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 (42):

By Effects:	Inhibitors (30) Degrader (1) Substrate (1) Ligand (1) Activators (2) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-138489

TRULI	Inhibitor	99.98%
TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues.

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.

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.

HY-103020

BAY-1816032	Inhibitor	99.73%
BAY-1816032, a chemical probe, is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC₅₀ of 7 nM.

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).

HY-181281

VU6080195	Activator
VU6080195 is a blood-brain barrier-permeable pan-TAOK activator. VU6080195 shows the highest potency against TAOK1 (EC₅₀ = 270 nM), followed by TAOK3 (EC₅₀ = 503 nM) and TAOK2 (EC₅₀ = 1,376 nM). VU6080195 can be used for the research of diseases such as neurodevelopmental disorders, tauopathies and breast cancer.

HY-E70950

Calmodulin-dependent Protein Kinase II, Rat
Calmodulin-dependent protein kinase II, Rat, is a serine-threonine protein kinase involved in neurotransmitter release, stimulation-induced gene expression control, and microtubule-associated protein phosphorylation.

HY-178974

STK10-IN-1	Inhibitor
SLK/STK10-IN-2 (Compound 23) is a highly selective STK10 inhibitor, with a K_d of 365 nM and an IC₅₀ of 0.85 μM. SLK/STK10-IN-2 exhibits EC₅₀ of 0.89 μM in NanoBRET cell experiments. SLK/STK10-IN-2 shows no significant binding to SLK, STK3/4. SLK/STK10-IN-2 can be used to study STK10-related diseases (such as abnormal lymphocyte migration).

HY-147165

VT02956	Inhibitor	99.58%
VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-108333

SB-633825	Inhibitor	98.05%
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC₅₀s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.

HY-115677

ILK-IN-3	Inhibitor	99.62%
ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model.

HY-104001

BAY-524	Inhibitor	98.36%
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.

HY-115719

NR162	Inhibitor	99.7%
NR162 is a selective CASK (Ca²⁺/calmodulin-dependent Ser/Thr kinase) inhibitor with an IC₅₀ of 80 nM and a Kd of 22 nM. NR162 shows about 50-fold selectivity for CASK than TYRO3. NR162 targets the unique GFG motif of CASK and has excellent shape complementarity to the CASK ATP binding pocket. NR162 can be used for the research of neurological diseases.

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.)

HY-N8146

Bruceantinol		98.89%
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC₅₀ = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells.

HY-171658

R1-ICR-5	Degrader	98.73%
R1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation.

HY-W013852

PKC-IN-6	Inhibitor	99.93%
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-145725A

Baliforsen	Inhibitor	98.12%
Baliforsen (ISIS 5987690) is an antisense oligonucleotide (ASO) that inhibits DMPK mRNA. Baliforsen binds within exon 9 of the human DMPK transcript to promote RNase H1-mediated degradation Baliforsen can be used for the research of myotonic dystrophy type 1.

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.

HY-172241

Tapencarium	Inhibitor	98.11%
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.

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