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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)
Literature (1)

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
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 Data for TL4-12

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 mL 9.99 mL 19.98 mL
2 mM 1 mL 4.99 mL 9.99 mL
10 mM 0.2 mL 1 mL 2 mL

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References for TL4-12

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

Tan et al (2015) Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J.Med.Chem. 58 183 PMID: 25075558

If you know of a relevant reference for TL4-12, please let us know.

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Keywords: TL4-12, TL4-12 supplier, MAP4K2, inhibitors, inhibits, mitogen, activated, protein, kinase, potent, Other, MAPK, 5910, Tocris Bioscience

Citations for TL4-12

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

MAPK Signaling Scientific Review

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.