WH-4-023

For research use only.

Catalog No.S7565 Synonyms: KIN001-112, KIN112, Dual LCK/SRC inhibitor

7 publications

WH-4-023 Chemical Structure

CAS No. 837422-57-8

WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, 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.

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Selleck's WH-4-023 has been cited by 7 publications

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  • (G-I) WB analysis of total LCK, LCK Y505, and Src Y416 expression in ALL-SIL, CCRF-CEM, and TALL-1. Cells were treated with DMSO only (Ctrl), dasatinib, bosutinib, nintedanib, or WH-4-023 overnight at the compound concentrations corresponding to the GI50 at 48 hr. Bos, bosutinib; Das, dasatinib; Nint, nintedanib; WH, WH-4-023.

    Blood, 2017, 130(25):2750-2761. WH-4-023 purchased from Selleck.

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Description WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, 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.
Targets
Lck [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
2 nM 6 nM
In vitro

WH-4-023 shows little activity on p38 and KDR. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EM-2 NWG0dplOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEnVfpZKdmirYnn0bY9vKG:oIHj1cYFvKEWPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2w{txO MlftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE{OTByLze+V2FPT0WUPD;hQi=>
LAMA-84 NGWxW3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2OwbGlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODByMECzPO69VQ>? MkTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE{OTByLze+V2FPT0WUPD;hQi=>
EoL-1-cell NUXMNWtuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWnHSHNsUW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wNFAxODl3zszN NFy5R|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTNzMECvK|5USU6JRWK8M4E,
MEG-01 NFjRVVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPn[VVKUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByMECxOlPPxE1? MmP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE{OTByLze+V2FPT0WUPD;hQi=>
CTV-1 NVKyPIlTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4myXWlvcGmkaYTpc44hd2ZiaIXtZY4hS1SYLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlAxODB|MUlOwG0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVMyODBxJ{7TRW5ITVJ:L3G+
BL-70 MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGJNNTdyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wNFAxPDd{zszN NEfXXIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTNzMECvK|5USU6JRWK8M4E,
K-562 MnW5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjRfFFKdmirYnn0bY9vKG:oIHj1cYFvKEtvNU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xODBzNkG3{txO M2ToNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyOzFyMD:nQnNCVkeHUkyvZV4>
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DOHH-2 NVzDOZhbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXnJcohq[mm2aX;uJI9nKGi3bXHuJGRQUEhvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFAxPTl4Od88US=> NY\COphzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF|MUCwM{c,W0GQR1XSQE9iRg>?
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LB2518-MEL NWiycnJ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGDuNGJKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC0OlY4|ryP NX7QeoJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF|MUCwM{c,W0GQR1XSQE9iRg>?
D-336MG NUTxRWp2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXWw[Y9XUW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNE[4Ne69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVMyODBxJ{7TRW5ITVJ:L3G+
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LB1047-RCC MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1W1WWlvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEe1PVLPxE1? Mo\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE{OTByLze+V2FPT0WUPD;hQi=>
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LB831-BLC NFfDeWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGxDQDNzLVLMR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ5MUZOwG0> NVT6VWF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF|MUCwM{c,W0GQR1XSQE9iRg>?
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... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 12 mg/mL warmed (21.1 mM)
Water Insoluble
Ethanol '6 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 568.67
Formula

C32H36N6O4

CAS No. 837422-57-8
Storage powder
in solvent
Synonyms KIN001-112, KIN112, Dual LCK/SRC inhibitor
Smiles CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID