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Results for "

serine phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (1) SRPK (1) Amino Acid Derivatives (1) Apoptosis (4) c-Met/HGFR (1) Casein Kinase (1) CDK (4) Dipeptidyl Peptidase (1) Fluorescent Dye (1) HSP (3) Isotope-Labeled Compounds (1) JAK (1) LIM Kinase (LIMK) (2) MAP4K (1) MAPKAPK2 (MK2) (2) MNK (2) p38 MAPK (1) PD-1/PD-L1 (2) Phosphatase (1) PPAR (1) Tau Protein (1) VEGFR (1) Wnt (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

MCE Kits

Isotope-Labeled Compounds

Targets Recommended: Oxidative Phosphorylation Serine Racemase (SR) Microtubule‐associated serine/threonine kinase (MAST) SRPK SHMT Ser/Thr Protease DYRK STK33 ASCT Ser/Thr Kinase Serpin MASTL TMPRSS6 Enteropeptidase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12834

MK2-IN-1 5 Publications Verification	MAPKAPK2 (MK2) HSP	Cancer
MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 0.11 uM for MK2 and an EC₅₀ of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein .

HY-12834A

MK2-IN-1 hydrochloride 5 Publications Verification	MAPKAPK2 (MK2) HSP	Cancer
MK2-IN-1 hydrochloride (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 0.11 uM for MK2 and an EC₅₀ of 0.35 uM for pHSP27. MK2-IN-1 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein .

HY-P5455

S3 Fragment	LIM Kinase (LIMK)	Others
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)

HY-136276

DMNB-caged-Serine	Amino Acid Derivatives	Others
DMNB-caged-Serine is a photocaged amino acid. DMNB-caged-Serine can be used as a catalytic residue, hydrogen bonding partner or site of post-translational modification. DMNB-caged-Serine can be used for the control of protein phosphorylation .

HY-153244

MFH290 1 Publications Verification	CDK	Cancer
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .

HY-136433

N,N'-Dinitrosopiperazine 1,4-Dinitrosopiperazine; DNP	Others	Cancer
N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568 .

HY-145232

PhosTAC7 3 Publications Verification	Phosphatase Tau Protein	Neurological Disease Cancer
PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tau protein-related neurodegenerative diseases (Alzheimer's disease) .

HY-N9725

16-Hydroxycleroda-3,13-dien-15,16-olide 16ξ-Hydroxycleroda-3,13-dien-15,16-olide	Dipeptidyl Peptidase	Metabolic Disease
16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy .

HY-E70691

CLK1 Recombinant Human Active Protein Kinase	CDK	Cancer
CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .

HY-136433S

N,N'-Dinitrosopiperazine-d8 1,4-Dinitrosopiperazine-d₈; DNP-d₈	Isotope-Labeled Compounds	Cancer
N,N'-Dinitrosopiperazine-d₈ is the deuterium labeled N,N'-Dinitrosopiperazine . N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568 .

HY-117661

SPHINX31 Maximum Cited Publications 11 Publications Verification	SRPK VEGFR	Cardiovascular Disease Cancer
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC₅₀ of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A₁₆₅a isoform. SPHINX31 can be used to research neovascular eye disease .

HY-168209

LBM22	Wnt CDK Apoptosis	Cancer
LBM22 is a CDC2-like kinase 2 (CLK2) inhibitor with the IC₅₀ of 3.9 nM. LBM22 has antiproliferative activity and inhibits serine/arginine-rich (SR) protein phosphorylation. LBM22 down-regulates the expression of Wnt-related proteins and anti-apoptotic proteins and can be used for study of non-small cell lung cancer .

HY-50683

JNJ-38877605 5 Publications Verification	c-Met/HGFR	Metabolic Disease Cancer
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC₅₀ of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .

HY-118034

MTBT 1 Publications Verification	p38 MAPK Apoptosis	Cancer
MTBT is an anticancer agent and p38 MAPK activator. MTBT can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. The specific inhibitor of p38 MAPK, Adezmapimod (HY-10256), can abrogate the cell cycle arrest induced by MTBT .

HY-E70841

LIMK2 Recombinant Human Active Protein Kinase	LIM Kinase (LIMK)	Cancer
LIM kinase 2 (LIMK2) is a serine/threonine and tyrosine kinases. LIMK2 plays a crucial role in the regulation of cytoskeleton dynamics by controlling actin filaments and microtubule turnover, especially through the phosphorylation of cofilin, an actin depolymerising factor. LIMK2 Recombinant Human Active Protein Kinase is a recombinant LIMK2 protein that can be used to study LIMK2-related functions .

HY-E70830

HIPK2 Recombinant Human Active Protein Kinase	DYRK	Cancer
Homeodomain interacting protein kinase 2 (HIPK2) is an evolutionary conserved serine/threonine kinase that regulates gene expression by phosphorylation of transcription factors and accessory components of the transcription machinery. HIPK2 is activated in response to DNA-damaging agents or morphogenic signals. HIPK2 Recombinant Human Active Protein Kinase is a recombinant HIPK2 protein that can be used to study HIPK2-related functions .

HY-100022A

Tomivosertib hydrochloride eFT508 hydrochloride	MNK PD-1/PD-L1	Cancer
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC₅₀s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC₅₀=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .

HY-100022

Tomivosertib Maximum Cited Publications 11 Publications Verification eFT508	MNK PD-1/PD-L1	Cancer
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC₅₀s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC₅₀=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .

HY-144088

ZYF0033 2 Publications Verification HPK1-IN-22	MAP4K	Inflammation/Immunology Cancer
ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a ⁺CD8 ⁺ T cells, but not T cells, PD-1 ⁺CD8 ⁺ T cells, TIM-3 ⁺CD8 ⁺ Infiltration of T cells and LAG3 ⁺CD8 ⁺ T cells was reduced .

HY-171786

CDK12-IN-8	CDK	Cancer
CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer .

HY-13775

XL019 5+ Cited Publications	JAK Apoptosis	Cancer
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .

HY-174347

Hsp90-Cdc37-IN-4	HSP Casein Kinase Apoptosis	Cancer
Hsp90-Cdc37-IN-4, a Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity .

HY-126969

C333H	PPAR	Metabolic Disease
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .

HY-D2946

CLIP-TMR BC-TMR	Fluorescent Dye	Infection
CLIP-TMR is a TMR-labeled CLIP tag fluorescent probe. CLIP-TMR combines the high specificity recognition ability of the CLIP-tag and the excellent optical performance of the TMR fluorophore, and can be used for the specific labeling and visualization of the HCV NS5A protein .

Cat. No.	Product Name

HY-L081

Phosphatase Inhibitor Library	161 compounds
Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc. Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action. MCE supplies a unique collection of 161 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.

Phosphatase Inhibitor Library

161 compounds

Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc.

Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action.

MCE supplies a unique collection of 161 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.

HY-L024

Histone Modification Research Compound Library	823 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 823 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Histone Modification Research Compound Library

823 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 823 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

HY-L018

TGF-beta/Smad Compound Library	357 compounds
The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc. MCE designs a unique collection of 357 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

TGF-beta/Smad Compound Library

357 compounds

The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.

MCE designs a unique collection of 357 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

CLIP-TMR BC-TMR	Fluorescent Dye
CLIP-TMR is a TMR-labeled CLIP tag fluorescent probe. CLIP-TMR combines the high specificity recognition ability of the CLIP-tag and the excellent optical performance of the TMR fluorophore, and can be used for the specific labeling and visualization of the HCV NS5A protein .

Cat. No.	Product Name	Target	Research Area

HY-P5455

S3 Fragment	LIM Kinase (LIMK)	Others
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)

HY-P5429

DNA-PK Substrate	Peptides	Others
DNA-PK Substrate is a biological active peptide. (A substrate for DNA-dependent protein kinase (DNA-PK), phosphorylation. DNA-PK is essential for the repair of DNA double-strand breaks. This peptide corresponding to 11–24 amino acids of human p53 with threonine 18 and serine 20 changed to alanine is used as a substrate for the assay of DNA-PK activityPyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)

Cat. No.	Product Name

HY-K0021

Phosphatase Inhibitor Cocktail I (100× in DMSO) 590+ Cited Publications
Phosphatase Inhibitor Cocktail I (100× in DMSO) is a blend of 2 phosphatase inhibitors that can effectively inhibit alkaline phosphatases and serine/threonine phosphatases. It is used to maintain the phosphorylation status of proteins.

HY-K0023

Phosphatase Inhibitor Cocktail Ⅲ (100× in DMSO) 235+ Cited Publications
Phosphatase Inhibitor Cocktail Ⅲ (100× in DMSO) is a blend of 3 phosphatase inhibitors that can effectively inhibit serine/threonine phosphatases and alkaline phosphatases. It is used to maintain the phosphorylation status of proteins.

Cat. No.	Product Name	Chemical Structure

HY-136433S

N,N'-Dinitrosopiperazine-d8
N,N'-Dinitrosopiperazine-d₈ is the deuterium labeled N,N'-Dinitrosopiperazine . N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568 .

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