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Results for "

conformational shift

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

1

Fluorescent Dye

2

Biochemical Assay Reagents

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159520
    Ofirnoflastum

    Ofirnoflast; HT-6184

    		 NEKs NOD-like Receptor (NLR) Caspase Apoptosis Pyroptosis NF-κB Cardiovascular Disease Inflammation/Immunology Cancer
    Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
    Ofirnoflastum
  • HY-117389
    Homocarbonyltopsentin

    PK4C9

    		 DNA/RNA Synthesis Others
    Homocarbonyltopsentin (PK4C9) is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing with EC50 value of 16 μM .
    Homocarbonyltopsentin
  • HY-112273
    CD532
    1 Publications Verification

    		 Aurora Kinase Cancer
    CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
    CD532
  • HY-160406
    SNX281

    		STING IFNAR Interleukin Related Inflammation/Immunology Cancer
    SNX281 is a selective STING agonist, with IC50 values of 4.1, 4.5, 10.7, and 3.7 μM against human, mouse, rat, and monkey STING, respectively. SNX281 undergoes homodimerization at the STING binding site, triggering a conformational shift of STING from an inactive open state to an active closed state, thereby driving downstream STING-dependent signaling pathways. SNX281 induces type I interferons, IFN-β, TNF-α, IL-6, cytokine release, T cell responses, and long-lasting immune memory. SNX281 exhibits anti-tumor activity and is applicable to research related to colorectal cancer, melanoma, advanced solid tumors, lymphoma, and ovarian cancer .
    SNX281
  • HY-112273A
    CD532 hydrochloride
    1 Publications Verification

    		 Aurora Kinase Cancer
    CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
    CD532 hydrochloride
  • HY-134136
    Octanoyl Coenzyme A

    		Endogenous Metabolite Others
    Octanoyl coenzyme A is an enoyl-CoA hydratase binder. Octanoyl coenzyme A binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
    Octanoyl Coenzyme A
  • HY-134136B
    Octanoyl coenzyme A triammonium

    S-Octanoate-CoA triammonium; S-​Octanoate-coenzyme A triammonium

    		 Biochemical Assay Reagents Others
    Octanoyl coenzyme A triammonium is an enoyl-CoA hydratase binder. Octanoyl coenzyme A triammonium binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
    Octanoyl coenzyme A triammonium
  • HY-168636
    p53 Activator 13

    		DNA Methyltransferase MDM-2/p53 Cancer
    p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNA damage response via p53 activation. p53 Activator 13 can be utilized in cancer research .
    p53 Activator 13
  • HY-181128
    QO-83

    		Potassium Channel Neurological Disease
    QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies .
    QO-83
  • HY-179506
    p53 Activator 16

    		MDM-2/p53 Apoptosis Cancer
    P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers .
    p53 Activator 16
  • HY-D3404
    BODi-1

    		DNA Stain Others
    BODi-1 is a fluorescent modulator targeting dsDNA, which binds to dsDNA via a bis-intercalation mechanism (Ex=465 nm, Em=490 nm). BODi-1 exhibits a fluorescence enhancement effect upon binding to nucleic acids, but its fluorescence intensity, anisotropy and average lifetime decrease at higher dye/DNA ratios. When BODi-1 binds to DNA in liposome complexes, it also shows red-shifted emission spectra, along with reduced quantum yield and average lifetime. BODi-1 does not induce significant DNA conformational changes when the dye/DNA ratio is below 0.01. BODi-1 can be used as a fluorescent probe for the characterization of liposome complexes and FRET studies at this ratio .
    BODi-1
  • HY-179507
    p53 Activator 17

    		MDM-2/p53 Apoptosis Cancer
    p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer .
    p53 Activator 17

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