激酶(Kinase)作为关键酶家族成员,通过将ATP或GTP的γ-磷酸转运到底物特定的氨基酸残基上使底物磷酸化(图1-2)。
图1 功能蛋白激酶的通用催化结构域示意图(Lahiry P, et al, Nat Rev Genet, 2010)
图2 激酶参与蛋白质磷酸化过程(Ardito F, et al, Int J Mol Med. 2017)
蛋白激酶涉及多种细胞信号转导途径,参与细胞凋亡、细胞周期调节、血管生成、细胞代谢等通路,在肿瘤免疫、炎症、心血管疾病等领域发挥了重要作用。目前,FDA批准的小分子激酶抑制剂(Small-Molecule Kinase Inhibitors,SMKI)已超过80种,作用于21个激酶家族靶点,约占激酶组的20%。激酶突变与获得性耐药性有关,突变型激酶(Mutant Kinase)已成为药物发现和开发的重点,“靶向”突变驱动的耐药性已成为未满足的临床需求。因此,对激酶及其突变体的深入研究、基于激酶靶点的小分子抑制剂的筛选与改造已成为癌症治疗的基石之一。
劲帆生物医药科技(武汉)有限公司,致力于为全球学术界、制药公司和生物技术企业的科学家提供临床前一站式激酶靶点开发及药物筛选研究服务。劲帆生物拥有全球领先的One-Bac 4.0规模化蛋白制备专利技术平台,工艺开发及cGMP级蛋白生产平台。团队现已开发出超50种高生物活性激酶及相关蛋白突变体,也可提供定制化激酶表达、生化活性筛选及体内/外药效评价一站式服务。围绕这一关键酶家族开展科学探索,推动药物发现、疾病治疗,守护人类健康福祉。
货号 |
激酶 |
靶点家族 |
结构 |
标签及位置 |
种属 |
表达系统 |
最低购买量 |
KN2 |
AKT1 |
AKT |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN51 |
AKT3 |
AKT |
Catalytic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN43 |
MER(MERTK) |
Axl |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN16 |
PIM1 |
CAMK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN17 |
PIM2 |
CAMK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN7 |
RAF1 |
CAMKL |
Catalytic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN3 |
CDK2 |
CDK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN8 |
CLK3 |
CMGC |
Full-length |
N-6His |
human |
sf9 |
5ug |
KN9 |
MAPKAPK3 |
CMGC |
Full-length |
N-6His |
human |
sf9 |
5ug |
KN10 |
MAPKAPK5 |
CMGC |
Full-length |
N-6His |
human |
sf9 |
5ug |
KN11 |
CLK2 |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN12 |
CDK7 |
CMGC |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN13 |
DYRK1B |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN14 |
CLK1 |
CMGC |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN15 |
CDK8 |
CMGC |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN22 |
CDK4 |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN23 |
CDK6 |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN24 |
CDK6tb |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN49 |
CLK4 |
CMGC |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN27 |
PIK3CB |
Lipid kinase |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN31 |
PIK3CG |
Lipid kinase |
Full-length |
N-6His |
human |
sf9 |
5ug |
KN18 |
PLK1 |
Other |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN19 |
PLK3 |
Other |
Catalytic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN20 |
TTK |
Other |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN21 |
PLK2 |
Other |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN44 |
PDGFRB |
PDGFR |
Cytoplasmic domain |
N-6HIS-GST |
human |
sf9 |
5ug |
KN40 |
BRK(PTK6) |
Src |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN41 |
LYNa |
Src |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN42 |
LYNb |
Src |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN1 |
MAP2K2 |
STE |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN4 |
MAP2K6 |
STE |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN5 |
MAP2K3 |
STE |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN6 |
MAP2K5 |
STE |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN50 |
MAP4K2 |
STE |
Full-length |
N-6HIS-GST |
human |
sf9 |
5ug |
KN25 |
DDR1 |
TK |
Cytoplasmic domain |
N-6HIS-GST |
human |
sf9 |
5ug |
KN26 |
SRC |
TK |
full length |
N-GST-6His |
human |
sf9 |
5ug |
KN28 |
FGFR1 |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN29 |
AXL |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN30 |
SYK |
TK |
full length |
N-GST-6His |
human |
sf9 |
5ug |
KN34 |
BTK |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN35 |
BTK T316A |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN36 |
BTK M437R |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN37 |
BTK T474I |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN38 |
BTK T474S |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN39 |
BTK C481S |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN47 |
YES1(YES) |
TK |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
KN48 |
RET |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN78 |
EGFR |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN60 |
FGFR3 |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN66 |
ALK |
TK |
Cytoplasmic domain |
N-GST-6His |
human |
sf9 |
5ug |
KN32 |
ACVR2B |
TKL |
Cytoplasmic domain |
N-6HIS-GST |
human |
sf9 |
5ug |
KN33 |
ACVRL1 |
TKL |
Truncated |
N-6HIS-GST |
human |
sf9 |
5ug |
KN45 |
BMPR2 |
TKL |
Cytoplasmic domain |
N-6HIS-GST |
human |
sf9 |
5ug |
KN46 |
IRAK4 |
TKL |
Full-length |
N-GST-6His |
human |
sf9 |
5ug |
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