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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
16 Results for "
conformational shift
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 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
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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
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 .
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-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-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-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-184447
CAS No.: 3091508-49-2
RN193 is a type II kinase inhibitor with a human PAK1 IC50 of 4.28 μM. RN193 functionally inhibits kinase activity of PAK1, PAK2, and PAK3, and engages with their kinase domains in live cells. RN193 induces thermal shifts in CLK1, GSK3B, ULK1, MELK, MAPK13, BRAF, and STK10, indicating binding and stabilization of these proteins. RN193 induces formation of PAK3:PAK2 heterodimers and displaces PAK2 homodimers in live cells. RN193 acts as a tool compound for studying group I PAK conformational states .
Cat. No.: HY-D3404
CAS No.: 169454-13-1
Cat. No.: HY-179507
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 .
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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
