WH-4-023 Chemical Properties

Boiling point:

743.2±70.0 °C(Predicted)

Density 

1.247±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (60 mg/ml)

form 

powder

pka

7.89±0.42(Predicted)

color 

white to beige

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 month.

Safety Information

RIDADR 

UN 2811 6.1 / PGIII

WH-4-023 Usage And Synthesis

Description

WH-4-23 (837422-57-8) is a potent and selective inhibitor of Src family kinases Lck and Src, IC50=2 and 6 nM respectively.1,2 Also inhibits SIK, IC50=10, 22 and 60 nM for SIK 1, 2 and 3 respectively.3 May be used along with PD-325901 and CHIR-99021 to support self-renewal of na?ve human embryonic stem cells.4

Uses

WH-4-023 is a potent and selective dual lymphocyte-specific kinase (Lck) inhibitor.

Definition

ChEBI: N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]carbamic acid (2,6-dimethylphenyl) ester is a member of piperazines.

Biochem/physiol Actions

WH-4-023 (KIN112) is a potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src. WH-4-023 is a somewhat less potent inhibitor of salt-inducible kinases (SIKs) with IC50 values of 10, 22 and 60 nM for SIK 1, 2 and 3 respectively. WH-4-023 was found to support self-renewal of naive human embryonic stem cells, in particular in combination with PD 0325901 (PZ0162), CHIR99021 (SML1046), and SB-590885 (SML0501).

storage

Store at -20°C

References

[1] MATTHEW W. MARTIN. Novel 2-Aminopyrimidine Carbamates as Potent and Orally Active Inhibitors of Lck: Synthesis, SAR, and in Vivo Antiinflammatory Activity[J]. Journal of Medicinal Chemistry, 2006, 49 16: 4981-4991. DOI:10.1021/jm060435i
[2] JAMIE A. MOROCO. A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region[J]. Chemical Biology & Drug Design, 2014, 86 2: 144-155. DOI:10.1111/cbdd.12473
[3] KRISTOPHER CLARK. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2012: 16986-16991. DOI:10.1073/pnas.1215450109
[4] Systemic identification of culture conditions for introduction and maintenance of naïve human pluripotency

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