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TargetMol | Tags Cell Cycle/Checkpoint
TargetMol | Tags Metabolism

Serine/threonin kinase

Serine threonine kinase belongs to protein kinase, which can phosphorylate the OH group of serine or threonine residues. Serine threonine kinases contain Rho kinase, Aurora kinase, AMP kinase, RAF kinase, Polo like kinase, PIM kinase, ATM kinase and other kinases. The cAMP/cGMP, Ca2+/calmodulin and diacylglycerol and multiple chenmical signals can regulate the activity of serine threonine kinases.

  • Wortmannin
    T628319545-26-7
    Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.
    • $32
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    TargetMol | Citations Cited
  • HTH-01-091
    T241522000209-42-5In house
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.
    • $296
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  • Piceatannol
    T061010083-24-6
    Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.
    • $39
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    TargetMol | Citations Cited
  • Upamostat
    T13257590368-25-5
    Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.
    • $97
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  • HA-1004
    T2752591742-10-8In house
    HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.
    • $195
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  • LP-935509
    T157811454555-29-3
    LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).
    • $33
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  • (+)-Isocorydine hydrochloride
    T429113552-72-2
    (+)-Isocorydine hydrochloride (Isocorydine HCl) is a eukaryote protein kinases Inhibitor.
    • $37
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  • SPHINX31
    T51941818389-84-2
    SPHINX31 is a potent inhibitor of serine arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).
    • $34
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  • Fasudil hydrochloride
    T3060105628-07-7
    Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
    • $35
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    TargetMol | Citations Cited
  • Camostat mesylate
    T239159721-29-8
    Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.
    • $43
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    TargetMol | Citations Cited
  • Pinostrobin
    TN2082480-37-5
    Pinostrobin, a potent flavonoid inducer, exerts a neuroprotective effect against Aα²(25-35)-induced neurotoxicity in PC12 cells, at least in part, via inhibiting oxidative damage and calcium overload, as well as suppressing the mitochondrial pathway of ce
    • $81
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  • CRT0066101 dihydrochloride
    TQ01041883545-60-5
    CRT0066101 dihydrochloride is an effective and selective PKD inhibitor (IC50s: 1, 2.5 and 2 nM for PKD1, 2, and 3).
    • $31
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  • Benzamidine hydrochloride
    T83621670-14-0
    Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).
    • $40
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  • SBC-115076
    T2626489415-96-5
    SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.
    • $34
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  • Fasudil
    T1606103745-39-7
    Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
    • $33
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  • Nafamostat mesylate
    T239282956-11-4
    Nafamostat mesylate (FUT-175), a synthetic serine protease inhibitor, has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.
    • $39
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    TargetMol | Citations Cited
  • N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine
    T92561071135-06-2
    N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor[1].
    • $148
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  • WNK463
    T70172012607-27-9
    WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4).
    • $72
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  • CID755673
    T2458521937-07-5
    CID755673 is an effective and specific cell-active inhibitor for PKD (IC50: 182 nM); exhibits selective PKD1 inhibition when compared with PLK1, AKT, CAMKIIα, CAK, and PKC isoforms.
    • $35
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  • ML-7 hydrochloride
    T3050110448-33-4
    ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.
    • $30
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    TargetMol | Citations Cited
  • R-IMPP
    T40582133832-83-2
    R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.
    • $32
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  • 1-NM-PP1
    T2153221244-14-0
    1-NM-PP1 (PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
    • $43
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  • SM1-71
    T366802088179-99-9
    SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1 2 3 4 6 7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A B, MAPK1 3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.
    • $44
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  • SBC-115337
    T9276423148-46-3
    SBC-115337 is a PCSK9 inhibitor.
    • $53
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  • SRPIN340
    T1954218156-96-8
    SRPIN340 (SRPK inhibitor), a serine/arginine-rich protein kinase (SRPK)-specific inhibitor, is potent for SRPK1 (IC50 = 0.89 uM).
    • $39
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  • Chymotrypsin
    T735949004-07-3
    Chymotrypsin (Chymotrypsin A) is a serine protease synthesized by the pancreas, which cleaves protein chains on the carboxyl side of aromatic amino acids.
    • $29
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  • WNK-IN-11
    T54562123489-30-3
    WNK-IN-11 (Allosteric WNK Kinase Inhibitor) is an allosteric With-No-Lysine (WNK) kinase inhibitor,WNK1(IC50 : 4 nM)
    • $84
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  • Cetraxate hydrochloride
    T1976327724-96-5
    Cetraxate hydrochloride (DV10062) is an oral gastrointestinal medication. It has a cytoprotective effect.
    • $40
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  • GAK inhibitor 49
    T8535319492-82-5
    GAK inhibitor 49 is a highly selective and ATP-competitive cyclin G associated kinase (GAK) inhibitor (IC50: 56 nM; Ki: 0.54 nM ).
    • $87
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  • SBC-110736
    T45241629166-02-4
    SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).
    • $30
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  • FOY 251
    T867671079-09-9
    FOY 251 is a proteinase inhibitor, and is an anti-proteolytic active metabolite camostate.
    • $49
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  • MLCK inhibitor peptide 18 acetate
    TP1890L1
    MLCK inhibitor peptide 18 acetate is a selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.
    • $47
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    TargetMol | Citations Cited
  • kb NB 142-70
    T20621233533-04-4
    kb NB 142-70 is a selective protein kinase D (PKD) inhibitor with IC50 values of 28.3 nM, 58.7 nM, and 53.2 nM for PKD1, PKD2, and PKD3 respectively.
    • $40
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  • SGC-GAK-1
    T51692226517-76-4
    SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).
    • $43
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  • CID 2011756
    T1863638156-11-3
    CID 2011756 is an ATP-competitive and specific PKD1 inhibitor.
    • $39
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  • BioE-1115
    T105471268863-35-9
    BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).
    • $30
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  • 6-(Dimethylamino)purine
    T7444938-55-6
    6-(Dimethylamino)purine (N,N-Dimethyladenine) is a serine threonine protein kinase and CDK inhibitor
    • $29
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  • CRT0066101 dihydrochloride(956121-30-5 free base)
    T8957L2308510-39-4
    CRT0066101 dihydrochloride is an inhibitor of PKD.
    • $30
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  • BMT-124110 Formate
    T10572L In house
    BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.
    • $195
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  • MS-444
    T16145150045-18-4In house
    MS-444 (BE-34776) is a smooth muscle myosin light chain kinase (MLCK) and HuR inhibitor with antitumor activity for triple-negative breast and colorectal cancer.
    • $624
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  • CID-797718
    T1858370586-05-3
    CID-797718 is a protein kinase D1 (PKD1) inhibitor.
    • $98
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  • kb-NB77-78
    T18081350622-33-1
    kb-NB77-78 is an analog of CID797718, which is a by-product of the synthesis of the parental compound, CID755673(PKD1 inhibitor).
    • $29
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  • SRPKIN-1
    T169312089226-94-6
    SRPKIN-1 is a covalent and irreversible inhibitor of SRPK1 2 (IC50s: 35.6 and 98 nM, respectively).
    • $1,170
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  • IPR-803
    T11666892243-35-5
    IPR-803 is an effective inhibitor of the uPAR·uPA protein-protein interaction (PPI) with anti-tumor activity. IPR-803 binds directly to uPAR with a Ki of 0.2 μM.
    • $84
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  • PCSK9-IN-10
    T72025368434-98-4
    PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.
    • $41
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  • TAO Kinase inhibitor 2
    T77501850467-77-5
    TAO Kinase inhibitor 2 is a TAO kinase inhibitor with an IC50 of 50-500 nM. TAO Kinase inhibitor 2 inhibits KIAA1361 and JIK with IC50s of 50-500 nM.
    • $30
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  • PKD-IN-1
    T8957956121-30-5
    PKD-IN-1 is an inhibitor of PKD.
    • $119
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