2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Ser/Thr Kinase

Ser/Thr Kinase

Protein Serine-Threonine Kinase

Ser/Thr Kinase belongs to the eukaryotic protein kinase (ePK) superfamily and can use ATP to phosphorylate the hydroxyl group of serine or threonine residues in the kinase recognition amino acid sequence. The widely known anticancer targets in the Ser/Thr Kinase family are protein kinase C (PKC) and cyclin-dependent kinases (CDKs). There are two types of Ser/Thr Kinase: one is a kinase that phosphorylates receptor molecules, i.e., receptor protein serine/threonine kinases, such as activated receptor kinases and transforming growth factor β receptor kinases; the other is a kinase that acts as an intracellular signal transduction protein. The latter can phosphorylate several key targets of multiple signaling pathways and affect a variety of biological functions including growth, differentiation, cell cycle progression, and metabolism. This family contains several different groups of kinases, including (1) the CK group of kinases: casein kinases; (2) the AGC group: the kinases protein kinase A (PKA), protein kinase B (PKB or v-akt murine thymoma viral oncogene homolog 1: AKT1), and protein kinase C (PKC); (3) the CAMK group of kinases: Ca2+/calmodulin-dependent kinases; (4) the CMGC group of kinases: mos/raf kinases, mitogen-activated kinases (MAPKs), cyclin-dependent kinases (CDKs), and glycogen synthase kinases (GSKs); and (5) the STE group of kinases: homologs of yeast sterile kinases 7, 11, and 20 kinases.Ser/Thr Kinase family regulates the glucocorticoid receptor (GR), a nuclear hormone receptor superfamily protein. For example, MAPK, CDK, PKB/AKT1 and GSK3β can phosphorylate GR at specific residues; PKA, AKT1, PKC, MAPK, AMPK and mTOR can additionally phosphorylate other kinases and/or transcriptional cofactors associated with DNA-associated GR to indirectly regulate GR. It is worth mentioning that p38 MAPK in the MAPK family regulates serine phosphorylation of GR through upstream MAP2K2/4, while another JNK inhibits GR transcriptional activity by enhancing the nuclear export of the receptor[1][2].

Ser/Thr Kinase Isoform Specific Products:

Ser/Thr Kinase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161111
    KVS0001
    		Inhibitor 99.14%
    KVS0001 is a selective SMG1 inhibitor. KVS0001 elevates the expression of transcripts and proteins resulting from truncating mutations. KVS0001 increased the presentation of immune-targetable HLA class I-associated peptides from nonsense-mediated decay (NMD)-downregulated proteins on the surface of cancer cells. KVS0001 exerts anti-tumor properties and can be studied in research for NMD-related diseases, including cancer and inherited diseases.
    KVS0001
  • HY-132868
    SLK/STK10-IN-1
    		Inhibitor 99.78%
    SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.
    SLK/STK10-IN-1
  • HY-103020
    BAY-1816032
    		Inhibitor 99.73%
    BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM.
    BAY-1816032
  • HY-P990043
    Iluzanebart
    		Activator 98.63%
    Iluzanebart is a human monoclonal IgG1 antibody and is the agonist antibody for human TREM2 (hTREM2). Iluzanebart improves the survival and function of microglia by activating the TREM2 signaling pathway to compensate for the loss of CSF1R function. Iluzanebart can be used for research of adult-onset leukoencephalopathy associated with CSF1R (colony stimulating factor 1 receptor) (CSF1R-ALSP).
    Iluzanebart
  • HY-104001
    BAY-524
    		Inhibitor 99.48%
    BAY-524 is a potent Bub1 kinase inhibitor. BAY-524 inhibits the recombinant catalytic domain of human Bub1 with an IC50 of 450 nM. BAY-524 can be used for the research of anti-cancer in combination with other agents.
    BAY-524
  • HY-W013852
    PKC-IN-6
    		Inhibitor 99.63%
    PKC-IN-6 (Compound 21) is a selective inhibitor of tyrosine and serine kinases. PKC-IN-6 shows inhibitory activity against PKC-α, PKC-δ, PKA, EGF-R with IC50 values of 240, >500, >500, >100 μM, respectively. PKC-IN-6 is promising for research of cancers.
    PKC-IN-6
  • HY-173186
    TLK1-IN-1
    		Inhibitor
    TLK1-IN-1 (Compound 5n) is a TLK1 inhibitor with an IC50 of 7.2 μM against TLK1B and a GI50 of 2.7 μM in LNCaP cells. TLK1-IN-1 induces DNA damage and apoptosis in cancer cells, making it a potential candidate for prostate cancer research.
    TLK1-IN-1
  • HY-170574
    CQ627
    		Degrader
    CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model.
    CQ627
  • HY-147655
    CQ211
    		Inhibitor 99.58%
    CQ211 is a potent and selective RIOK2 inhibitor with a Kd of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines.
    CQ211
  • HY-112158
    NSC139021
    		Inhibitor 99.86%
    NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling.
    NSC139021
  • HY-162426
    UNC-CA2-103
    		Inhibitor 99.26%
    UNC-CA2-103 (compound 128) is a potent inhibitor of Tousled like kinase 2 (TLK2), with the IC50 of 18 nM.
    UNC-CA2-103
  • HY-145725A
    Baliforsen
    		Inhibitor
    Baliforsen is an antisense oligonucleotide (16 nucleotides) designed to target myotonic dystrophy protein kinase (DMPK) mRNA and research myotonic dystrophy.
    Baliforsen
  • HY-116559
    TIBI
    		Inhibitor 99.62%
    TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC50: 0.09 μM, Ki: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1.
    TIBI
  • HY-115719
    CASK-IN-1
    		Inhibitor 99.7%
    CASK-IN-1 is a highly potent and selective CASK inhibitor with a Kd value of 0.022 μM.
    CASK-IN-1
  • HY-P3935
    Arg-Gly-Tyr-Ser-Leu-Gly
    		99.44%
    Arg-Gly-Tyr-Ser-Leu-Gly is corresponding to the sequence of residues from 21 through 26 in lysozyme. Arg-Gly-Tyr-Ser-Leu-Gly can be used as a substrate for the protein kinase, and phosphorylated at serine residue by protein kinase.
    Arg-Gly-Tyr-Ser-Leu-Gly
  • HY-P99121
    Anti-Mouse CD11b Antibody (M1/70)
    Anti-Mouse CD11b Antibody is an anti-mouse CD11b IgG2b antibody inhibitor derived from the host Rat.
    Anti-Mouse CD11b Antibody (M1/70)
  • HY-12240
    B32B3
    		Inhibitor
    B32B3 is an inhibitor of VprBP with an IC50 value of 0.5 μM at the H2AT120p cell. B32B3 can suppress tumor growth.
    B32B3
  • HY-P5435
    LKBtide
    		Substrate
    LKBtide is a biological active peptide. (This is a peptide substrate that is phosphorylated by Serine/Threonine kinase 11 (STK11), also known as LKB1. LKBtide is derived from sucrose non-fermenting 1 (SNF1) protein kinase, which is normally activated by the LKB1/AMP-activated protein kinase (AMPK) signaling pathway.)
    LKBtide
  • HY-172241
    Tapencarium
    		Inhibitor
    Tapencarium (RZL-012) is a serine/threonine kinase inhibitor. Tapencarium can reduce subcutaneous fat volume. Tapencarium is promising for research of fat-related disorders such as Dercum’s disease and aesthetic applications.
    Tapencarium
  • HY-P10943
    APO-15
    		Substrate
    APO-15 is a fluorogenic imaging agent targeting phosphatidylserine (PS) exposed on the cell membrane of apoptotic cells. APO-15 can selectively bind to apoptotic cells, enabling staining and imaging of apoptotic cells in a calcium-independent and wash-free manner. APO-15 is promising for research of inflammatory diseases and cancers.
    APO-15
Ser/Thr Kinase Isoform Comparison

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