WH-4-023
Synonym(s):2,6-Dimethylphenyl N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]carbamate;KIN112
- CAS NO.:837422-57-8
- Empirical Formula: C32H36N6O4
- Molecular Weight: 568.67
- MDL number: MFCD28138072
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is WH-4-023?
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
The Uses of WH-4-023
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
Properties of WH-4-023
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) |
pka | 7.89±0.42(Predicted) |
form | powder |
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 for WH-4-023
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral |
Precautionary Statement Codes |
P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. P405:Store locked up. P501:Dispose of contents/container to..… |
Computed Descriptors for WH-4-023
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