KinaseProfiler Reference Inhibitors
As the leaders in functional enzyme profiling, we at Millipore value the trust our customers place in us for superior quality data, and we pride ourselves on our continued process improvements. As part of this ongoing effort, Millipore has introduced new processes in adding reference inhibitors to each plate in our KinaseProfiler™ and IC50Profiler™ services.
As of July 31, 2009, these new processes include:
- A chosen inhibitor for each specific kinase will be added to each plate in duplicate at a concentration known to result in complete inhibition. This replaces the previous process of using acid blanks.
- A full 8 point reference curve will be run for each new batch of kinase with stringent upper and lower limits for the reference inhibitor IC50 value. This batch validation is your assurance that your data meet the strictest quality control standards.
- For kinases where no known inhibitor exists, 30% phosphoric acid will replace the inhibitor blank (see table below)
These process improvements will allow us to build a framework to deliver continued reductions in project turnaround times while maintaining our strict quality control standards.
The reference inhibitors used in KinaseProfiler are listed below, grouped with the appropriate protein kinases.
| ERK Inhibitor II |
| MAPK1(h), MAPK2(h) and MAPK2(m) |
| JAK Inhibitor I |
| AMPK(r), Aurora-A(h), BrSK1(h), CaMKIIβ(h), CaMKIIγ(h), CaMKIIδ(h), CaMKIδ(h), CHK2(I157T)(h), CHK2(R145W)(h), JNK1α1(h), JNK2α2(h), JNK3(h), MARK1(h), Mer(h), MSSK1(h), NEK3(h), NEK6(h), NEK7(h), NLK(h), PAR-1Bα(h), PDK1(h), PhKγ2(h), PKG1α(h), PKG1β(h), Rsk1(h), Rsk2(h), Rsk3(h), Rsk4(h), SAPK2a(T106M)(h), TBK1(h), TSSK1(h), WNK2(h), WNK3(h) |
| JNK Inhibitor II |
| CK1γ1(h), CK1γ2(h), CK1γ3(h), CK2(h), CK2α2(h), HIPK1(h), JAK2(h), JAK3(h), PDGFRα(D842V)(h), TrkB(h) |
| PI-103 |
| mTOR(h) |
| Rapamycin |
| mTOR/FKBP12(h) |
| PP2 |
| EphB3(h), EphB4(h) |
| Ro 31-8220 |
| Blk(m) |
| SB203580 |
| c-RAF(h), SAPK2a(h), SAPK2b(h), VRK2(h) |
| ST638 |
| ALK4(h), eEF-2K(h), EGFR(T790M,L858R)(h) |
| Staurosporine |
| Abl (H396P)(h), Abl (M351T)(h), Abl (Q252H)(h), Abl(h), Abl(m), Abl(T315I)(h), Abl(Y253F)(h), ACK1(h), ALK(h), Arg(h), Arg(m), ARK5(h), ASK1(h), Axl(h), Bmx(h), BRK(h), BrSK2(h), BTK(h), BTK(R28H)(h), CaMKI(h), CaMKII(r), CaMKIV(h), CDK1/cyclinB(h), CDK2/cyclinA(h), CDK2/cyclinE(h), CDK3/cyclinE(h), CDK5/p25(h), CDK5/p35(h), CDK6/cyclinD3(h), CDK7/cyclinH/MAT1(h), CDK9/cyclin T1(h), CHK1(h), CHK2(h), CK1(y), CK1δ(h), cKit(D816H)(h), cKit(D816V)(h), cKit(h), cKit(V560G)(h), cKit(V654A)(h), CLK2(h), CLK3(h), CSK(h), cSRC(h), DAPK1(h), DAPK2(h), DCAMKL2(h), DDR2(h), DMPK(h), DRAK1(h), DYRK2(h), EGFR(h), EGFR(L858R)(h), EGFR(L861Q)(h), EGFR(T790M)(h), EphA1(h), EphA2(h), EphA3(h), EphA4(h), EphA5(h), EphA7(h), EphA8(h), EphB1(h), EphB2(h), ErbB4(h), FAK(h), Fer(h), Fes(h), FGFR1(h), FGFR1(V561M)(h), FGFR2(h), FGFR2(N549H)(h), FGFR3(h), FGFR4(h), Fgr(h), Flt1(h), Flt3(D835Y)(h), Flt3(h), Flt4(h), Fms(h), Fyn(h), GCK(h), GRK5(h), GRK6(h), GRK7(h), GSK3α(h), GSK3β(h), Haspin(h), Hck(h), HIPK2(h), HIPK3(h), IGF-1R(h), IKKα(h), IKKβ(h), IR(h), IRAK1(h), IRAK4(h), IRR(h), Itk(h), KDR(h), Lck(h), LIMK1(h), LKB1(h), LOK(h), Lyn(h), Lyn(m), MAPKAP-K2(h), MAPKAP-K3(h), MEK1(h), MELK(h), Met(h), MINK(h), MKK4(m), MKK6(h), MKK7β(h), MLCK(h), MLK1(h), Mnk2(h), MRCKα(h), MRCKβ(h), MSK1(h), MSK2(h), MST1(h), MST2(h), MST3(h), MuSK(h), NEK11(h), NEK2(h), p70S6K(h), PAK2(h), PAK3(h), PAK4(h), PAK5(h), PAK6(h), PASK(h), PDGFRα(h), PDGFRα(V561D)(h), PDGFRβ(h), Pim-1(h), Pim-2(h), Pim-3(h), PKA(h), PKBα(h), PKBβ(h), PKBγ(h), PKCα(h), PKCβI(h), PKCβII(h), PKCγ(h), PKCδ(h), PKCε(h), PKCζ(h), PKCη(h), PKCθ(h), PKCι(h), PKCμ(h), PKD2(h), Plk1(h), PRAK(h), PRK2(h), PrKX(h), PTK5(h), Pyk2(h), Ret(V804L)(h), Ret(h), Ret(V804M)(h), RIPK2(h), ROCK-I(h), ROCK-II(h), ROCK-, I(r), Ron(h), Ros(h), Rse(h), Rsk1(r), SAPK3(h), SAPK4(h), SGK(h), SGK2(h), SGK3(h), SIK(h), Snk(h), Src(1-530)(h), Src(T341M)(h), SRPK1(h), SRPK2(h), STK33(h), Syk(h), TAK1(h), TAO1(h), TAO2(h), TAO3(h), Tie2(h), Tie2(R849W)(h), Tie2(Y897S)(h), TLK2(h), TrkA(h), TSSK2(h), Txk(h), ULK2(h), ULK3(h), Yes(h), ZAP-70(h), ZIPK(h) |
| Wortmannin |
| Plk3(h) |
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