Search Result

Results for "

phosphorylation Site

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (1) Oxidative Phosphorylation (1) Akt (1) Apoptosis (3) ATM/ATR (1) CaMK (1) Casein Kinase (1) Checkpoint Kinase (Chk) (1) EGFR (1) FAK (2) FLAP (1) Histone Methyltransferase (1) HIV (1) iGluR (1) LIM Kinase (LIMK) (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) PI3K (1) PKA (3) PKC (2) Src (1) STAT (2) Survivin (1) Tie (1) Toll-like Receptor (TLR) (1) TRP Channel (1)
By Research Areas:	Cancer (13) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Targets Recommended: Oxidative Phosphorylation DYRK BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12289A

Defactinib hydrochloride Maximum Cited Publications 38 Publications Verification VS-6063 hydrochloride; PF 04554878 hydrochloride	FAK	Cancer
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

HY-136276

DMNB-caged-Serine	Others	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-B0789

SU6656 10+ Cited Publications	Src FAK Akt	Cancer
SU6656 is a Src family kinases inhibitor with IC₅₀s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.

HY-149007

STAT3-IN-11 1 Publications Verification	STAT Apoptosis	Cancer
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers .

HY-114302

CCB02 1 Publications Verification	Microtubule/Tubulin	Cancer
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC₅₀ of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .

HY-P3745

*H1-7 (histone H1 phosphorylation* site), PKA Substrate**	PKA	Others
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate .

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-P3812

Woodtide	DYRK	Neurological Disease
Woodtide is a substrate for the DYRK (DYRK) family of kinases whose sequence is based on that around the DYRK phosphorylation site in FKHR .

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-149292

SR-4133	Casein Kinase	Cancer
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC₅₀ of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .

HY-P1597

Malantide 1 Publications Verification	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

HY-164523

PV1162	Checkpoint Kinase (Chk)	Cancer
PV1162 is a selective Chk2 inhibitor with an IC₅₀ of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .

HY-135741

NYX-2925	iGluR	Neurological Disease
NYX-2925 is an orally active NMDAR modulator. NYX-2925 restores levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the mPFC. NYX-2925 shows no effect on CAMKII, and any addictive or sedative/ataxic side effects. NYX-2925 can be used for research of a variety of NMDA receptor-mediated central nervous system disorders .

HY-P5525

AC3-I, myristoylated Autocamtide-3 Derived Inhibitory Peptide	CaMK	Others
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)

HY-P10465

TRPV1-Tat	TRP Channel	Inflammation/Immunology
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .

HY-151379

EM127	Histone Methyltransferase	Cancer
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (K_D=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .

HY-101562

Inavolisib 3 Publications Verification GDC-0077; RG6114	PI3K Apoptosis	Cancer
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC₅₀=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .

HY-110282

S3QEL-2	Oxidative Phosphorylation Mitochondrial Metabolism	Metabolic Disease
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC₅₀=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation .

HY-160708

Tie2 kinase inhibitor 3	Tie	Cancer
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC₅₀=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .

HY-169797

STAT3-IN-38	STAT Survivin Apoptosis	Cancer
STAT3-IN-38 (Compound 4m) is an inhibitor of STAT3 (K_D of rhSTAT3: 45.33 µM). STAT3-IN-38 binds to the SH2 domain of STAT3 protein and suppresses the STAT3’s phosphorylation at site pTyr705 as well as its downstream genes (Survivin and Mcl-1). STAT3-IN-38 could block cell-cycle and induce Apoptosis in colorectal cancer cells .

HY-123834

FEN1-IN-1 5 Publications Verification	FLAP ATM/ATR	Cancer
FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg ²⁺ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .

HY-P5395

TAT-GluR23A Fusion Peptide	HIV	Others
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)

HY-D1056B3

Lipopolysaccharides, from Klebsiella pneumoniae LPS, from bacterial (Klebsiella pneumoniae)	Toll-like Receptor (TLR)	Inflammation/Immunology
Lipopolysaccharides, from Klebsiella, are lipopolysaccharide endotoxins. Lipopolysaccharides, from Klebsiella pneumoniae, consist of three parts: lipid A, core oligosaccharide, and O-specific antigen or O-side chain. In smooth LPS, the core region is divided into two areas: the inner core near the lipid A and the outer core that provides attachment sites for the O-antigen. In the lipopolysaccharide of Klebsiella pneumoniae, the l,d-HeppII at the O-3 position can be replaced by an α-d-galacturonic acid residue (α-d-GalpA). In most studied Enterobacteriaceae, the core LPS contains inner core phosphorylation modifications, but the core LPS of Klebsiella pneumoniae lacks this modification. The unique core structure plays an important role in the outer membrane permeability and pathogenesis of Klebsiella pneumoniae .

Cat. No.	Product Name

HY-L165

Dopamine Receptor Compound Library	211 compounds
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life. MCE designs a unique collection of 211 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Dopamine Receptor Compound Library

211 compounds

Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life.

MCE designs a unique collection of 211 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Cat. No.	Product Name	Type

HY-D1056B3

Lipopolysaccharides, from Klebsiella pneumoniae LPS, from bacterial (Klebsiella pneumoniae)	Carbohydrates
Lipopolysaccharides, from Klebsiella, are lipopolysaccharide endotoxins. Lipopolysaccharides, from Klebsiella pneumoniae, consist of three parts: lipid A, core oligosaccharide, and O-specific antigen or O-side chain. In smooth LPS, the core region is divided into two areas: the inner core near the lipid A and the outer core that provides attachment sites for the O-antigen. In the lipopolysaccharide of Klebsiella pneumoniae, the l,d-HeppII at the O-3 position can be replaced by an α-d-galacturonic acid residue (α-d-GalpA). In most studied Enterobacteriaceae, the core LPS contains inner core phosphorylation modifications, but the core LPS of Klebsiella pneumoniae lacks this modification. The unique core structure plays an important role in the outer membrane permeability and pathogenesis of Klebsiella pneumoniae .

Lipopolysaccharides, from Klebsiella pneumoniae

LPS, from bacterial (Klebsiella pneumoniae)

Carbohydrates

Lipopolysaccharides, from Klebsiella, are lipopolysaccharide endotoxins. Lipopolysaccharides, from Klebsiella pneumoniae, consist of three parts: lipid A, core oligosaccharide, and O-specific antigen or O-side chain. In smooth LPS, the core region is divided into two areas: the inner core near the lipid A and the outer core that provides attachment sites for the O-antigen. In the lipopolysaccharide of Klebsiella pneumoniae, the l,d-HeppII at the O-3 position can be replaced by an α-d-galacturonic acid residue (α-d-GalpA). In most studied Enterobacteriaceae, the core LPS contains inner core phosphorylation modifications, but the core LPS of Klebsiella pneumoniae lacks this modification. The unique core structure plays an important role in the outer membrane permeability and pathogenesis of Klebsiella pneumoniae .

Cat. No.	Product Name	Target	Research Area

HY-P1597

Malantide 1 Publications Verification	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

HY-P3745

*H1-7 (histone H1 phosphorylation* site), PKA Substrate**	PKA	Others
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate .

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-P3812

Woodtide	DYRK	Neurological Disease
Woodtide is a substrate for the DYRK (DYRK) family of kinases whose sequence is based on that around the DYRK phosphorylation site in FKHR .

HY-P5466

S6(229-239)	Peptides	Others
S6(229-239) is a biological active peptide. (This is a synthetic peptide substrate for S6 kinase shown to be phosphorylated by protein kinase c with phosphorylation site identified at Ser235)

HY-P5434

Jak3tide JAK3 Peptide substrate	Peptides	Others
Jak3tide (JAK3 Peptide substrate) is a biological active peptide. (This peptide is a substrate for Jak3. It may be used used in kinase assays. Jak3tide contains the phosphorylation site at Tyr7.)

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-P5513

Aquaporin-2 (254-267), pSER261, human	Peptides	Others
Aquaporin-2 (254-267), pSER261, human is a biological active peptide. (This peptide is a fragment of the human aquaporin-2 (AQP2) phosphorylated at Ser261. Protein phosphorylation plays a key role in vasopressin signaling in renal-collecting duct. Phosphorylation at several AQP2 residues including Ser256 and Ser261, is altered in response to vasopressin. It is possible that both sites are involved in vasopressin-dependent AQP2 trafficking.)

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

HY-P5525

AC3-I, myristoylated Autocamtide-3 Derived Inhibitory Peptide	CaMK	Others
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)

HY-P10465

TRPV1-Tat	TRP Channel	Inflammation/Immunology
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .

HY-P5395

TAT-GluR23A Fusion Peptide	HIV	Others
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: