WH-4-023

WH-4-023 Property

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

RIDADR 

UN 2811 6.1 / PGIII

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P405Store locked up.

P501Dispose of contents/container to..…

WH-4-023 Chemical Properties,Usage,Production

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