12 Results for "

substrate-binding domain

" in MedChemExpress (MCE) Product Catalog:
Products (12)

12 Results for "substrate-binding domain" in MCE Product Catalog:

Cat. No.: HY-168437
Target:  

MicroRNA

Research Areas:  

Cancer

LIN28-IN-2 is a Lin28 inhibitor with activity against Lin28a, Lin28b, and their zinc knuckle domain. LIN28-IN-2 blocks Lin28-RNA substrate binding, perturbs zinc knuckle domain conformation. LIN28-IN-2 inhibits cancer cell proliferation, spheroid growth, and induces G2/M phase arrest. LIN28-IN-2 suppresses cancer stem cell phenotypes, Lin28-mediated stress granule formation, let-7 target genes, cancer stem cell biomarkers, and neuroendocrine biomarkers expression in cancer cells. LIN28-IN-2 can be used for the research of cancer .
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Cat. No.: HY-122184
CAS No.: 34387-64-9
Target:  

HSP Apoptosis

Research Areas:  

Cancer

PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma .
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Cat. No.: HY-157558
Synonyms: 8SGE
Target:  

Ligands for E3 Ligase

Research Areas:  

Others

KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
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Cat. No.: HY-P3892
CAS No.: 309247-48-1
Target:  

PKC

Research Areas:  

Inflammation/Immunology

Protein Kinase C (19-35) Peptide is the PKC pseudosubstrate inhibitor/region. Protein Kinase C (19-35) Peptide possibly blocks the substrate-binding site in its kinase domain, makes the cytoplasmic form of PKC inactive .
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Cat. No.: HY-P11080
CAS No.: 1235497-90-1
Target:  

Bacterial

Research Areas:  

Infection

Oncocin is an antibacterial peptide. It belongs to proline-rich antimicrobial peptides (PrAMPs). Oncocin works against Gram-negative bacteria. It has MIC values of 0.125-8 μg/mL for 34 strains and clinical isolates of Enterobacteriaceae and nonfermenters. Oncocin binds to the substrate-binding domain of the chaperone DnaK. The binding has dissociation constants in the micromolar range. This binding causes protein misfolding and aggregation and the bacteria death .
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Cat. No.: HY-157559
Target:  

Ligands for E3 Ligase

Research Areas:  

Others

KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
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Cat. No.: HY-183406
CAS No.: 102616-62-6
Research Areas:  

Neurological Disease Cancer

AS15 is a PDIA1 inhibitor with an IC50 value of 300 nM. AS15 interacts with the active-site cysteine of PDIA1, and this process is independent of the substrate-binding domain of PDIA1. AS15 acts as a synergistic cell growth inhibitor with buthionine sulfoximine (BSO) (HY-106376), a glutathione synthesis inhibitor. AS15 can be used in the research of glioblastoma .
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Cat. No.: HY-P6300
CAS No.: 169062-92-4
Target:  

Bacterial Parasite

Research Areas:  

Infection

Cyclomarin A is an antibacterial agent with a Kd of 2.3 nM against Mycobacterium tuberculosis ClpC1, a Kd of 2.2 nM against ClpC2, and an IC50 of 0.004 μM against Plasmodium falciparum PfAp3Aase. Cyclomarin A binds to the N-terminal domain of ClpC1, stimulates ATPase and proteolytic activities, dysregulates proteolysis, and induces proteome imbalance; it also binds to ClpC2 and upregulates its transcription level. Cyclomarin A binds to PfAp3Aase in dimeric form, blocks the substrate-binding pathway, inhibits the growth of Plasmodium falciparum in the erythrocytic stage, and shows no activity against human cells. Cyclomarin A exhibits moderate cytotoxicity against a variety of cancer cell lines. Cyclomarin A can serve as a lead compound for the development of Homo-BacPROTAC. Cyclomarin A is applicable to research related to tuberculosis and malaria .
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Cat. No.: HY-P11620
CAS No.: 290810-63-8
Target:  

Drug Derivative

Research Areas:  

Others

H-Asn-Pro-Glu-Tyr(PO3H2)-OH is a phosphorylated peptide derivative of the tetramine motif Asn-Pro-Glu-Tyr (NPEY), and is a substrate binding domain common to the insulin-like growth factor-I receptor (IGF-IR) and the insulin receptor (IR).
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Cat. No.: HY-181810
CAS No.: 2215779-34-1
Target:  

HSP Bacterial

Research Areas:  

Infection

EG36 is a selective E. coli DnaK inhibitor that inhibits DnaK ATPase activity at a concentration of 100 μM. EG36 directly binds to the nucleotide-binding domain (NBD) of E. coli DnaK by disrupting the DnaK-DnaJ interaction. EG36 can be used for research on bacterial infectious diseases .
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Cat. No.: HY-182372
CAS No.: 1638153-78-2
Target:  

Epoxide Hydrolase

Research Areas:  

Neurological Disease

SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
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Cat. No.: HY-138934
CAS No.: 1642375-66-3
Target:  

PDI

Research Areas:  

Cardiovascular Disease

Bepristat 1a is a reversible, selective protein disulfide isomerase (PDI) inhibitor with an IC50 of 0.7 μM. Bepristat 1a inhibits platelet aggregation in laser-injured mouse arterioles. Bepristat 1a is applicable for research related to thrombosis .
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