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 Related Products (9):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103020
    BAY-1816032
    		Inhibitor 99.05%
    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-161111
    KVS0001
    		Inhibitor 99.14%
    KVS0001 is a potent inhibitor of SMG1 and nonsense mediated decay (NMD) that has anti-tumor activity.
    KVS0001
  • 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-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-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-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-10424A
    Milciclib maleate
    		Inhibitor
    Milciclib (PHA-848125) maleate is a cyclin-dependent kinase inhibitor that impairs melanoma cell growth and modulates gene expression involved in cell cycle regulation. Milciclib maleate has been shown to significantly affect the expression of various genes, including down-regulating PTTG1, contributing to its antiproliferative activity. Milciclib maleate enhances sensitivity to treatment in p53 mutated melanoma cells when combined with PTTG1 silencing.
    Milciclib maleate
  • 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-156465
    RIOK2-IN-2
    		Inhibitor
    RIOK2-IN-2 (8) is a RIOK2 inhibitor, with IC50 values of 3.02 μM and 5.34 μM in MKN-1 and MOLT4 cells, respectively.
    RIOK2-IN-2