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UNC669, L3MBTL1 Domain Inhibitor

UNC669, L3MBTL1 Domain Inhibitor

$89.00
A potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1
Catalog No. Unit Price Qty
M60083-5s 5mg solid $89.00
M60083-5 10 mM DMSO (1.479 mL) $89.00

Details

Product Information
Molecular Weight: 338.24
Formula: C15H20BrN3O
Purity: ≥ 98%
CAS#: 314241-44-5
Solubility: DMSO up to 50 mM
Chemical Name: (2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

UNC669 is a potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC669 binds L3MBTL1 with a Kd of 5±1 μM (IC50 = 6 ±0.5 μM), exhibiting 5-fold greater affinity than the cognate peptide H4K20Me1, 6-fold selective over its close homologue L3MBTL3 and 10-fold selective over L3MBTL4. The first cocrystal structure of UNC669 bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design. UNC669 can serve as a useful chemical tool to interrogate the functions of MBT proteins and probe methyl-lysine reader proteins as a target class.

 

How to Use:

  • In vitro:  UNC1215 was used at 10-25 µM final concentration in vitro and in cellular assays.
  • In vivo:   n/a

 

Reference:

  1. 1. Herold JM, et al. Small-molecule ligands of methyl-lysine binding proteins. (2011) J Med Chem. 54(7):2504-11.

 


Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 338.24
Formula: C15H20BrN3O
Purity: ≥ 98%
CAS#: 314241-44-5
Solubility: DMSO up to 50 mM
Chemical Name: (2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

UNC669 is a potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC669 binds L3MBTL1 with a Kd of 5±1 μM (IC50 = 6 ±0.5 μM), exhibiting 5-fold greater affinity than the cognate peptide H4K20Me1, 6-fold selective over its close homologue L3MBTL3 and 10-fold selective over L3MBTL4. The first cocrystal structure of UNC669 bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design. UNC669 can serve as a useful chemical tool to interrogate the functions of MBT proteins and probe methyl-lysine reader proteins as a target class.

 

How to Use:

  • In vitro:  UNC1215 was used at 10-25 µM final concentration in vitro and in cellular assays.
  • In vivo:   n/a

 

Reference:

  1. 1. Herold JM, et al. Small-molecule ligands of methyl-lysine binding proteins. (2011) J Med Chem. 54(7):2504-11.

 


Products are for research use only. Not for human use.

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