KinaseProfiler Reference Inhibitors
As part of our ongoing enhancements to provide you the most relevant, comprehensive data to advance your research, Millipore has established reference inhibitor quality control limits for over 95% of the protein kinases on our KinaseProfiler panel, at both KMand 10 µM ATP concentration. Effective March 2008, every KinaseProfiler report now includes Reference Inhibitor data providing IC50 values generated from 8-point curves using validated reference inhibitors for every kinase assayed in your project. If reference values generated fall outside our established limits, assays against that particular kinase are repeated.
As the leaders in functional enzyme profiling, Millipore’s Gold Standard KinaseProfiler and IC50 Profiler services are undergoing constant improvement. The introduction of stringent upper and lower limits for small molecule inhibitor IC50 values against the kinases used in your project is your assurance that your data meet the strictest quality control standards in the industry.
The reference inhibitors used in KinaseProfiler are listed below, grouped with the appropriate protein kinases. For a small minority of protein kinases, appropriate reference inhibitor IC50 limits are still being established.
Figure 1. Example Reference Inhibitor report
| 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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