WH-4-023

Pricing Availability   Qty
Description: Potent and selective Lck and Src inhibitor; also inhibits SIK
Alternative Names: KIN112
Chemical Name: 2,6-Dimethylphenyl-N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]carbamate
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (3)

Biological Activity for WH-4-023

WH-4-023 is a potent and selective Lck and Src inhibitor (IC50 values are 2 and 6 nM respectively). Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases. Supports self-renewal of naive hESCs in combination with PD 0325901, CHIR 99021 and SB 590885.

External Portal Information for WH-4-023

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of WH-4-023 is reviewed on the chemical probes website.

Compound Libraries for WH-4-023

WH-4-023 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for WH-4-023

M. Wt 568.67
Formula C32H36N6O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 837422-57-8
PubChem ID 11844351
InChI Key NBTNHSGBRGTFJS-UHFFFAOYSA-N
Smiles O=C(OC5=C(C)C=CC=C5C)N(C4=CC=C(OC)C=C4OC)C1=NC(NC(C=C3)=CC=C3N2CCN(C)CC2)=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WH-4-023

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.87 100

Preparing Stock Solutions for WH-4-023

The following data is based on the product molecular weight 568.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.76 mL 8.79 mL 17.58 mL
5 mM 0.35 mL 1.76 mL 3.52 mL
10 mM 0.18 mL 0.88 mL 1.76 mL
50 mM 0.04 mL 0.18 mL 0.35 mL

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References for WH-4-023

References are publications that support the biological activity of the product.

Theunissen et al (2014) Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell 15 471 PMID: 25090446

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.U.S.A. 109 16986 PMID: 23033494

Martin et al (2006) Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J.Med.Chem. 49 4981 PMID: 16884310


If you know of a relevant reference for WH-4-023, please let us know.

View Related Products by Product Action

View all Src Kinase Inhibitors

Keywords: WH-4-023, WH-4-023 supplier, Potent, selective, Lck, Src, inhibitors, inhibits, self-renewal, ESC, lymphocyte, specific, kinase, salt, inducible, SIK, KIN112, Kinases, Other, Stem, Cell, Proliferation, 5413, Tocris Bioscience

2 Citations for WH-4-023

Citations are publications that use Tocris products. Selected citations for WH-4-023 include:

Gao et al (2019) Establishment of porcine and human expanded potential stem cells. Nat Cell Biol 21 687 PMID: 31160711

Shahbazi et al (2017) Pluripotent state transitions coordinate morphogenesis in mouse and human embryos. Nature 552 239 PMID: 29186120


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Reviews for WH-4-023

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Literature in this Area

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