An inhibitor of Lck and Src
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WH-4-023

Item No. 9002067

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-carbamic acid, 2,6-dimethylphenyl ester
CAS Number
837422-57-8
Molecular Formula
C32H36N6O4
Formula Weight
568.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 0.3 mg/ml
λmax
284 nm
SMILES
COC1=CC=C(N(C(OC2=C(C)C=CC=C2C)=O)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C3)C(OC)=C1
InChi Code
InChI=1S/C32H36N6O4/c1-22-7-6-8-23(2)30(22)42-32(39)38(27-14-13-26(40-4)21-28(27)41-5)29-15-16-33-31(35-29)34-24-9-11-25(12-10-24)37-19-17-36(3)18-20-37/h6-16,21H,17-20H2,1-5H3,(H,33,34,35)
InChi Key
NBTNHSGBRGTFJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    WH-4-023 is a selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively).1,2 It inhibits the related kinases p38α and KDR at >300-fold higher concentrations (IC50s = 1.3 and 0.65 µM, respectively).1 At 1 µM, it has been used in combination with PD 0325901 (Item No. 13034), CHIR99021 (Item No. 13122), and SB-590885 (Item No. 16643) to support self-renewal of naïve human embryonic stem cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Martin, M.W., Newcomb, J., Nunes, J.J., et al. Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J. Med. Chem. 49(16), 4981-4991 (2006).

    2. Moroco, J.A., Baumgartner, M.P., Rust, H.L., et al. 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(2), 144-155 (2015).

    3. Theunissen, T.W., Powell, B.E., Wang, H., et al. Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell 15(4), 471-487 (2014).