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WH-4-023
Synonyms: KIN001-112, KIN112, Dual LCK/SRC inhibitor
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.
WH-4-023 Chemical Structure
CAS No. 837422-57-8
Purity & Quality Control
Batch:
Purity:
99.93%
99.93
WH-4-023 Related Products
| Related Targets | Lck Fyn Lyn Yes Fgr | Click to Expand |
|---|---|---|
| Related Products | Saracatinib (AZD0530) PP2 SU6656 PP1 Src Inhibitor 1 RK 24466 Myristic Acid eCF506 Tolimidone (MLR-1023) UM-164 | Click to Expand |
| Related Compound Libraries | Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library | Click to Expand |
Signaling Pathway
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| EM-2 | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0μM | SANGER | |||
| LAMA-84 | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.0000038μM | SANGER | |||
| EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000095μM | SANGER | |||
| MEG-01 | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.0000163μM | SANGER | |||
| CTV-1 | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.0000318μM | SANGER | |||
| BL-70 | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=0.0000472μM | SANGER | |||
| K-562 | Growth inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.0001617μM | SANGER | |||
| BV-173 | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.0005143μM | SANGER | |||
| DOHH-2 | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=0.0005969μM | SANGER | |||
| A704 | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=0.001268μM | SANGER | |||
| NCI-SNU-16 | Growth inhibition assay | Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50=0.01572μM | SANGER | |||
| LC-2-ad | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=0.02033μM | SANGER | |||
| LB2518-MEL | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.04667μM | SANGER | |||
| D-336MG | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.04681μM | SANGER | |||
| LB996-RCC | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=0.05668μM | SANGER | |||
| Becker | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50=0.06381μM | SANGER | |||
| LB1047-RCC | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=0.07592μM | SANGER | |||
| KS-1 | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.07758μM | SANGER | |||
| MPP-89 | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=0.08229μM | SANGER | |||
| RXF393 | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.10633μM | SANGER | |||
| LB831-BLC | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=0.12715μM | SANGER | |||
| HUTU-80 | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.17529μM | SANGER | |||
| A498 | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=0.18945μM | SANGER | |||
| MZ1-PC | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.22716μM | SANGER | |||
| TE-8 | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.23924μM | SANGER | |||
| MFH-ino | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.23925μM | SANGER | |||
| TE-15 | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.24276μM | SANGER | |||
| NTERA-S-cl-D1 | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=0.28855μM | SANGER | |||
| COLO-829 | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.31212μM | SANGER | |||
| SW684 | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay, IC50=0.32588μM | SANGER | |||
| OS-RC-2 | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.35011μM | SANGER | |||
| IST-MES1 | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=0.35723μM | SANGER | |||
| SNB75 | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay, IC50=0.35774μM | SANGER | |||
| SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.37163μM | SANGER | |||
| RCC10RGB | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=0.42631μM | SANGER | |||
| VA-ES-BJ | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=0.46261μM | SANGER | |||
| NCI-H1648 | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.51582μM | SANGER | |||
| PF-382 | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=0.70763μM | SANGER | |||
| Daudi | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=0.71411μM | SANGER | |||
| SW982 | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.85819μM | SANGER | |||
| SW872 | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.86458μM | SANGER | |||
| TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.88831μM | SANGER | |||
| HOP-62 | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.91599μM | SANGER | |||
| NOS-1 | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.95045μM | SANGER | |||
| BL-41 | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=1.00013μM | SANGER | |||
| TGBC24TKB | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50=1.03831μM | SANGER | |||
| KGN | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50=1.0521μM | SANGER | |||
| TK10 | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50=1.08418μM | SANGER | |||
| GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=1.16064μM | SANGER | |||
| GCIY | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay, IC50=1.2301μM | SANGER | |||
| LXF-289 | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.27256μM | SANGER | |||
| RL95-2 | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=1.32436μM | SANGER | |||
| SW962 | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay, IC50=1.33742μM | SANGER | |||
| HT-144 | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50=1.44517μM | SANGER | |||
| IST-SL2 | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=1.47421μM | SANGER | |||
| NB6 | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50=1.69698μM | SANGER | |||
| SF126 | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=1.73178μM | SANGER | |||
| BOKU | Growth inhibition assay | Inhibition of human BOKU cell growth in a cell viability assay, IC50=1.80527μM | SANGER | |||
| BB30-HNC | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.85472μM | SANGER | |||
| KLE | Growth inhibition assay | Inhibition of human KLE cell growth in a cell viability assay, IC50=1.86232μM | SANGER | |||
| MLMA | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50=1.9231μM | SANGER | |||
| KINGS-1 | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=1.96897μM | SANGER | |||
| ES6 | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50=2.05401μM | SANGER | |||
| SH-4 | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay, IC50=2.12055μM | SANGER | |||
| EB-3 | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay, IC50=2.15824μM | SANGER | |||
| KURAMOCHI | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=2.24236μM | SANGER | |||
| D-263MG | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay, IC50=2.28853μM | SANGER | |||
| SF268 | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50=2.48682μM | SANGER | |||
| NB17 | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay, IC50=2.62875μM | SANGER | |||
| DMS-114 | Growth inhibition assay | Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=2.79022μM | SANGER | |||
| MC116 | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay, IC50=2.85704μM | SANGER | |||
| MZ2-MEL | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=3.08643μM | SANGER | |||
| GI-ME-N | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=3.25166μM | SANGER | |||
| 697 | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=3.39644μM | SANGER | |||
| ACN | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay, IC50=4.22607μM | SANGER | |||
| TE-10 | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay, IC50=4.2795μM | SANGER | |||
| LS-123 | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay, IC50=4.35584μM | SANGER | |||
| TE-9 | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay, IC50=4.39183μM | SANGER | |||
| CAS-1 | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=4.4023μM | SANGER | |||
| BB65-RCC | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=4.69952μM | SANGER | |||
| MRK-nu-1 | Growth inhibition assay | Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=4.71792μM | SANGER | |||
| NCI-H1355 | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.87685μM | SANGER | |||
| KP-N-YS | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50=4.92086μM | SANGER | |||
| MZ7-mel | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=5.09269μM | SANGER | |||
| NCI-H747 | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=5.74159μM | SANGER | |||
| C2BBe1 | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=5.78469μM | SANGER | |||
| RPMI-6666 | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.9621μM | SANGER | |||
| PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.16376μM | SANGER | |||
| TE-1 | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50=6.71768μM | SANGER | |||
| ETK-1 | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=7.6356μM | SANGER | |||
| ST486 | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=8.27227μM | SANGER | |||
| KU812 | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.38738μM | SANGER | |||
| EHEB | Growth inhibition assay | Inhibition of human EHEB cell growth in a cell viability assay, IC50=9.0509μM | SANGER | |||
| IMR-5 | Growth inhibition assay | Inhibition of human IMR-5 cell growth in a cell viability assay, IC50=9.28459μM | SANGER | |||
| BB49-HNC | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=9.96548μM | SANGER | |||
| NCI-H1581 | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=10.3373μM | SANGER | |||
| CP66-MEL | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=10.6469μM | SANGER | |||
| NMC-G1 | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.0324μM | SANGER | |||
| SIMA | Growth inhibition assay | Inhibition of human SIMA cell growth in a cell viability assay, IC50=11.2916μM | SANGER | |||
| A101D | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=11.8487μM | SANGER | |||
| IST-MEL1 | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=12.5986μM | SANGER | |||
| no-10 | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay, IC50=13.1434μM | SANGER | |||
| KALS-1 | Growth inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=13.16μM | SANGER | |||
| GI-1 | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay, IC50=13.2491μM | SANGER | |||
| ONS-76 | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.3728μM | SANGER | |||
| D-247MG | Growth inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay, IC50=13.7709μM | SANGER | |||
| NCI-H446 | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50=14.1409μM | SANGER | |||
| NALM-6 | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=14.2358μM | SANGER | |||
| SK-N-DZ | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=14.442μM | SANGER | |||
| QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=14.5247μM | SANGER | |||
| MHH-NB-11 | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=14.6569μM | SANGER | |||
| A388 | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50=14.6758μM | SANGER | |||
| EVSA-T | Growth inhibition assay | Inhibition of human EVSA-T cell growth in a cell viability assay, IC50=15.2484μM | SANGER | |||
| JVM-2 | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=16.4704μM | SANGER | |||
| EW-16 | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50=17.7718μM | SANGER | |||
| CP67-MEL | Growth inhibition assay | Inhibition of human CP67-MEL cell growth in a cell viability assay, IC50=18.5863μM | SANGER | |||
| NB13 | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=19.0437μM | SANGER | |||
| NCCIT | Growth inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay, IC50=20.0093μM | SANGER | |||
| SNU-C2B | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=20.5124μM | SANGER | |||
| SK-NEP-1 | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=22.2335μM | SANGER | |||
| TE-6 | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50=22.3864μM | SANGER | |||
| HCE-4 | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=22.927μM | SANGER | |||
| TGBC1TKB | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50=23.3177μM | SANGER | |||
| L-540 | Growth inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay, IC50=23.3231μM | SANGER | |||
| 8-MG-BA | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.9588μM | SANGER | |||
| OPM-2 | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=25.106μM | SANGER | |||
| MHH-PREB-1 | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=26.2134μM | SANGER | |||
| ALL-PO | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=26.6132μM | SANGER | |||
| LB771-HNC | Growth inhibition assay | Inhibition of human LB771-HNC cell growth in a cell viability assay, IC50=27.8393μM | SANGER | |||
| NEC8 | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50=29.0389μM | SANGER | |||
| MSTO-211H | Growth inhibition assay | Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=29.059μM | SANGER | |||
| ATN-1 | Growth inhibition assay | Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=29.7028μM | SANGER | |||
| LB373-MEL-D | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=29.7129μM | SANGER | |||
| NB69 | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=30.374μM | SANGER | |||
| LOXIMVI | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.8334μM | SANGER | |||
| HC-1 | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50=32.8423μM | SANGER | |||
| SK-UT-1 | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=32.9447μM | SANGER | |||
| KARPAS-422 | Growth inhibition assay | Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=33.2528μM | SANGER | |||
| KP-N-RT-BM-1 | Growth inhibition assay | Inhibition of human KP-N-RT-BM-1 cell growth in a cell viability assay, IC50=33.8198μM | SANGER | |||
| SIG-M5 | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=34.6805μM | SANGER | |||
| TE-11 | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50=38.0936μM | SANGER | |||
| RKO | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=38.4067μM | SANGER | |||
| LS-411N | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay, IC50=38.8809μM | SANGER | |||
| OCUB-M | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=40.2533μM | SANGER | |||
| OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=40.5786μM | SANGER | |||
| JiyoyeP-2003 | Growth inhibition assay | Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=41.2672μM | SANGER | |||
| no-11 | Growth inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay, IC50=41.8283μM | SANGER | |||
| NCI-H1694 | Growth inhibition assay | Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=43.3351μM | SANGER | |||
| IST-SL1 | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=46.6838μM | SANGER | |||
| T cells | Function assay | Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells, IC50=1.9μM | 16884310 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| Click to View More Cell Line Experimental Data | ||||||
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 |
|
| In vitro | ||||
| In vitro | WH-4-023 shows little activity on p38 and KDR. [1] |
|||
|---|---|---|---|---|
| Kinase Assay | Lck 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 MnCl, 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. Assays for other kinases are done in a similar way as described above, varying the concentrations of enzyme, peptide substrate, and ATP added to the reaction, depending on the specific activity of the kinase and measured Kms for the substrates. | ||||
Chemical Information & Solubility
| Molecular Weight | 568.67 | Formula | C32H36N6O4 |
| CAS No. | 837422-57-8 | SDF | Download WH-4-023 SDF |
| 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 | ||
| Storage (From the date of receipt) | |||
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In vitro |
DMSO : 12 mg/mL ( (21.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 6 mg/mL Water : Insoluble |
Molecular Weight Calculator |
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In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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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.
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