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| | WH-4-023 Basic information |
| Product Name: | WH-4-023 | | Synonyms: | WH-4-023;2,6-DIMETHYLPHENYL 2,4-DIMETHOXYPHENYL(2-(4-(4-METHYLPIPERAZIN-1-YL)PHENYLAMINO)PYRIMIDIN-4-YL)CARBAMATE;Carbamic acid, N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-, 2,6-dimethylphenyl ester;KIN001-112;KIN112;2,6-dimethylphenyl (2,4-dimethoxyphenyl)(2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamate WH-4-023;WH-4-023 2,6-DIMETHYLPHENYL 2,4-DIMETHOXYPHENYL(2-(4-(4-METHYLPIPERAZIN-1-YL)PHENYLAMINO)PYRIMIDIN-4-YL)CARBAMATE;WH-4-023, >=98% | | CAS: | 837422-57-8 | | MF: | C32H36N6O4 | | MW: | 568.67 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 837422-57-8.mol |  |
| | 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. |
| 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 Preparation Products And Raw materials |
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