TL4-12

Name: TL4-12
Brand: Tocris Bioscience
SKU: 5910

Tocris Bioscience, part of Bio-Techne | Catalog # 5910

Citations (1)

COA / SDS

Potent MAP4K2 (GCK) inhibitor

Key Product Details

Description:	Potent MAP4K2 (GCK) inhibitor
Chemical Name:	4-Methyl-3-[[6-(methylamino)-4-pyrimidinyl]oxy]-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]benzamide
Purity:	≥98% (HPLC)
Molecular Weight:	500.53

View Full Technical Details for TL4-12

Technical Data
Citations

Biological Activity for TL4-12

TL4-12 is a potent MAP4K2 (GCK) inhibitor (IC₅₀ = 37 nM). Exhibits >70-fold selectivity for MAP4K2 over TAK1 (IC₅₀ = 2.7 μM for TAK1). Inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation, in vitro.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Compound Libraries for TL4-12

TL4-12 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for TL4-12

M. Wt	500.53
Formula	C₂₅H₂₇F₃N₆O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1620820-12-3
PubChem ID	134812827
InChi Key	HXKJJIMUMNPQQY-UHFFFAOYSA-N
Smiles	O=C(C1=CC=C(C)C(OC2=CC(NC)=NC=N2)=C1)NC3=CC(N4CCN(C)CC4)=CC(C(F)(F)F)=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for TL4-12

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	10.01	20
	1eq. HCl	10.01	20

Preparing Stock Solutions for TL4-12

The following data is based on the product molecular weight 500.53.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.99 mL	49.95 mL	99.89 mL
1 mM	2.00 mL	9.99 mL	19.98 mL
2 mM	1.00 mL	4.99 mL	9.99 mL
10 mM	0.20 mL	1.00 mL	2.00 mL

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References for TL4-12

References are publications that support the biological activity of the product.

Tan Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J.Med.Chem. 2015 PMID: 25075558