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UNC1215, L3MBTL3 Domain Inhibitor

UNC1215, L3MBTL3 Domain Inhibitor

$119.00
A highly potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL3.
Catalog No. Unit Price Qty
M60084-5s 5mg solid $119.00
M60084-5 10 mM DMSO (0.944 mL) $119.00

Details

Product Information
Molecular Weight: 529.34
Formula: C32H43N5O2
Purity: ≥ 98%
CAS#: 1415800-43-9
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:

UNC1215 is a highly potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC1215 binds to L3MBTL3 with a Kd of 120 nM (IC50 ~ 20 nM), competitively displacing mono- or dimethyl-lysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family.  It also displays >100-fold selectivity over a panel of more than 200 histone methyltransferases, kinases, ion channels and 7-TM receptors. In cells, UNC1215 is nontoxic and directly binds to L3MBTL3 via the Kme-binding pocket of the MBT domains. It increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization. UNC1215 was used to reveal a new Kme-dependent interaction of L3MBTL3 with BCLAF1, a protein implicated in DNA damage repair and apoptosis. UNC1215 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 1-5 µM final concentration in vitro and in cellular assays.
  • In vivo:   n/a

 

Reference:

 1. James Li, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. (2013) Nat Chem Biol. In press.


    

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


Description

Details

Product Information
Molecular Weight: 529.34
Formula: C32H43N5O2
Purity: ≥ 98%
CAS#: 1415800-43-9
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:

UNC1215 is a highly potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC1215 binds to L3MBTL3 with a Kd of 120 nM (IC50 ~ 20 nM), competitively displacing mono- or dimethyl-lysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family.  It also displays >100-fold selectivity over a panel of more than 200 histone methyltransferases, kinases, ion channels and 7-TM receptors. In cells, UNC1215 is nontoxic and directly binds to L3MBTL3 via the Kme-binding pocket of the MBT domains. It increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization. UNC1215 was used to reveal a new Kme-dependent interaction of L3MBTL3 with BCLAF1, a protein implicated in DNA damage repair and apoptosis. UNC1215 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 1-5 µM final concentration in vitro and in cellular assays.
  • In vivo:   n/a

 

Reference:

 1. James Li, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. (2013) Nat Chem Biol. In press.


    

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


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