1; green is GFP-L3MBTL3; blue is Hoechst).J Med Chem. 2013 Sep 26;56(18):7358-71. |
Scatter plot showing the excellent, linear correlation between L3MBTL3 AlphaScreen data and L3MBTL3 TR-FRET data.
Western analysis of biotin-1pull-down experiments in G-401 cell lysates.J Med Chem. 2013 Sep 26;56(18):7358-71. |
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