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WH-4-023

Catalog No. T1811 CAS 837422-57-8

Synonyms: KIN112, KIN001-112, Dual LCK/SRC inhibitor

WH-4-023 (Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

WH-4-023, CAS 837422-57-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 47.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 101.00
25 mg	In stock	$ 165.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 85.00

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Purity: 99.75%

Purity: 99.29%

Purity: 99.05%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	WH-4-023 (Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.
Targets&IC50	Lck:2 nM, Src:6 nM
In vitro	WH-4-023 shows little activity on p38 and KDR. [1]
Kinase Assay	The Lck HTRF kinase assay involves ATP-dependent phosphorylation of a biotinylated substrate peptide of gastrin in the presence or absence of inhibitor compound. The final concentration of gastrin is 1.2 μM. The final concentration of ATP is 0.5 μM (Km app =0.6±0.1 μM), and the final concentration of Lck (a GST-kinase domain fusion (AA 225?509)) is 250 pM. Buffer conditions are as follows: 50 mM HEPES pH=7.5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl2, 2 mM DTT, 0.05% BSA. The assay is quenched and stopped with 160 μL of detection reagent. Detection reagents are as follows: Buffer made of 50 mM Tris, pH=7.5, 100 mM NaCl, 3 mM EDTA, 0.05% BSA, 0.1% Tween20. Prior to reading, Streptavidin allophycocyanin (SA-APC) is added at a final concentration in the assay of 0.0004 mg/mL, along with europilated anti-phosphotyrosine Ab (Eu-anti-PY) at a final conc of 0.025 nM. The assay plate is read in a Discovery fluorescence plate reader with excitation at 320 nm and emission at 615 and 655 nm[1].
Cell Research	WH-4-023 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. The purpose of this assay is to test the potency of T cell receptor (TCR; CD3) and CD28 signaling pathway inhibitors in human T cells. T cells are purified from human peripheral blood lymphocytes (hPBL) and preincubated with or without compound prior to stimulation with a combination of an anti-CD3 and an anti-CD28 antibody in 96-well tissue culture plates (1×105 T cells/well). Cells are cultured for ~20 h at 37°C in 5% CO2 and then secreted IL-2 in the supernatants is quantified by cytokine ELISA. The cells remaining in the wells are then pulsed with 3H-thymidine overnight to assess the T cell proliferative response. Cells are harvested onto glass fiber filters and 3H-thymidine incorporation into DNA is analyzed by liquid scintillation counter. For comparison purposes, phorbol myristic acid (PMA) and calcium ionophore are used in combination to induce IL-2 secretion from purified T cells. Potential inhibitor compounds are tested for inhibition of this response as described above for anti-CD3 and -CD28 antibodies. Human whole-blood anti-CD3/CD28-induced IL-2 secretion assays are run in a similar fashion as described above using whole blood from normal volunteers diluted 50% in tissue culture medium prior to stimulation[1].

Synonyms	KIN112, KIN001-112, Dual LCK/SRC inhibitor
Molecular Weight	568.67
Formula	C32H36N6O4
CAS No.	837422-57-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 10 mg/mL (17.6 mM)

Ethanol: 6 mg/mL (10.55 mM), Heating is recommended.

References and Literature

1. Martin MW, et al. J Med Chem. 2006, 49(16), 4981-4991.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Anti-Cancer Metabolism Compound Library HIF-1 Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Reprogramming Compound Library

Related Products

Related compounds with same targets

CHIR-98014 PD180970 PD173955 TPX-0046 HPK1-IN-2 AD80 A-770041 PD173074

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

WH-4-023 837422-57-8 Angiogenesis Tyrosine Kinase/Adaptors Src WH 4 023 KIN112 inhibit Inhibitor KIN 112 KIN-112 KIN001-112 WH4023 Dual LCK/SRC inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.