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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 "
hinge region
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "hinge region" in MCE Product Catalog:
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3 Cited Publications
Synonyms: TAS6417; CLN-081
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
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1 Cited Publications
Cat. No.: HY-E70365
CAS No.: 2764750-38-9
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IdeS protease is an IgG-specific endopeptidase, which is highly specific for the lower hinge region of IgG. IdeS protease represses innate immune responses to promote streptococcal survival in an inflammatory environment .
Cat. No.: HY-P99391
CAS No.: 1781223-80-0
Synonyms: ABT-700; ABBV-400 Antibody
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Telisotuzumab (ABT-700) is a bivalent humanized IgG1 anti-c-Met monoclonal antibody. Telisotuzumab binds cellular c-Met and disrupts its productive dimerization and activation induced by HGF or by the high density of c-Met on the cell surface independent of ligand. Telisotuzumab induces apoptosis. The Fc hinge region of Telisotuzumab has been engineered to enhance its rigidity by introducing a new disulfide bond (K222C) and shortening the hinge length (T223del, T225del). Telisotuzumab can be used for the study of cancers harboring amplified MET, such as gastric and lung cancers .
Cat. No.: HY-N10472
CAS No.: 123297-90-5
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Cat. No.: HY-E70364
CAS No.: 1892548-76-3
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IgdE protease is a cysteine protease, which is initially isolated from Streptococcus agalactiae. IgdE protease digests monoclonal antibodies (mAbs) of the IgG1 type specifically at their upper hinge region, produces Fc/2, hinge peptide dimers, and Fab fragment. IgdE protease can be used in disulfide bonds and free thiol analysis, as it requires no reducing agents for cleavage .
Cat. No.: HY-L907
12,372 compounds
The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity.
The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments.
MCE provides over 12,372 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.
Cat. No.: HY-P99391B
CAS No.: 1781223-80-0
Synonyms: ABT-700 (WT IgG1); ABBV-400 Antibody (WT IgG1)
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Telisotuzumab (WT IgG1) is a monoclonal antibody that retains the natural wild-type IgG1 Fc structure without engineering modification. Telisotuzumab (HY-P99391) is a humanized IgG1 anti-c-Met monoclonal antibody; its Fc hinge region has been engineered to enhance hinge rigidity by introducing a new disulfide bond (K222C) and shortening the hinge length (T223del, T225del) .
Cat. No.: HY-189951
CAS No.: 260046-94-4
Pim-1 kinase-IN-18 is a Pim-1 kinase inhibitor with an IC50 of 5.77 µM. Pim-1 kinase-IN-18 inhibits Pim serine/threonine kinase activity by occupying the ATP binding site, its pyrazole ring forms dual polar interactions with residues in the catalytic region, and its oxindole binds to the hinge region. Pim-1 kinase-IN-18 can be used in cancer-related research .
Cat. No.: HY-189843
CAS No.: 3135322-96-9
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ZJCK-6-72 is a potent, orally effective DYRK1A inhibitor that crosses the blood-brain barrier, with an IC50 of 8.64 nM. ZJCK-6-72 binds to the hinge region of the ATP pocket of DYRK1A and reduces P-gp efflux, thereby blocking the activation of NF-κB and the NLRP3 inflammasome, and significantly downregulating pro-inflammatory cytokines such as TNF-α and IL-6, NO levels, and Pyroptosis. ZJCK-6-72 can be used for research on Alzheimer's disease .
Cat. No.: HY-P11905
CAS No.: 874909-17-8
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FcIII peptide is a 13-amino-acid peptide that competitively binds the hinge region of IgG Fc fragment with high affinity. FcIII peptide has an inhibition constant Ki of 25 nM when competing with Protein A for binding sites. FcIII peptide displays high selectivity toward human IgG subtypes yet weak binding affinity for murine IgG1. FcIII peptide anchors IgG Fc through hydrophobic interactions formed by tryptophan and valine residues, alongside multiple hydrogen bonds and salt bridges. FcIII peptide alters the local microenvironment of conjugated fluorescein after binding IgG Fc, which triggers enhanced fluorescent signals. FcIII peptide can be applied to researches related to monoclonal antibody production. .
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-187340
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CSF1R/c-Kit-IN-1 is a CSF-1R and c-Kit inhibitor, with an IC50 of 5.88 nM against human CSF-1R and an IC50 of 1.47 nM against human c-Kit. CSF1R/c-Kit-IN-1 binds to the ATP-binding pocket of CSF-1R, forming a hinge interaction with Cys666 via the oxazole nitrogen atom and adjacent amino group, and binds to residues in the hydrophobic binding pocket. CSF1R/c-Kit-IN-1 binds to the ATP-binding pocket of c-Kit, maintains a hinge interaction through its 2-amino-oxazole core, and binds to a broader hydrophobic surface near the solvent-exposed region via its morpholine substituent. CSF1R/c-Kit-IN-1 inhibits CSF-1-induced phosphorylation of ERK, which is a downstream readout of the CSF-1R signaling pathway. CSF1R/c-Kit-IN-1 can be used in the research of neuroinflammation-related neurodegenerative diseases .
Cat. No.: HY-182281
FLT3-IN-41 is a highly potent FLT3 inhibitor. The IC50 values of FLT3-IN-41 against human FLT3-ITD and FLT3-WT are 3.16 nM and 294.7 nM, respectively. By binding to the ATP-binding pockets of FLT3-ITD and FLT3-WT and forming hydrogen bonds with hinge region residues and Phe830, FLT3-IN-41 inhibits the STAT5, Akt and Erk signaling pathways. FLT3-IN-41 induces G2/M phase arrest and promotes apoptosis in FLT3-ITD-positive acute myeloid leukemia cells, exhibiting significant antiproliferative activity. FLT3-IN-41 serves as a valuable tool for the study of acute myeloid leukemia .
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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
