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].

References:

[1]. Kino T. GR-regulating Serine/Threonine Kinases: New Physiologic and Pathologic Implications. Trends Endocrinol Metab. 2018 Apr;29(4):260-270. [Content Brief]

[2]. Protein Serine-Threonine Kinase - an overview.

[3]. Serine/Threonine-Specific Protein Kinase - an overview.

Ser/Thr Kinase Related Products (38):

By Effects:	Ligand (1) Inhibitors (27) Substrates (2) Degraders (2) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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.

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.

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.

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.

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.

HY-175733

CQ3196	Inhibitor
CQ3196 is an orally active RIOK2 inhibitor with a K_d of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC₅₀ value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research.

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.

HY-156792

RIOK2-IN-1	Inhibitor
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.

HY-178214

CSBP ligand 1	Ligand
CSBP ligand 1 (Compound 36) is a ligand of CSBP, with an IC₅₀ of 0.08 μM for CSBP binding. CSBP ligand 1 can inhibit the production of TNF in mice treated with LPS (HY-D1056). CSBP ligand 1 has no significant inhibitory activity against PGHS-1 (IC₅₀: 16 μM) and 5-LO (IC₅₀: 60 μM). CSBP ligand 1 can be used in the research of inflammation-related diseases.

HY-E70788

BARK1 Recombinant Human Active Protein Kinase
BARK1 Recombinant Human Active Protein Kinase is a membrane LRR-RLK (leucine-rich repeat receptor-like kinase) protein that specifically binds to BAK1 and its homologs.

HY-171294

Protein kinase inhibitor 16	Inhibitor
Protein kinase inhibitor 16 exhibits inhibitory activity against a variety of Ser/Thr kinase or receptor or non-receptor tyrosine kinase.

HY-171276

Anti-neuroinflammation agent 3	Inhibitor
Anti-neuroinflammation agent 3 (Compound A.10.3) exhibits inhibitory activity against a variety of Ser/Thr kinase or receptor or non-receptor tyrosine kinase.

HY-171291

Protein kinase inhibitor 14	Inhibitor
Protein kinase inhibitor 14 (Compound 13) exhibits inhibitory effects against a variety of serine/threonine kinase and receptor/non-receptor tyrosine kinase.

HY-169587

Protein kinase G inhibitor-3	Inhibitor
Protein kinase G inhibitor-3 (Compound 177) is an inhibitor of mycobacterial serine/threonine protein kinases. Protein kinase G inhibitor-3 can be used in the research of diseases related to mycobacterial infections.

HY-171293

Protein kinase inhibitor 15	Inhibitor
Protein kinase inhibitor 15 (Compound A.35.3) exhibits inhibitory activity against a variety of Ser/Thr kinase or receptor or non-receptor tyrosine kinase.

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.

HY-122735

Inh2-B1	Inhibitor
Inh2-B1 is a Ser/Thr protein kinase (STK1) inhibitor. Inh2-B1 specifically inhibits STK1 activity by directly binding to its ATP-binding catalytic domain. Inh2-B1 down-regulates cell wall hydrolase genes and disrupts the biofilm formation of Methicillin-resistant Staphylococcus aureus (MRSA) clearly.

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