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

Martin et al. (2006), Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity; J. Med. Chem., 49 4981 Moroco et al. (2015), A discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region; Chem. Biol. Drug. Des., 86 144 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. USA, 109 16986 Theunissen et al. (2014), Systemic identification of culture conditions for introduction and maintenance of na?ve human pluripotency; Cell Stem Cell, 15 471

WH-4-023(837422-57-8)Related Product Information

• GW441756
• ZM 306416 hydrochloride
• 2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
• JX401
• JAK3 INHIBITOR II
• JAK3 INHIBITOR I
• 4-PHENYLAMINO-6,7-DIMETHOXYQUINAZOLINE
• 4-AMINO-3-CYANO-1,2,5,6-TETRAHYDROPYRIDINE
• 7-BROMO-1,2,3,4-TETRAHYDRO-QUINOLINE HYDROCHLORIDE
• Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-
• Y27632 (hydrochloride)
• Saracatinib
• SB590885
• PD 0325901
• IM-12
• Olaparib