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Submit ReviewPF 06260933 dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.
Sold for research purposes under agreement from Pfizer Inc.
PF 06260933 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 369.68 |
Formula | C16H13ClN4.2HCl |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 1883548-86-4 |
PubChem ID | 118701007 |
InChI Key | VRQXEOPUAQLBQI-UHFFFAOYSA-N |
Smiles | NC1=NC=C(C3=CN=C(N)C=C3)C=C1C2=CC=C(Cl)C=C2.Cl.Cl |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 36.97 | 100 | |
DMSO | 7.39 | 20 |
The following data is based on the product molecular weight 369.68. 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 |
---|---|---|---|
1 mM | 2.71 mL | 13.53 mL | 27.05 mL |
5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
References are publications that support the biological activity of the product.
Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID: 26617966
If you know of a relevant reference for PF 06260933 dihydrochloride, please let us know.
Keywords: PF 06260933 dihydrochloride, PF 06260933 dihydrochloride supplier, PF06260933, dihydrochloride, MAP4K4, HGK, inhibitors, inhibits, antidiabetic, diabetes, MINK, TNIK, mitogen-activated, kinases, hepatocyte, germinal, pogenitor, kinase-like, center, kinase, Other, MAPK, Kinases, 5752, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PF 06260933 dihydrochloride include:
Sebastian et al (2019) Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol 26 1703-1715.e37 PMID: 31676236
Gao et al (2017) MAP4K4 is a novel MAPK/ERK pathway regulator required for lung adenocarcinoma maintenance. Mol Oncol 11 628 PMID: 28306189
Do you know of a great paper that uses PF 06260933 dihydrochloride from Tocris? Please let us know.
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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.
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.