General Information of the Protein
Protein ID
PT01150
Protein Name
Serine/threonine-protein kinase 3
Secondarily
Protein Name
Mammalian STE20-like protein kinase 2
STE20-like kinase MST2
Serine/threonine-protein kinase Krs-1
Gene Name
STK3
Secondarily
Gene Name
KRS1
MST2
Sequence
MEQPPAPKSKLKKLSEDSLTKQPEEVFDVLEKLGEGSYGSVFKAIHKESGQVVAIKQVPVESDLQEIIKEISIMQQCDSPYVVKYYGSYFKNTDLWIVMEYCGAGSVSDIIRLRNKTLIEDEIATILKSTLKGLEYLHFMRKIHRDIKAGNILLNTEGHAKLADFGVAGQLTDTMAKRNTVIGTPFWMAPEVIQEIGYNCVADIWSLGITSIEMAEGKPPYADIHPMRAIFMIPTNPPPTFRKPELWSDDFTDFVKKCLVKNPEQRATATQLLQHPFIKNAKPVSILRDLITEAMEIKAKRHEEQQRELEEEEENSDEDELDSHTMVKTSVESVGTMRATSTMSEGAQTMIEHNSTMLESDLGTMVINSEDEEEEDGTMKRNATSPQVQRPSFMDYFDKQDFKNKSHENCNQNMHEPFPMSKNVFPDNWKVPQDGDFDFLKNLSLEELQMRLKALDPMMEREIEELRQRYTAKRQPILDAMDAKKRRQQNF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE20 family
>
STE protein kinase MST subfamily
Function
Stress-activated, pro-apoptotic kinase which, following caspase-cleavage, enters the nucleus and induces chromatin condensation followed by internucleosomal DNA fragmentation. Key component of the Hippo signaling pathway which plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ (PubMed:23972470). Phosphorylation of YAP1 by LATS2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. STK3/MST2 and STK4/MST1 are required to repress proliferation of mature hepatocytes, to prevent activation of facultative adult liver stem cells (oval cells), and to inhibit tumor formation. Phosphorylates NKX2-1 (By similarity). Phosphorylates NEK2 and plays a role in centrosome disjunction by regulating the localization of NEK2 to centrosome, and its ability to phosphorylate CROCC and CEP250 (PubMed:21723128). In conjunction with SAV1, activates the transcriptional activity of ESR1 through the modulation of its phosphorylation. Positively regulates RAF1 activation via suppression of the inhibitory phosphorylation of RAF1 on 'Ser-259'. Phosphorylates MOBKL1A and RASSF2. Phosphorylates MOBKL1B on 'Thr-74'. Acts cooperatively with MOBKL1B to activate STK38.
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Uniprot ID
Primary ID:
Q13188

Secondarily ID:
A8K722
B3KYA7
Q15445
Q15801
Q96FM6
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Ensembl ID
ENSG00000104375
HGNC ID
HGNC:11406
Subcellular Location
Cytoplasm
Nucleus
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0534855
N-[1-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]piperidin-4-yl]acetamide
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C19H20ClN5O
 1
1
IC50 = 139 nM
   TI
   LI
   LO
   TS
CP0088382
3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H15N5O
 1
1
IC50 = 197 nM
   TI
   LI
   LO
   TS
CP0090031
4-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
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C16H15ClN4O
 1
1
IC50 = 235 nM
   TI
   LI
   LO
   TS
CP0951028
3-((5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)(methyl)amino)-2-methylpropan-1-ol
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C17H19ClN4O
 1
1
IC50 = 289 nM
   TI
   LI
   LO
   TS
CP0331115
US9156845, 215
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C17H17N5O2
 1
1
IC50 = 303 nM
   TI
   LI
   LO
   TS
CP0283532
US9156845, 91
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C16H15FN4O
 1
1
IC50 = 373 nM
   TI
   LI
   LO
   TS
CP0488662
4-[3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]morpholine
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C17H16ClN3O
 1
1
IC50 = 373 nM
   TI
   LI
   LO
   TS
CP0571168
1-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-N-methylpiperidin-4-amine
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C18H20ClN5
 1
1
IC50 = 417 nM
   TI
   LI
   LO
   TS
CP0357337
1-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]piperidin-4-ol
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C17H17ClN4O
 1
1
IC50 = 433 nM
   TI
   LI
   LO
   TS
CP0097255
US9156845, 107
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C17H18N4O
 1
1
IC50 = 434 nM
   TI
   LI
   LO
   TS
CP0546027
2-[[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-methylamino]ethanol
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C15H15ClN4O
 1
1
IC50 = 631 nM
   TI
   LI
   LO
   TS
CP0534854
3-[[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]propan-1-ol
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C15H15ClN4O
 1
1
IC50 = 668 nM
   TI
   LI
   LO
   TS
CP0546007
5-(3-chlorophenyl)-4-piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine
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C17H17ClN4
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0464211
4-[(2,9-dimethyl-8-oxo-6-thia-2,9,12,14-tetrazatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-13-yl)amino]benzenesulfonamide
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C17H16N6O3S2
 1
1
IC50 = 1510 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0464211
4-[(2,9-dimethyl-8-oxo-6-thia-2,9,12,14-tetrazatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-13-yl)amino]benzenesulfonamide
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C17H16N6O3S2
 2
1 IC50 = 18.2 nM
2 Kd = 11 nM
CP0088382
3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H15N5O
 1
1 IC50 = 22 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01768 Serine/threonine-protein kinase 4 Homo sapiens, Human