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intracellular domain

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

11

Peptides

1

Inhibitory Antibodies

1

Natural
Products

1

Recombinant Proteins

8

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50845
    Avagacestat
    2 Publications Verification

    BMS-708163

    		 γ-secretase Notch Cancer
    Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
    Avagacestat
  • HY-B1201
    Tiratricol
    1 Publications Verification

    3,3',5-Triiodothyroacetic acid

    		 Flavivirus Thyroid Hormone Receptor TNF Receptor Endocrinology
    Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication. .
    Tiratricol
  • HY-P10152
    INF7

    		Biochemical Assay Reagents Infection
    INF7 is a derivative of the N-terminal domain of the HA2 protein and is sensitive to pH. INF7 disrupts the stability of endosomal membranes through a mechanism independent of membrane fusion. INF7 can be used to enhance the endosome escape of complex or liposome-encapsulated proteins. Co-encapsulation of INF7 and molecular imaging probes in liposomes can enhance intracellular signaling and probe retention .
    INF7
  • HY-103693
    NAZ2329
    3 Publications Verification

    		 Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
    NAZ2329
  • HY-P4076
    MPG peptides, Pβ

    		HIV DNA Alkylator/Crosslinker Infection
    MPG peptides, Pβ is an amphipathic cell-penetrating peptide. MPG peptides, Pβ consists of three components: the hydrophobic fusion sequence (GALFLGFLGAAGSTMGA) of HIV glycoprotein 41, a spacer domain (WSQP), and the nuclear localization signal (KKKRKV) of the large T antigen of Simian virus 40. MPG peptides, Pβ can form stable non-covalent complexes with nucleic acids (including DNA) through electrostatic interactions and improve their intracellular delivery. MPG peptides, Pβ can be used in studies of HIV-1-related immune responses .
    MPG peptides, Pβ
  • HY-132182
    HPA-12
    1 Publications Verification

    		 Ceramidase Autophagy Apoptosis ATF6 Neurological Disease Cancer
    HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
    HPA-12
  • HY-P1985
    Notch 1

    		Notch Cardiovascular Disease Cancer
    Notch 1 (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types .
    Notch 1
  • HY-N2452
    Cochinchinenin C

    		GLP Receptor Cardiovascular Disease Infection Metabolic Disease
    Cochinchinenin C is a GLP-1R agonist that binds to the extracellular domain of the receptor via hydrophobic interactions and hydrogen bonds, and promotes glucose-dependent insulin secretion from pancreatic β-cells. Cochinchinenin C also increases intracellular cAMP and ATP levels. At low concentrations, Cochinchinenin C binds to human serum albumin, alters its microenvironment, and induces dominant static fluorescence quenching. Cochinchinenin C shows almost no cytotoxicity to pancreatic β-cells, and exerts a synergistic effect with Loureirin A (HY-N1505) when binding to human serum albumin. Cochinchinenin C has been widely used in studies of type 2 diabetes, Helicobacter pylori infection, thrombotic diseases, and other conditions .
    Cochinchinenin C
  • HY-P10471A
    MPSD TFA

    MARCKS-ED TFA

    		 MARCKS PKC Others
    MPSD TFA (MARCKS-ED TFA) is the TFA salt form of MPSD (HY-P10471). MPSD TFA is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS). MPSD TFA can sense membrane curvature and recognize phosphatidylserine. MPSD TFA can be utilized as biological probe to study membrane shape and lipid composition .
    MPSD TFA
  • HY-P10471E
    MPSD control peptide TFA

    MARCKS-ED control peptide TFA

    		 MARCKS Others
    MPSD control peptide (MARCKS-ED control peptide) TFA is the control peptide of MPSD (HY-P10471). MPSD (MARCKS-ED) is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS) .
    MPSD control peptide TFA
  • HY-P11071
    PCSK9 Inhibitor, EGF-A

    		PCSK9 Cardiovascular Disease
    PCSK9 Inhibitor, EGF-A is a PCSK9 inhibitor. PCSK9 Inhibitor, EGF-A is residues 293-334 of the EGF-A domain of the low-density lipoprotein (LDL) receptor. PCSK9 Inhibitor, EGF-A can prevent PCSK9-induced intracellular LDLR degradation. PCSK9 Inhibitor, EGF-A can be used in the study of hypercholesterolemia and premature atherosclerosis .
    PCSK9 Inhibitor, EGF-A
  • HY-P1985A
    Notch 1 TFA

    		Notch Cardiovascular Disease Cancer
    Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types .
    Notch 1 TFA
  • HY-E70873
    Tyk2(JH1/JH2) Recombinant Human Active Protein Kinase

    		JAK Cancer
    TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). Tyk2(JH1/JH2) Recombinant Human Active Protein Kinase is a recombinant Tyk2(JH1/JH2) protein that can be used to study Tyk2(JH1/JH2)-related functions .
    Tyk2(JH1/JH2) Recombinant Human Active Protein Kinase
  • HY-E70869
    TRKA(NTRK1) Recombinant Human Active Protein Kinase

    		Trk Receptor Neurological Disease
    TRKA (also named NTRK1) is a potential new member of the tyrosine kinase gene family. TRKA is a receptor tyrosine kinase that is phosphorylated in response to NGF. A single transmembrane domain divides TRKA into an extracellular domain, important for NGF binding, and an intracellular tyrosine kinase domain, important for signal transduction. TRKA(NTRK1) Recombinant Human Active Protein Kinase is a recombinant TRKA(NTRK1) protein that can be used to study TRKA(NTRK1)-related functions .
    TRKA(NTRK1) Recombinant Human Active Protein Kinase
  • HY-162094
    CMX410

    		Acyltransferase Bacterial Infection
    CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis .
    CMX410
  • HY-113646
    Shield-2

    		FKBP Others
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
    Shield-2
  • HY-P10471
    MPSD

    MARCKS-ED

    		 MARCKS PKC Others
    MPSD (MARCKS-ED) is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS). MPSD can sense membrane curvature and recognize phosphatidylserine. MPSD can be utilized as biological probe to study membrane shape and lipid composition .
    MPSD
  • HY-P10319
    RI-STAD-2

    		PKA Cardiovascular Disease Cancer
    RI-STAD-2 is a high-affinity interfering peptide that regulates the subunit RI of protein kinase A (PKA). RI-STAD-2 interferes with the binding of AKAPs and PKA-RI by simulating the interaction between AKAPs' α-helix domain and PKA-RI's dimerization/anchoration (D/D) domain, thereby affecting PKA activity and intracellular localization. RI-STAD-2 can be used to study the role of AKAPs interaction with PKA-RI in pathological processes such as cardiovascular disease and cancer .
    RI-STAD-2
  • HY-P10471D
    MPSD control peptide

    MARCKS-ED control peptide

    		 MARCKS PKC Others
    MPSD control peptide (MARCKS-ED control peptide) is a control peptide for MPSD peptide (HY-P10471). MPSD (MARCKS-ED) is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS). MPSD can sense membrane curvature and recognize phosphatidylserine. MPSD can be utilized as biological probe to study membrane shape and lipid composition .
    MPSD control peptide
  • HY-159808
    TCL1

    		Proteasome Cancer
    TCL1 is a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit in the 19S regulatory particle (19S RP) of the proteasome with an IC50 value of approximately 26 μM. TCL1 interferes with the recognition and transport of ubiquitinated proteins by Rpn-13, inhibits the degradation of proteins by the proteasome, and thus affects the balance of intracellular protein metabolism. TCL1 is promising for research of hematological malignancies .
    TCL1
  • HY-B1201R
    Tiratricol (Standard)

    3,3',5-Triiodothyroacetic acid (Standard)

    		 Flavivirus Thyroid Hormone Receptor Reference Standards TNF Receptor Endocrinology
    Tiratricol (Standard) is the analytical standard of Tiratricol. This product is intended for research and analytical applications. Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication. .
    Tiratricol (Standard)
  • HY-E70872
    TYK2(JH1) Recombinant Human Active Protein Kinase

    		JAK Cancer
    TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). TYK2(JH1) Recombinant Human Active Protein Kinase is a recombinant TYK2(JH1) protein that can be used to study TYK2(JH1)-related functions .
    TYK2(JH1) Recombinant Human Active Protein Kinase
  • HY-E70874
    TYK2(JH2) Recombinant Human Active Protein Kinase

    		JAK Cancer
    TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). TYK2(JH2) Recombinant Human Active Protein Kinase is a recombinant TYK2(JH2) protein that can be used to study TYK2(JH2)-related functions .
    TYK2(JH2) Recombinant Human Active Protein Kinase
  • HY-E70717
    FGFR1 V561M Recombinant Human Active Protein Kinase

    		FGFR Cancer
    FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions .
    FGFR1 V561M Recombinant Human Active Protein Kinase
  • HY-50845R
    Avagacestat (Standard)

    BMS-708163 (Standard)

    		 γ-secretase Notch Reference Standards Cancer
    Avagacestat (Standard) is the analytical standard of Avagacestat. This product is intended for research and analytical applications. Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
    Avagacestat (Standard)
  • HY-P992094
    Capromab

    		PSMA Cancer
    Capromab is an anti-human PSMA-targeting monoclonal antibody. Capromab binds specifically to the intracellular domain of PSMA, does not undergo internalization after binding, and targets necrotic cells with disrupted membranes. Capromab can be used for the research of prostate cancer .
    Capromab
  • HY-182464
    DABMA

    		Potassium Channel Infection Others
    DABMA is a TMEM175 channel activator with a human EC50 of 17.9 μM. DABMA directly increases TMEM175 channel current via interaction with intracellular, transmembrane, or endosomal lumen-associated domains, and does not alter TMEM175 mRNA or protein levels. DABMA delays endolysosomal substrate degradation, modulates endolysosomal trafficking, increases acidic organelle accumulation, induces cholesterol accumulation and altered late endosome morphology. DABMA can be used for the research of coronavirus disease, Clostridium difficile infection, Pseudomonas aeruginosa infection, rabies, and influenza virus infection .
    DABMA
  • HY-124253
    SMDC818909

    		p97 Cancer
    SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms .
    SMDC818909
  • HY-181560
    SLD1121

    		Wnt β-catenin Metabolic Disease
    SLD1121 is an agonist of the Wnt/β-catenin signaling pathway that enhances Wnt signaling by targeting LRP6 (Kd: 4.52-7.49 nM). SLD1121 interacts with the intracellular domain of LRP6, stabilizes LRP6, promotes its nuclear translocation, and facilitates its binding to β-catenin, TCF4 or LEF1 in the nucleus, thereby inducing the expression of Wnt-regulated genes and stem cell-related genes. SLD1121 induces the transition of hair follicles from telogen to anagen in the mouse hair growth cycle and promotes hair growth in mice. SLD1121 is applicable to hair loss-related research .
    SLD1121
  • HY-183683
    DQ-9

    		Proteasome Apoptosis Cancer
    DQ-9 is a selective immunoproteasome β5i inhibitor (IC50=0.0019 μM). DQ-9 generates additional inhibitory substances via iron-mediated intracellular activation, and induces oxidative stress, carbon-centered free radicals and macromolecular damage through its artemisinin domain. DQ-9 induces apoptosis in leukemia and multiple myeloma cells. DQ-9 exhibits selective cytotoxicity against leukemia and multiple myeloma cells by elevating the labile iron pool. DQ-9 can be used in the research of hematological malignancies (leukemia, multiple myeloma, mantle cell lymphoma, acute myeloid leukemia) .
    DQ-9
  • HY-175824
    PSD-95/nNOS PPI-IN-1

    		iGluR NO Synthase Apoptosis Reactive Oxygen Species (ROS) Neurological Disease
    PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
    PSD-95/nNOS PPI-IN-1
  • HY-103693R
    NAZ2329 (Standard)

    		Reference Standards Phosphatase Cancer
    NAZ2329 (Standard) is the analytical standard of NAZ2329 (HY-103693). This product is intended for research and analytical applications. NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
    NAZ2329 (Standard)

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