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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
411 Results for "
Conformational
" in MedChemExpress (MCE) Product Catalog:
Products (411)
411 Results for "Conformational" in MCE Product Catalog:
127
127 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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Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
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29 Cited Publications
Cat. No.: HY-16926
CAS No.: 442633-00-3
Target:
CK-666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC50=12 μM). CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation .
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15 Cited Publications
CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
14
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 .
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11 Cited Publications
Research Areas:
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
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9 Cited Publications
Cat. No.: HY-P1740
CAS No.: 114681-65-1
Research Areas:
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9 Cited Publications
Cat. No.: HY-P1740A
Research Areas:
8
8 Cited Publications
Cat. No.: HY-18669
CAS No.: 100872-83-1
ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27 .
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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 .
7
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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6 Cited Publications
Synonyms: GDC-9545; RG6171
Target:
Research Areas:
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 .
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6 Cited Publications
Synonyms: Methylmaleic acid
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4 Cited Publications
Cat. No.: HY-19896
CAS No.: 1039455-84-9
COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
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4 Cited Publications
Cat. No.: HY-P99129
Target:
Research Areas:
3
3 Cited Publications
Synonyms: Guanidinium chloride; Aminoformamidine hydrochloride
Target:
3
3
3
3 Cited Publications
Target:
Research Areas:
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) .
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3 Cited Publications
Target:
Research Areas:
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) .
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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
