WH-4-023

Cat. No. 5413

WH-4-023 C32H36N6O4 [837422-57-8]

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Alternative Name: KIN112

Chemical Name: 2,6-Dimethylphenyl-N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]carbamate

Biological Activity

Potent and selective Lck and Src inhibitor (IC50 values are 2 and 6 nM respectively). Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases. Supports self-renewal of naive hESCs in combination with PD 0325901, CHIR 99021 and SB 590885.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of WH-4-023 is reviewed on the chemical probes website.

Technical Data

M.Wt:
568.67
Formula:
C32H36N6O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
837422-57-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Theunissen et al (2014) Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell 15 471. PMID: 25090446.

Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986. PMID: 23033494.

Martin et al (2006) Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J.Med.Chem. 49 4981. PMID: 16884310.

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Citations are publications that use Tocris products.

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View Related Products by Product Action

Keywords: WH-4-023, supplier, Potent, selective, Lck, Src, inhibitors, inhibits, self-renewal, ESC, lymphocyte, specific, kinase, salt, inducible, kinase, SIK, Tocris Bioscience, Src Kinase Inhibitor products

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