Mutant Kinases

Mutant Kinases

Members of the kinase superfamily are key regulators of pivotal cell signaling pathways. Genetic alterations in protein kinases compromise their biological functions resulting in deregulated cellular pathways such as apoptosis, cell cycle regulation, proliferation, angiogenesis, differentiation, cellular metabolism. Mutations in kinase-encoding genes have been observed in many pathological conditions, ranging from cancer, inflammatory disorders, cardiovascular diseases to neurodegeneration (1). Furthermore, mutations of certain kinases have been linked to acquired drug resistance. As a result, mutant kinases quickly established themselves as important drug targets and have been the focus of drug discovery and development efforts (2).

In an effort to support the advancement of next generation of kinase-targeted therapeutic programs, SignalChem has developed and manufactured over 250 clinically relevant active kinase mutants, representing the most comprehensive list of this class of proteins in the industry.

References:
1. Kumar R et al., CancerDR: cancer drug resistance database. Sci Rep. 2013;3:1445. doi: 10.1038/srep01445.
2. Torkamani, A., Verkhivker, G., & Schork, N. J. (2009). Cancer driver mutations in protein kinase genes. Cancer Letters, 281(2), 117–127. http://doi.org/10.1016/j.canlet.2008.11.008

Home     >     Enzymes
Name Catalog Number
ABL1 (E255K), Active A03-12BG
ABL1 (E255V), Active A03-12HH
ABL1 (F317I), Active A03-12JG
ABL1 (F317L), Active A03-12IG
ABL1 (G250E), Active A03-12CG
ABL1 (H396P), Active A03-12LG
ABL1 (M351T), Active A03-12KG
ABL1 (Q252H), Active A03-12FG
ABL1 (T315I), Active A03-12DG
ABL1 (V299L), Active A03-12MG
ABL1 (Y253F), Active A03-12EG
ABL1 (Y253H), Active A03-12GH
AKT1 (E17K), Active A16-12G
AKT2 (E17K), Active A17-12G
AKT2 (R274H), Active A17-12BG
AKT3 (E17K), Active A18-12G
AKT3 (G171R), Active A18-12BG
ALK (C1156Y), Active A19-12DG
ALK (F1174L), Active A19-12EG
ALK (F1174S), Active A19-12FG
ALK (G1202R), Active A19-12HG
ALK (G1269A), Active A19-12JG
ALK (G1269S), Active A19-12KG
ALK (L1152R), Active A19-12CG
ALK (L1196M G1202R), Active A19-12NG
ALK (L1196M), Active A19-12GG
ALK (R1275Q), Active A19-12LG
ALK (S1206R), Active A19-12IG
ALK (T1151M), Active A19-12BG
ALK (T1151_L1152insT), Active A19-12G
ALK2 (G328E), Active A06-12GG
ALK2 (G328V), Active A06-12HG
ALK2 (G328W), Active A06-12IG
ALK2 (G356D), Active A06-12JG
ALK2 (PF197_198L), Active A06-12FG
ALK2 (Q207D), Active A06-13CG
ALK2 (Q207E), Active A06-13DG
ALK2 (R202I), Active A06-12EG
ALK2 (R206H), Active A06-12BG
ALK2 (R258G), Active A06-12KG
ALK3 (Q233D), Active B04-12BG
ALK3 (R486Q), Active B04-12CG
ANXA4-PKN1(Aex2Pex13), Active P70-19G
AURORA B (G160L), Active A31-10BG
AXL (R499C), Active A34-12BG
BCR-RET, Active R02-19EG
BRAF (d485-489 P490Y), Active B08-12IG
BRAF (G464V), Active B08-12JG
BRAF (G469A), Active B08-12FG
BRAF (K601E), Active B08-12BG
BRAF (L597V), Active B08-12HG
BRAF (R506_K507insVLR), Active B08-13CG
BRAF (T599_V600insT), Active B08-13BG
BRAF (V600A), Active B08-12EG
BRAF (V600D), Active B08-12CG
BRAF (V600E), Active B08-12G
BRAF (V600K), Active B08-12DG
BTK (C481F), Active B10-12FH
BTK (C481R), Active B10-12GH
BTK (C481S), Active B10-12CH
BTK (P190K), Active B10-12BH
c-KIT (A829P), Active C06-12HG
c-KIT (d557-558), Active K06-12WG
c-KIT (D816E), Active C06-12IG
c-KIT (D816F), Active C06-12JG
c-KIT (D816H), Active C06-12KG
c-KIT (D816I), Active K06-12XG
c-KIT (D816V), Active C06-12LG
c-KIT (D816Y), Active C06-12MG
c-KIT (D820E), Active K06-12BG
c-KIT (D820Y), Active K06-12CG
c-KIT (K642E), Active C06-12NG
c-KIT (L576P), Active K06-12UG
c-KIT (N822K), Active K06-12DG
c-KIT (T670E), Active K06-12EG
c-KIT (T670I), Active C06-12FG
c-KIT (V559A), Active C06-12OG
c-KIT (V559D T670I), Active K06-12QG
c-KIT (V559D V654A), Active K06-12RG
c-KIT (V559D), Active C06-12PG
c-KIT (V560G D816V), Active C06-12TG
c-KIT (V560G N822K), Active K06-12VG
c-KIT (V560G), Active C06-12SG
c-KIT (V654A), Active K06-13G
c-KIT (Y823D), Active K06-12GG
c-MER (A708S), Active M51-12BG
CK1 epsilon (R178C), Active C66-12BG
DDR1 (S496A), Active D05-12G
DDR2 (T654M), Active D06-12G
EGFR (A763_Y764insFHEA), Active E10-132BG
EGFR (A763_Y764insFQEA), Active E10-132UG
EGFR (A767-S768insTLA), Active E10-132CG
EGFR (C775S T790M L858R), Active E10-122D2G
EGFR (C797S L858R), Active E10-122ZG
EGFR (C797S), Active E10-122SG
EGFR (d746), Active E10-12IG
EGFR (d746-750 C775S T790M L858R), Active E10-122E2G
EGFR (d746-750 C797A), Active E10-122C2G
EGFR (d746-750 C797S), Active E10-122TG
EGFR (d746-750 T790M C797S L858R), Active E10-122YG
EGFR (d746-750 T790M C797S), Active E10-122UG
EGFR (d746-750 T790M L858R), Active E10-122XG
EGFR (d746-750 T790M L978I), Active E10-122WG
EGFR (d746-750 T790M), Active E10-122KG
EGFR (d746-750), Active E10-122JG
EGFR (d747-749 A750P), Active E10-12MG
EGFR (d747-749), Active E10-12LG
EGFR (d747-752 P753S), Active E10-12NG
EGFR (d752-759), Active E10-12OG
EGFR (D761Y), Active E10-12QG
EGFR (D761Y), Active E10-122QG
EGFR (D770GY), Active E10-13KG
EGFR (D770GY), Active E10-132KG
EGFR (D770_N771insGF) Protein E10-13IG
EGFR (D770_N771insNPG), Active E10-132GG
EGFR (G719C), Active E10-12FG
EGFR (G719D), Active E10-12GG
EGFR (G719S), Active E10-12HG
EGFR (H773_V774insAH) Protein E10-13PG
EGFR (H773_V774insH) Protein E10-13RG
EGFR (K716A C797S L858R), Active E10-122S2G
EGFR (K716A T790M C797S L858R), Active E10-122P2G
EGFR (K716A), Active E10-122M2G
EGFR (K716Q L718Q), Active E10-122T2G
EGFR (K728A T790M C797S L858R), Active E10-122Q2G
EGFR (K728A), Active E10-122N2G
EGFR (L718Q T790M L858R), Active E10-122H2G
EGFR (L718Q), Active E10-122G2G
EGFR (L747S), Active E10-12PG
EGFR (L747S), Active E10-122Y2G
EGFR (L792F L858R), Active E10-122U2G
EGFR (L792F), Active E10-122I2G
EGFR (L792H C797S L858R), Active E10-122V2G
EGFR (L792H), Active E10-122J2G
EGFR (L858R), Active E10-122BG
EGFR (L861Q), Active E10-12CG
EGFR (N771-P772insH), Active E10-132WG
EGFR (P772_H773insNPH), Active E10-13MG
EGFR (R999A), Active E10-122O2G
EGFR (T790M C797S L858R R999A), Active E10-122R2G
EGFR (T790M C797S L858R), Active E10-122VG
EGFR (T790M C797S), Active E10-122B2G
EGFR (T790M L792F C797S L858R), Active E10-122W2G
EGFR (T790M L792F L858R), Active E10-122K2G
EGFR (T790M L792H C797S L858R), Active E10-122X2G
EGFR (T790M L792H L858R), Active E10-122L2G
EGFR (T790M L858R), Active E10-122DG
EGFR (T790M), Active E10-122EG
EGFR (V769-D770insGE), Active E10-132VG
EGFR Mutant (C797A), Active E10-12RG
EML4-ALK (Eex13Aex20), Active A19-19G
EML4-ALK (Eex14Aex20), Active A19-19GG
EML4-ALK (Eex20Aex20), Active A19-19HG
EML4-ALK (Eex6Aex20), Active A19-19FG
ERN1 (R727A), Active E31-12BG
ERN1 (R728A), Active E31-12CG
FAM131B-BRAF (Fex2Bex9), Active B08-19EG
FGFR1 (V561M), Active F04-13G
FGFR1OP-FGFR1, Active F04-19BG
FGFR2 (C491A), Active F05-12HG
FGFR2 (C491F), Active F05-12IG
FGFR2 (C491S), Active F05-12JG
FGFR2 (E565G), Active F05-12CG
FGFR2 (K526E), Active F05-12BG
FGFR2 (K641R), Active F05-12DG
FGFR2 (K659N), Active F05-12EG
FGFR2 (N549H), Active F05-12G
FGFR2 (R612T), Active F05-12GG
FGFR2 (V564F), Active F05-12FG
FGFR3 (G697C), Active F06-12FG
FGFR3 (K650E), Active F06-12CG
FGFR3 (K650M), Active F06-12DG
FGFR3 (K650Q), Active F06-12EG
FGFR3 (V555M), Active F06-12GG
FGFR4 (N535K), Active F07-12G
FGFR4 (V550E), Active F07-12BG
FGFR4 (V550L), Active F07-12CG
FGFR4 (V550M), Active F07-12DG
FIP1L1-PDGFR alpha, Active P12-19BG
FLT3 (D835Y), Active F12-12BG
FLT3 (F594_R595insR), Active F12-12EG
FLT3 (F594_R595insREY), Active F12-12FG
FLT3 (N676K), Active F12-12IG
FLT3 (R595_E596insEY), Active F12-12GG
FLT3 (Y591-V592insVDFREYEYD), Active F12-12HG
FLT3-ITD-NPOS, Active F12-12DG
FLT3-ITD-W51, Active F12-12CG
GOPC-ROS1, Active R14-19BG
HER2 (A775_G776insYVMA), Active E27-13BG
HER2 (d755-759), Active E27-12BG
HER2 (D769H), Active E27-12GG
HER2 (D769Y), Active E27-12HG
HER2 (G776VC), Active E27-13EG
HER2 (I767M), Active E27-12NG
HER2 (L755S), Active E27-12EG
HER2 (L755W), Active E27-12FG
HER2 (P780_Y781insGSP), Active E27-13DG
HER2 (R896C), Active E27-12KG
HER2 (V777L), Active E27-12IG
HER2 (V777_G778insCG), Active E27-13CG
HER2 (V842I), Active E27-12JG
HER4 (R927Q), Active E29-12G
InsR (R1201Q), Active I08-122G
JAK1 (R724H), Active J01-12BG
KIAA1549-BRAF (Kex15Bex9), Active B08-19CG
KIAA1549-BRAF (Kex16Bex9), Active B08-19BG
KIF5B-ALK (Kex24Aex20), Active A19-19MG
KIF5B-MET (Kex24Mex14), Active M52-19BG
KIF5B-RET (Kex15Rex14), Active R02-19FG
KIF5B-RET (V804L), Active R02-19HG
KIF5B-RET (V804M), Active R02-19GG
KLC1-ALK (Kex8Aex20), Active A19-19IG
KSR1 (A635F), Active K07-12G
KSR1 (A635F), Active K07-122G
KSR1 (L639F), Active K07-12BG
KSR1 (L639F), Active K07-122BG
KSR2 (R676S), Active K08-12BG
LRRK2 (D1994A), Active L10-12FG
LRRK2 (G2019S), Active L10-12GG
LRRK2 (G2385R), Active L10-12IG
LRRK2 (I2020T), Active L10-12HG
LRRK2 (R1441C), Active L10-12G
LRRK2 (R1441G), Active L10-12BG
LRRK2 (R1441H), Active L10-12CG
LRRK2 (Y1699C), Active L10-12DG
LRRK2 (Y1699G), Active L10-12EG
MELK (T460M), Active M50-12G
MET (D1228A), Active M52-12ZG
MET (D1228G), Active M52-12B2G
MET (D1228H), Active M52-12HG
MET (D1228N), Active M52-12IG
MET (D1228V), Active M52-12C2G
MET (D1228Y), Active M52-12D2G
MET (Del Ex14), Active M52-12PG
MET (F1200I), Active M52-12GG
MET (G1163R), Active M52-12XG
MET (H1094L), Active M52-12VG
MET (H1094Y), Active M52-12WG
MET (K1244R), Active M52-12QG
MET (L1195F), Active M52-12YG
MET (L1195V), Active M52-12TG
MET (M1250I), Active M52-12SG
MET (M1250T), Active M52-12BG
MET (P991S), Active M52-12CG
MET (R970C), Active M52-12OG
MET (T1173I), Active M52-12FG
MET (T992I), Active M52-12DG
MET (V1092I), Active M52-12EG
MET (Y1230A), Active M52-12JG
MET (Y1230C), Active M52-12KG
MET (Y1230D), Active M52-12LG
MET (Y1230H), Active M52-12MG
MET (Y1230S), Active M52-12UG
MET (Y1235D), Active M52-12NG
NPM1-ALK (F1174L), Active A19-19EG
NPM1-ALK, Active A19-19BG
PDGFR alpha (D842V), Active P12-12BG
PDGFR alpha (T674I), Active P12-12CG
PKD2 (G848E), Active P76-12BG
PKD2 (G870E), Active P76-12CG
PTC1 (CCDC6-RET), Active R02-19BG
PTC2 (PRKAR1A-RET), Active R02-19CG
PTC3 (NCOA4-RET), Active R02-19DG
RET (A883F), Active R02-12MG
RET (E762Q), Active R02-12FG
RET (G691S), Active R02-12DG
RET (L790F), Active R02-12LG
RET (M918T), Active R02-12JG
RET (M918T), Active R02-12JH
RET (R749T), Active R02-12EG
RET (R813Q), Active R02-12HG
RET (R912P), Active R02-12PG
RET (S891A), Active R02-12IG
RET (S904A), Active R02-12OG
RET (S904A), Active R02-12OH
RET (S904F), Active R02-12NG
RET (S904F), Active R02-12NH
RET (V778I), Active R02-12KG
RET (V804L), Active R02-12BG
RET (V804M), Active R02-12GG
RET (Y791F), Active R02-12CG
RNF130-BRAF (Rex3Bex9), Active B08-19GG
ROS1 (G2032R), Active R14-12BG
RSK2 (I416V), Active R17-12BG
RSK2 (L608F), Active R17-12CG
RSK2 (Y483C), Active R17-12DG
SRGAP3-BRAF (Sex12Bex9), Active B08-19FG
STRN-ALK (Sex3Aex20), Active A19-19JG
TECR-PKN1(Tex1Pex10), Active P70-19BG
TFG-ALK (Tex4Aex20), Active A19-19KG
TFG-ALK (Tex5Aex20), Active A19-19CG
TFG-MET (Tex5Mex15), Active M52-19G
TFG-TRKA (TRK-T3), Active N16-19CG
TGFBR1 (T204D), Active T07-13G
TIE2 (A1124V), Active T04-12GG
TIE2 (L914F), Active T04-12IG
TIE2 (P883A), Active T04-12CG
TIE2 (R849W), Active T04-12BG
TIE2 (R915C), Active T04-12JG
TIE2 (Y1108F), Active T04-12FG
TIE2 (Y897C), Active T04-12DG
TIE2 (Y897H R915C), Active T04-12KG
TIE2 (Y897H), Active T04-12HG
TIE2 (Y897S), Active T04-12EG
TPM1-ALK, Active A19-19LG
TPM3-ALK, Active A19-19DG
TPM3-PDGFR beta, Active P13-19DG
TPM3-ROS1, Active R14-19CG
TPM3-TRKA, Active N16-19DG
TPR-TRKA (TRK-T1), Active N16-19BG
TRKA (A608D), Active N16-12DG
TRKA (F589L), Active N16-12EG
TRKA (G595R A608D), Active N16-12FG
TRKA (G595R G667A), Active N16-12JG
TRKA (G595R G667C), Active N16-12KG
TRKA (G595R G667S), Active N16-12LG
TRKA (G595R L657M), Active N16-12GG
TRKA (G595R), Active N16-12BG
TRKA (G667A), Active N16-12MG
TRKA (G667C), Active N16-12CG
TRKA (G667S), Active N16-12NG
TRKA (L657M), Active N16-12HG
TRKC (G623E), Active N18-12BH
TRKC (G623R L686M), Active N18-12EH
TRKC (G623R), Active N18-12CH
TRKC (G696A), Active N18-12FH
TRKC (G696C), Active N18-12GH
TRKC (L686M), Active N18-12DH
YES1 (T348I), Active Y01-12BG
ZAP70 (Y319F), Active Z02-12BG

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