37 Results for "

cleavable site

" in MedChemExpress (MCE) Product Catalog:
Products (37)

37 Results for "cleavable site" in MCE Product Catalog:

  • Targets Recommended:
4
4 Cited Publications
Cat. No.: HY-D2449
DQ-BSA-Red is a bovine serum albumin labeled with a red fluorescent dye that can be used to detect lysosomal activity. The excitation wavelength and emission wavelength of DQ-BSA-Red are 590 nm and 620 nm, respectively. The BSA molecule in DQ-BSA-Red is labeled with high concentration of red fluorescent dye in multiple sites, which shows high fluorescence self-inhibition. Once DQ-BSA-RED enters the lysosome, DQ-BSA is cleaved by lysosomal proteases, resulting in unquenched and released fluorescent fragments, emitting bright fluorescence. Inactivated lysosomes are unable to degrade the BSA protein and thus have a lower or even no fluorescent signal .
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2
2 Cited Publications
Cat. No.: HY-13240
CAS No.: 1262036-50-9
Purity:  99.72%
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
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2
2 Cited Publications
Cat. No.: HY-13438
CAS No.: 1227163-84-9
Purity:  99.91%
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

AZD3839 is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 can be used in the field of Alzheimer's disease research .
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1
1 Cited Publications
Cat. No.: HY-119689
CAS No.: 1387560-01-1
Purity:  99.81%
Synonyms: CNP520
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively . Umibecestat can be used for the research of alzheimer's disease.
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1
1 Cited Publications
Cat. No.: HY-109052
CAS No.: 1200493-78-2
Purity:  99.77%
Synonyms: JNJ-54861911
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
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1
1 Cited Publications
Cat. No.: HY-112157
CAS No.: 1818339-66-0
Purity:  99.23%
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
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1
1 Cited Publications
Cat. No.: HY-E70365A
Research Areas:  

Inflammation/Immunology

IdeS (Immobilized, Microspin) is a resin that covalently couples IdeS protease to agarose beads and cleaves IgG at specific sites to generate F(ab')2 and Fc fragments. After IdeS (Immobilized, Microspin) digestion, F(ab')2 and Fc fragments are obtained in the solution without IdeS enzyme.
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Cat. No.: HY-123740
CAS No.: 1351828-03-9
Purity:  99.00%
Synonyms: DSSO
Research Areas:  

Others

Disuccinimidyl sulfoxide (DSSO) is a sulfoxide-containing crosslinker targeting amino groups that can be cleaved by MS, and it is suitable for model peptides, proteins, and multisubunit protein complexes. Disuccinimidyl sulfoxide contains two symmetric collision-induced dissociation (CID)-cleavable sites, enabling the identification of DSSO-crosslinked peptides based on different fragmentation patterns .
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Cat. No.: HY-P3208B
CAS No.: 72561-05-8
Research Areas:  

Others

Endoproteinase Lys-C (MS grade) is a hydrolase that cleaves peptide bonds at the carboxyl side of lysine residues. Endoproteinase Lys-C (MS grade) causes non-specific hydrolysis of peptide bonds linked to the carboxyl groups of non-lysine residues, resulting in partial cleavage at these sites .
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Cat. No.: HY-D1078
CAS No.: 127770-45-0
5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
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Cat. No.: HY-163944
CAS No.: 3081311-94-3
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
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Cat. No.: HY-130426
CAS No.: 518044-40-1
Purity:  ≥98.0%
Synonyms: Mal-PEG3-acid
Research Areas:  

Cancer

Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-specific cysteine mutant trastuzumab-A114C conjugation . Maleimido-tri(ethylene glycol)-propionic acid also can be used as a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Cat. No.: HY-P99238
CAS No.: 2095467-30-2

Target:  

ADC Antibodies

Research Areas:  

Inflammation/Immunology Cancer

Rolinsatamab is a IgG1κ type chimeric antibody targeting to PRLR (prolactin receptor). Rolinsatamab can be conjugated with pyrrolobenzodiazepine (PDB) dimer SGD-1882 (HY-101127) via a cleavable maleimidocaproyl type linker, to form an antibody-drug conjugate, Rolinsatamab talirine. One Rolinsatamab talirine has an average of 2 site-specific drug attachment engineered cysteines (S239C). The linker equips the valine-alanine dipeptide, as cathepsine B cleavage site. on an average of 2 site-specific drug attachment engineered cysteines (S239C) .
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Cat. No.: HY-145657
CAS No.: 207671-99-6
Purity:  99.89%
Synonyms: BQQ
Research Areas:  

Others

Benzoquinoquinoxaline (BQQ) is a heterocyclic compound with an aminoalkyl side chain. Benzoquinoquinoxaline preferentially binds to DNA triplex structures, intercalates between the bases, thus, stabilising the triplex conformation. Conjugation of Benzoquinoquinoxaline to 1,10-phenanthroline specifically binds and cleaves double strand DNA at the site of formation of a triplex structure .
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Cat. No.: HY-P2754
CAS No.: 9013-53-0
Target:  

Endonuclease Bacterial

Research Areas:  

Infection

Micrococcal nuclease is a secreted nuclease from Staphylococcus aureus. It digests single-stranded and double-stranded DNA (ssDNA and dsDNA) as well as RNA, cleaves oligonucleotide linkers with T-T sites, and cuts neutrophil extracellular traps and biofilm extracellular DNA into mononucleotides and dinucleotides. Micrococcal nuclease stimulates the formation of Staphylococcus aureus biofilms and mediates immune evasion. It triggers on-demand release of antibiotics from hydrogel coatings, prolongs the formation of neutrophil extracellular traps, and promotes the dissemination and survival of MRSA during infection. Micrococcal nuclease is applicable to research and characterization related to Staphylococcus aureus infection .
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Cat. No.: HY-108966
CAS No.: 99119-73-0
Purity:  99.58%
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM .
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Cat. No.: HY-P5272
CAS No.: 112844-49-2
Target:  

Bacterial

Research Areas:  

Inflammation/Immunology

Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
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Cat. No.: HY-144741
CAS No.: 2872604-91-4
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM .
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Cat. No.: HY-175466
Research Areas:  

Cancer

BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib (HY-10162). BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
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Cat. No.: HY-13438A
CAS No.: 1421852-78-9
Target:  

Beta-secretase

Research Areas:  

Cancer

AZD3839 fumarate is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 fumarate inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 fumarate inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 fumarate binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 fumarate can be used in the field of Alzheimer's disease research .
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