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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
333 Results for "
binding pocket
" in MedChemExpress (MCE) Product Catalog:
Products (333)
333 Results for "binding pocket" in MCE Product Catalog:
2
2 Cited Publications
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
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2 Cited Publications
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6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes .
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1 Cited Publications
Synonyms: PLB-1001; CBT-101; Vebreltinib
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Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily .
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1 Cited Publications
Cat. No.: HY-W011417
CAS No.: 606-59-7
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Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
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1 Cited Publications
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WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. WNK1-IN-1 inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for the research of blood pressure regulation and cancer .
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1 Cited Publications
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
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1 Cited Publications
Cat. No.: HY-W040230
CAS No.: 86636-92-2
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1 Cited Publications
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BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
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1 Cited Publications
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TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM .
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1 Cited Publications
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NVS-STG2 is a molecular glue that targets STINGbinding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
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1 Cited Publications
Cat. No.: HY-W195984
CAS No.: 1016340-64-9
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Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer .
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Cat. No.: HY-160412
CAS No.: 2248726-53-4
Synonyms: SAR-441566; TNFα activity modulator 3
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Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases .
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Naa50-IN-1 is an N-alpha-acetyltransferase 50 (Naa50) inhibitor with an IC50 of 7 nM against the human protein. Naa50-IN-1 exhibits selectivity toward the related enzymes Naa10 and Naa60. Naa50-IN-1 binds to the substrate-binding pocket of Naa50, and its binding affinity is enhanced by AcCoA .
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NR162 is a selective CASK (Ca 2+/calmodulin-dependent Ser/Thr kinase) inhibitor with an IC50 of 80 nM and a Kd of 22 nM. NR162 shows about 50-fold selectivity for CASK than TYRO3. NR162 targets the unique GFG motif of CASK and has excellent shape complementarity to the CASK ATP binding pocket. NR162 can be used for the research of neurological diseases .
Cat. No.: HY-155583
Purity: 98.08%
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RNase L-IN-1 is a RNase L inhibitor with an IC50 of 15.9 μM. RNase L-IN-1 binds to the ATP-binding pocket of RNase L, and inhibits ribosomal RNA cleavage. RNase L-IN-1 can be used for the research of RNase L-associated cellular processes .
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PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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DAUDA is a fluorescent fatty acid analog probe, with Kd values of 0.63 μM, 0.82 μM, and 0.66 μM against subtypes/mutants of Schistosoma mansoni Sm14 fatty acid-binding protein, respectively. DAUDA binds to Sm14 fatty acid-binding protein variants, enters their non-polar binding pockets and alters fluorescence emission properties. DAUDA serves as a tracer in competitive binding assays with natural fatty acids to evaluate the fatty acid-binding capacity of Sm14 protein variants. DAUDA is applicable to the research of schistosomiasis .
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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
