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Results for "

active conformation

" in MedChemExpress (MCE) Product Catalog:

26

Inhibitors & Agonists

1

Biochemical Assay Reagents

3

Peptides

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18343A
    CP-31398 dihydrochloride

    		MDM-2/p53 Cancer
    CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53 .
    CP-31398 dihydrochloride
  • HY-123054
    BTSA1
    1 Publications Verification

    		 Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis .
    BTSA1
  • HY-139984
    BIIB091

    		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-109176
    Giredestrant
    5 Publications Verification

    GDC-9545; RG6171

    		 Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
    Giredestrant
  • HY-113655
    AD-5075

    		PPAR Metabolic Disease
    AD-5075 is an orally active insulin sensitizer. AD-5075 mediates its antidiabetic activity by binding to PPARγ and thereby generating an active conformation of the receptor .
    AD-5075
  • HY-163947
    UG-480

    		VD/VDR Cancer
    UG-480 is a gemini analog that effectively stabilizes the active VDR conformation. UG-480 has antiproliferative effects in estrogen receptor-positive MCF-7 breast adenocarcinoma cells. UG-480 can be used in cancer research .
    UG-480
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate; RG6171 tartrate

    		 Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
    Giredestrant tartrate
  • HY-135864
    KRAS inhibitor-6

    		Ras Cancer
    KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .
    KRAS inhibitor-6
  • HY-135866
    KRAS inhibitor-8

    		Ras Cancer
    KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C .
    KRAS inhibitor-8
  • HY-135865
    KRAS inhibitor-7

    		Ras Cancer
    KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .
    KRAS inhibitor-7
  • HY-150097
    Recombinant Human Serum Albumin(rHSA)

    		Biochemical Assay Reagents Others
    Recombinant Human Serum Albumin (rHSA) is an active compound and possesses an identical conformation to plasma derived HSA. Recombinant Human Serum Albumin (rHSA) has no difference between rHSA and plasma derived HSA. The main physiological function of Recombinant Human Serum Albumin (rHSA) is to regulate plasma pH and maintain plasma osmotic pressure .
    Recombinant Human Serum Albumin(rHSA)
  • HY-157887
    ADT-007

    		Ras Cancer
    ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
    ADT-007
  • HY-116182
    RO5487624

    		Influenza Virus Infection
    RO5487624, an analogue of RO5464466 (HY-120690), is an orally active hemagglutinin (HA) inhibitor of influenza H1N1 viruses that abolishes influenza virus fusion by blocking HA conformational changes in low pH environments. RO5487624 displays a protective effect on mice that are lethally challenged with influenza H1N1 virus .
    RO5487624
  • HY-13299
    MK-8033
    2 Publications Verification

    		 c-Met/HGFR Cancer
    MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
    MK-8033
  • HY-13299A
    MK-8033 hydrochloride
    2 Publications Verification

    		 c-Met/HGFR Cancer
    MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
    MK-8033 hydrochloride
  • HY-101561
    Avapritinib
    Maximum Cited Publications
    6 Publications Verification

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • HY-P99155
    Zalutumumab

    		EGFR Cancer
    Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .
    Zalutumumab
  • HY-110112
    BTT-3033

    		Integrin Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease .
    BTT-3033
  • HY-101561R
    Avapritinib (Standard)

    		c-Kit PDGFR Cancer
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib (Standard)
  • HY-144998
    NVP-DKY709

    		IKZF Family Molecular Glues Inflammation/Immunology Cancer
    NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
    NVP-DKY709
  • HY-P1928
    Humanin

    		Bcl-2 Family Neurological Disease Endocrinology
    Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging .
    Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG .
    Humanin
  • HY-18343
    CP-31398

    		MDM-2/p53 Apoptosis Cancer
    CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
    CP-31398
  • HY-156078
    α-Glucosidase-IN-32

    		Glycosidase Metabolic Disease
    α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
    α-Glucosidase-IN-32
  • HY-110088
    SCH529074
    1 Publications Verification

    		 MDM-2/p53 Cancer
    SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
    SCH529074
  • HY-112306
    Ripretinib

    DCC-2618

    		 c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
    Ripretinib
  • HY-116716
    PIN1 inhibitor API-1

    		MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
    PIN1 inhibitor API-1

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