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Protein conformation

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

4

Screening Libraries

1

Fluorescent Dye

2

Biochemical Assay Reagents

3

Peptides

1

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18669
    ML346
    5 Publications Verification

    HSP Cancer
    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27 .
    ML346
  • HY-141667

    7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole

    Fluorescent Dye Others
    MBD (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), a new fluorescent probe for protein and nucleoprotein conformation, is applied to bacterial ribosomes and to bovine trypsinogen and trypsin. MBD is strongly fluorescent upon binding to a hydrophobic area of a macromolecule .
    MBD
  • HY-18563

    HCV Infection
    4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
    4-Phenoxybenzylamine
  • HY-138865

    Prion Protein Infection
    BiCAPPA is the first bivalent antiprion ligand. BiCAPPA can decrease infectious conformational form of prion protein (PrP Sc) from scrapie-infected cells, with an EC50 of 0.32 μM .
    BiCAPPA
  • HY-139984

    Btk Neurological Disease Inflammation/Immunology
    BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis .
    BIIB091
  • HY-130149
    Adagrasib
    35+ Cited Publications

    MRTX849

    Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
    Adagrasib
  • HY-P10829

    Dengue Virus Infection
    MLH40 is a peptide inhibitor with activity against Dengue virus (DENV) infection, which is found in the conserved ectodomain region of DENV membrane protein. MLH40 inhibits DENV through its N-terminal loop interaction with DENV envelope protein and altering the dimer conformation .
    MLH40
  • HY-P10534

    Prion Protein Infection Neurological Disease
    CCβ is a simple 17-amino acid peptide designed in research. CCβ is able to mimic the conformational transition of proteins from α-helix to β-sheet, which is a key step in the aggregation of proteins associated with many diseases, such as Alzheimer's disease and prion disease. CCβ can be used to study diseases related to protein aggregation .
    ccβ
  • HY-160550

    Phosphatase Inflammation/Immunology
    DPM-1003 is a PTP1B conformational inhibitor that targets the non-catalytic, disordered segment at the C-terminus of the PTP1B protein, showing improvement in lung inflammation in mice .
    DPM-1003
  • HY-162505

    CCR CXCR Inflammation/Immunology Cancer
    SQA1, a squaramide (SQA) derivative, is a CCR6 antagonist with a Kd of 250 nM. SQA1 is also a CXCR2 inhibitor. The intracellular pocket occupied by SQA1 overlaps with the G protein binding site and stabilizes the closed conformation of the intracellular pocket .
    SQA1
  • HY-D0896

    ANSA; 8-Anilino-1-naphthalenesulfonic acid

    Bacterial Infection
    ANS (8-Anilino-1-naphthalenesulfonic acid) is a competitive inhibitor targeting thyroxine binding globulin (TBG) (Ki=2.09×10 6 M -1). ANS is used in radioimmunoassay by displacing bound triiodothyronine (T3) to improve detection sensitivity. ANS can block the protein binding site of T3 and release free T3 for antibody recognition. As a fluorescent probe, ANS can specifically bind to the hydrophobic region of proteins (such as membrane proteins) and monitor the dynamics of protein conformation through changes in fluorescent signals. It is widely used in biochemical research and antibacterial material development .
    ANS
  • HY-16926
    CK-666
    5+ Cited Publications

    Arp2/3 Complex HIV Infection Cancer
    CK-666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC50=12 μM). CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation .
    CK-666
  • HY-152468

    Apoptosis Cancer
    Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
    Antitumor agent-83
  • HY-15463
    Imatinib
    Maximum Cited Publications
    99 Publications Verification

    STI571; CGP-57148B

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib
  • HY-15463S2

    STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride

    Autophagy Bcr-Abl c-Kit SARS-CoV PDGFR Cancer
    Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-d3 hydrochloride
  • HY-131275

    Drug Metabolite Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib Impurity E
  • HY-15463R

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib (Standard)
  • HY-106964A

    5-HT Receptor Neurological Disease
    (Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia .
    (Rac)-S 16924
  • HY-15463S3

    STI571-13C,d3; CGP-57148B-13C,d3

    Isotope-Labeled Compounds Autophagy SARS-CoV Bcr-Abl PDGFR c-Kit Cancer
    Imatinib- 13C,d3 (STI571- 13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib-13C,d3
  • HY-12534
    Wiskostatin
    1 Publications Verification

    Arp2/3 Complex Neurological Disease
    Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC50 value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC50 value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line .
    Wiskostatin
  • HY-158107

    Ras Cancer
    BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .
    BBO-8520
  • HY-161577

    Bcl-2 Family Cancer
    BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells .
    BFC1103
  • HY-Y1754

    TOAC

    Biochemical Assay Reagents
    2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid (TOAC) is a compound with the ability to probe conformational changes, folding processes and interactions of peptides and proteins. 2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid is often used in relevant biological research to gain a deeper understanding of the behavior and function of biomacromolecules. 2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid plays an important role in analyzing the interactions and dynamic responses of biological systems.
    2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid
  • HY-W017113

    Endogenous Metabolite Aryl Hydrocarbon Receptor Metabolic Disease
    2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
    2-Mercaptobenzothiazole

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