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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
33 Results for "
closed conformation
" in MedChemExpress (MCE) Product Catalog:
Products (33)
33 Results for "closed conformation" in MCE Product Catalog:
135
135 Publications Verification
Synonyms: STI571; CGP-57148B
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 .
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eCF506 (NXP900) is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer .
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2 Cited Publications
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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 .
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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 .
Synonyms: CC-99282
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Golcadomide (CC-99282) is a blood-brain barrier-permeable, orally active Cereblon (CRBN) E3 ligase modulator. Golcadomide induces Cereblon to form a closed active conformation, thereby recruiting and triggering the ubiquitin-mediated proteasomal degradation of transcription factors IKZF1, IKZF3, Ikaros and Aiolos. Golcadomide is applicable to research related to relapsed or refractory non-Hodgkin lymphoma, chronic lymphocytic leukemia/small lymphocytic lymphoma, and diffuse large B-cell lymphoma .
Cat. No.: HY-174801
CAS No.: 3117797-30-2
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XL-3156 is a cGAS inhibitor. XL-3156 occupies both allosteric and orthosteric sites simultaneously, and inhibits the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of diseases such as autoimmune diseases and inflammation .
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LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
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Phosphoglycerate kinase (PGK), yeast is a monomeric glycolytic/gluconeogenic enzyme that can be found in Saccharomyces cerevisiae. Phosphoglycerate kinase, yeast catalyzes phosphoryl-group transfer from 1,3-bisphosphoglycerate to ADP to form 3-phosphoglycerate and ATP, binds 3PGA, ATP, and Mg 2+, and adopts a closed conformation. Phosphoglycerate kinase, yeast is commonly used in biochemical research .
Cat. No.: HY-161431
CAS No.: 3035072-48-8
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RTx-152 is a potent and selective Polθ-pol allosteric inhibitor with an IC50 of 6.2 nM. RTx-152 binds to the allosteric pocket of the Polθ-pol finger domain, locking it in a closed conformation on the DNA substrate, thereby effectively inhibiting its catalytic cycle. RTx-152 synergizes with Olaparib (HY-10162) in BRCA2-deficient cells and synergizes with PARP inhibitors in homologous recombination-deficient cells. RTx-152 can be used for research on homologous recombination-deficient cancers such as BRCA2 mutations .
Cat. No.: HY-174802
CAS No.: 3117797-77-7
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XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
Cat. No.: HY-15463R
CAS No.: 152459-95-5
Synonyms: STI571 (Standard); CGP-57148B (Standard)
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 .
Cat. No.: HY-P1441
CAS No.: 1609937-15-6
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Cat. No.: HY-162505
CAS No.: 1255915-27-5
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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 .
Cat. No.: HY-114611
CAS No.: 2011754-00-8
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BDM44768 is an insulin-degrading enzyme (IDE) inhibitor (human IC50 = 0.06 μM; Ki = 60 nM). BDM44768 impairs D-Glucose (HY-B0389) tolerance, enhances Insulin (HY-P0035) signaling, and increases Amyloid-β concentration in an IDE-dependent manner by chelating the catalytic zinc, stabilizing the closed conformation, and binding the substrate/catalytic cleft. BDM44768 can be used in research on diabetes and metabolic dysfunction-associated steatotic liver disease (MASLD) .
Cat. No.: HY-112096S
Synonyms: NXP900-d5
Cat. No.: HY-15463S3
Synonyms: STI571-13C,d3; CGP-57148B-13C,d3
Cat. No.: HY-116205
CAS No.: 1357838-47-1
UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
Synonyms: STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
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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 .
Cat. No.: HY-131275R
CAS No.: 1365802-18-1
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Imatinib Impurity E (Standard) is the analytical standard of Imatinib Impurity E (HY-131275). This product is intended for research and analytical applications. 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 .
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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
