AssayQuantのKinSight™ Phosphatase Profilingでは、独自のPhosphoSens® Technologyを用いることにより、反応全体を通じて基質のリン酸化/脱リン酸化をリアルタイムで直接測定することが可能です。Nativeなリン酸化部位モチーフに基づいて設計された最適なリン酸化ペプチド基質により、End-pointでの阻害率評価だけでは得られない、Kinetic dataを取得できます。
Deliverables;
Detailed Kinetic Report for each compound that includes % inhibition presented in:
Numerical Format (Tabular), % inhibition for each enzyme
Graphical Format (Waterfall Plot), % inhibition for each enzyme
Graphical Format (Waterfall Plot), >70% inhibition
Visual Format (Kinome Tree), >70% inhibition
Also includes annotated progress curves for any exploitable mechanisms of actions (TDI).
KinSight™ Phosphatase Selectivity Profiling
| Target name | Approved Full Name | Ser (S), Thr (T), Tyr (Y) | |
|---|---|---|---|
| 1 | CDC25A | cell division cycle 25A | Dual (Y) |
| 2 | CDC25B | cell division cycle 25B | Dual (Y) |
| 3 | CDC25C | cell division cycle 25C | Dual (Y) |
| 4 | DUSP22 (JSP-1, LMW-DSP2, MKPX) | dual specificity phosphatase 22 | Dual |
| 5 | DUSP3 (VHR) | dual specificity phosphatase 3 | Dual (Y) |
| 6 | PPM1A (PP2Ca, PP2CA) | protein phosphatase, Mg2+/Mn2+ dependent 1A | S/T |
| 7 | PPM1D (WIP1, PP2C-delta) | protein phosphatase, Mg2+/Mn2+ dependent 1D | S/T |
| 8 | PPM1G (PP2Cg) | protein phosphatase, Mg2+/Mn2+ dependent 1G | S/T |
| 9 | PPM1F (CamKPase) | protein phosphatase, Mg2+/Mn2+ dependent 1F | S/T |
| 10 | PPP1CA (PP1A/PPP1A) | protein phosphatase 1 catalytic subunit alpha | S/T |
| 11 | PPP1CB (PP1B, PPP1B) | protein phosphatase 1 catalytic subunit beta | S/T |
| 12 | PPP2CA (PP2A α, RP-C) | protein phosphatase 2 catalytic subunit alpha | S/T |
| 13 | PPP2CB (PP2Abeta) | protein phosphatase 2 catalytic subunit beta | S/T |
| 14 | PPP3CA/B (Calcineurin A/B, CNA alpha/beta, CALNA/B) | protein phosphatase 3 catalytic subunit alpha/beta | S/T |
| 15 | PTPN1 (PTP1B, PTB1B) | protein tyrosine phosphatase non-receptor type 1 | Y |
| 16 | PTPN2 (TCPTP, PTPT) | protein tyrosine phosphatase non-receptor type 2 | Y |
| 17 | PTPN4 (MEG1) | protein tyrosine phosphatase non-receptor type 4 | Y |
| 18 | PTPN5 (STEP) | protein tyrosine phosphatase non-receptor type 5 | Y |
| 19 | PTPN6 (SHP 1, PTP-1C) | protein tyrosine phosphatase non-receptor type 6 | Y |
| 20 | PTPN7 (HEPTP, LC-PTP) | protein tyrosine phosphatase non-receptor type 7 | Y |
| 21 | PTPN9 (MEG2) | protein tyrosine phosphatase non-receptor type 9 | Y |
| 22 | PTPN11 (SHP 2, PTP2C, PTP1D) | protein tyrosine phosphatase non-receptor type 11 | Y |
| 23 | PTPN12 (PTP-PEST, PTPG1) | protein tyrosine phosphatase non-receptor type 12 | Y |
| 24 | PTPN13 (FAP-1, PTP-BAS, PTP-E1, PNP1) | protein tyrosine phosphatase non-receptor type 13 | Y |
| 25 | PTPN22 (PTPN8, Lyp) | protein tyrosine phosphatase non-receptor type 22 | Y |
| 26 | PTPRA (R-PTP-alpha, PTPA, LRP) | protein tyrosine phosphatase receptor type A | Y |
| 27 | PTPRB (R-PTP-beta, VE-PTP) | protein tyrosine phosphatase receptor type B | Y |
| 28 | PTPRC (L-CA, CD45, T200) | protein tyrosine phosphatase receptor type C | Y |
| 29 | PTPRE (R-PTP-epsilon) | protein tyrosine phosphatase receptor type E | Y |
| 30 | PTPRF (LAR) | protein tyrosine phosphatase receptor type F | Y |
| 31 | PTPRG (R-PTP-gamma) | protein tyrosine phosphatase receptor type G | Y |
| 32 | PTPRJ (R-PTP-eta, DEP1, CD148) | protein tyrosine phosphatase receptor type J | Y |
| 33 | PTPRM (PTPµ, PTPRL1, R-PTP-mu) | protein tyrosine phosphatase receptor type M | Y |
| 34 | PTPRS (R-PTP-sigma) | protein tyrosine phosphatase receptor type S | Y |