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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
conformational shift
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "conformational shift" in MCE Product Catalog:
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-160406
CAS No.: 2332803-84-4
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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 .
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1 Cited Publications
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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 .
Cat. No.: HY-159520
CAS No.: 2731294-23-6
Synonyms: Ofirnoflast; HT-6184
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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 .
Synonyms: PK4C9
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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 .
Cat. No.: HY-134136A
CAS No.: 324518-20-9
Synonyms: 7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole
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MBD (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole) is a hydrophobic fluorescent probe that is used to detect conformational changes of the complement subcomponent C1r during its autoactivation process. MBD acts by selectively binding to exposed hydrophobic regions on the C1r macromolecule. The detection wavelength of MBD in the free unbound state is Ex/Em = 490/560 nm, whereas the maximum emission wavelength of MBD upon binding to C1r exhibits a blue shift of approximately 20 nm relative to 560 nm .
Synonyms: BW 12C; 12C79; BW 12C79
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Velaresol (BW 12C) is a small molecule oxyhemoglobin stabilizer. Velaresol stabilizes hemoglobin’s oxy-conformation, shifts oxygen dissociation curves left, induces tumor hypoxia, alters radiosensitivity, protects normal tissues from radiation damage, and reduces sickled cell counts. Velaresol can be used for the research of cancer and sickle cell disease .
Cat. No.: HY-D1470
CAS No.: 210832-86-3
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BADAN is a thiol-reactive, environment-sensitive fluorescent probe used for site-specific labeling of protein cysteine residues to detect protein topology, local polarity, protein-lipid interactions, and conformational changes. The bromoacetyl group of BADAN covalently binds to cysteine thiols, and its fluorescence originates from the intramolecular charge transfer (ICT) excited state. The emission peak position varies with the polarity of the surrounding medium: it blue-shifts to approximately 488 nm in nonpolar environments (such as the hydrophobic core of lipid bilayers) and red-shifts to approximately 496-507 nm in polar environments (such as aqueous phases), independent of enzymes, pH, or membrane potential. Ex = 380-402 nm; Em = 400-600 nm .
Cat. No.: HY-P10984
CAS No.: 206536-96-1
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Cat. No.: HY-134136B
CAS No.: 799812-82-1
Synonyms: S-Octanoate-CoA triammonium; S-Octanoate-coenzyme A triammonium
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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 .
Cat. No.: HY-168636
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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 .
Cat. No.: HY-179506
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 .
Cat. No.: HY-Z20873
CAS No.: 84210-35-5
MK-4815 is an orally active small-molecule allosteric inhibitor of Falcilysin (FLN) with antimalarial activity. MK-4815 inhibits the viability of Plasmodium falciparum NF54 and Dd2 strains with IC50 values of 38 and 40 ng/mL, respectively. MK-4815 preferentially accumulates in erythrocytes containing mature trophozoite/schizont-stage parasites. MK-4815 preferentially binds to the partially closed conformation of FLN, shifting the FLN conformational equilibrium toward the partially closed state and restricting the hinge region-mediated transition from the partially closed state to the open state, thereby interfering with the catalytic cycle of FLN. MK-4815 can be used for malaria-related research .
Cat. No.: HY-181128
CAS No.: 2253948-15-9
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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 .
Cat. No.: HY-106509R
CAS No.: 77858-21-0
Synonyms: BW 12C (Standard); 12C79 (Standard); BW 12C79 (Standard)
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Velaresol (Standard) is the analytical standard of Velaresol. This product is intended for research and analytical applications. Velaresol (BW 12C) is a small molecule oxyhemoglobin stabilizer. Velaresol stabilizes hemoglobin’s oxy-conformation, shifts oxygen dissociation curves left, induces tumor hypoxia, alters radiosensitivity, protects normal tissues from radiation damage, and reduces sickled cell counts. Velaresol can be used for the research of cancer and sickle cell disease .
Cat. No.: HY-D3103
CAS No.: 1027058-07-6
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CMTDP is a Fluorescent probe for detecting local polarity changes around the Cys34 domain of bovine serum albumin during pH-induced N→B conformational transition. It is a thiol-specific and polarity-sensitive probe; it covalently labels the free cysteine residue at position 34 (Cys34) of bovine serum albumin, and its fluorescence maximum emission wavelength shifts in response to solvent polarity, but not to pH and temperature. When labeled to BSA, as the local polarity around the Cys34 domain increases with rising pH, the probe shows a bathchromic shift in fluorescence emission wavelength and a decrease in fluorescence intensity, which allows quantification of the local polarity change via the relationship between emission wavelength shift and dielectric constant. CMTDP itself has absorption peaks at ~392 and 508 nm, and CMTDP-labeled BSA has excitation maxima at 376 and 470 nm at pH 6.0, with the shorter-wavelength excitation peak red-shifting as pH increases while the longer one remains stable; when excited at 470 nm, the fluorescence emission maximum shifts from 570 nm at pH 6.0 to 577 nm at pH 9.1, while free CMTDP at pH 7.4 has an emission maximum at 621 nm. The excitation/emission wavelengths for CMTDP-labeled BSA are Ex/Em = 376/570 nm at pH 6.0, Ex/Em = ~376+/573 nm at pH 7.4, Ex/Em = ~376+/575 nm at pH 8.0, Ex/Em = ~376+/577 nm at pH 9.1, and for free CMTDP at pH 7.4, Ex/Em (when excited at 470 nm) = 470/621 nm[1].
Cat. No.: HY-D3377
CAS No.: 1616953-95-7
Synonyms: LysoRhoNox
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HMRhoNox-M (LysoRhoNox) is a selective fluorescent probe for detecting Fe 2+ (ferrous iron ions), with excitation/emission wavelengths of Ex/Em = 550/575 nm. HMRhoNox-M exists in a non-fluorescent spirocyclic closed conformation under physiological pH conditions. Fe 2+ triggers the deoxidation of its N-oxide group, shifting the equilibrium toward the fluorescent quinone-type (TMHMR) open conformation. HMRhoNox-M shows selectivity for Fe 2+ over other metal ions, as well as biologically relevant reactive oxygen species, reactive sulfur species, reactive nitrogen species and reducing agents. HMRhoNox-M can penetrate cell membranes and localize to lysosomes, enabling the imaging of intracellular Fe 2+ fluctuations, transferrin-mediated labile iron accumulation, and lysosomal Fe 2+ changes associated with ferroptosis .
Cat. No.: HY-D3111
CAS No.: 1240465-12-6
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DBHA is a long-wavelength polarity-sensitive fluorescent probe based on Nile Red. Under the catalysis of Pd (OAc)2/TPPTS, DBHA site-selectively labels protein tyrosine residues via a π-allyl palladium complex intermediate. Utilizing the property that its maximum emission wavelength blue-shifts with decreasing local polarity (650 nm in aqueous solution → 584-608 nm in hydrophobic domains), it detects changes in local polarity and conformation of protein tyrosine domains under acid/thermal denaturation conditions. DBHA can be used in studies related to SOD1-associated oxidative stress neurodegenerative diseases .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
