Search Result
Results for "
cleavable site
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-123740
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DSSO
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Biochemical Assay Reagents
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Others
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Disuccinimidyl sulfoxide (DSSO) is a mass spectrometry (MS)-cleavable cross-linker that is applicable for model peptides and proteins and a multisubunit protein complex. Disuccinimidyl sulfoxide contains two symmetric collision-induced dissociation (CID)-cleavable sites for identification of DSSO-cross-linked peptides based their distinct fragmentation patterns .
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- HY-112157
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Beta-secretase
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Neurological Disease
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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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- HY-N1255
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(-)-Scoulerine; Discretamine
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Microtubule/Tubulin
Beta-secretase
Apoptosis
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Cancer
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Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
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- HY-146125
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Endonuclease
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Metabolic Disease
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CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme .
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- HY-P2610
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Caspase
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Others
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Ac-VEID-pNA is an artificially synthesized peptide. Ac-VEID-pNA is utilized as substrate for caspase 6, that cleaves the lamin A at the cleavage site of VEID .
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- HY-144739
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- HY-144741
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- HY-E70128
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Others
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Others
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Leucyl aminopeptidase is a metallopeptidase that cleave N-terminal residues from proteins and peptides. Leucyl aminopeptidase serves as transcriptional repressors to control pyrimidine, alginate and cholera toxin biosynthesis, as well as mediate site-specific recombination events in plasmids and phages .
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- HY-E70393J
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Others
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Others
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Bovine Factor XIa is an enzyme, which is involved in the intrinsic pathway of blood coagulation. Bovine Factor XIa is highly selective and exhibits a minimal extended substrate recognition site of at least five residues long. Bovine Factor XIa is reactive as Bovine Factor IXa (HY-E70393I) does, that it cleaves all the peptides bearing factor IX activation site sequences .
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- HY-108966
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Beta-secretase
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Inflammation/Immunology
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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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- HY-P99238
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ADC Antibody
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Inflammation/Immunology
Cancer
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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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- HY-U00287
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Beta-secretase
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Neurological Disease
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BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
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- HY-145657
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BQQ
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Others
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Others
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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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- HY-119689
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CNP520
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Beta-secretase
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Neurological Disease
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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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- HY-15908
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BCA
5 Publications Verification
Disodium bicinchoninate
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Beta-secretase
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Neurological Disease
Cancer
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BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
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- HY-109052
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JNJ-54861911
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Beta-secretase
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Neurological Disease
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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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- HY-130244
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Beta-secretase
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Neurological Disease
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BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
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- HY-P10668
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Dengue virus
Flavivirus
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Infection
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Ac-EVKKQR-pNA is a competitive chromogenic para-nitroanilide substrate corresponding to the P6-P1 segment amino-terminal to the NS2B-NS3 cleavage site but with a more reactive, hydrolytically cleavable, para-nitroanilide at the P1’ position. Ac-EVKKQR-pNA is promising for research of dengue 2 virus and flavivirus virus infection .
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- HY-130426
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Mal-PEG3-acid
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ADC Linker
PROTAC Linkers
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Cancer
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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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- HY-13240
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Beta-secretase
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Neurological Disease
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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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- HY-13240A
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Beta-secretase
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Neurological Disease
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LY2886721 hydrochloride 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 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
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- HY-128774
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Beta-secretase
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Neurological Disease
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AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P5272
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Bacterial
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Inflammation/Immunology
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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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- HY-D2449
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Fluorescent Dye
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Others
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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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- HY-P5415
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HIV
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Others
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DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-kD protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
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Cat. No. |
Product Name |
Type |
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- HY-D2449
-
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Dyes
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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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Cat. No. |
Product Name |
Type |
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- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Biochemical Assay Reagents
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5272
-
|
Bacterial
|
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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- HY-P2610
-
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Caspase
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Others
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Ac-VEID-pNA is an artificially synthesized peptide. Ac-VEID-pNA is utilized as substrate for caspase 6, that cleaves the lamin A at the cleavage site of VEID .
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- HY-P5274
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Peptides
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Others
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BACE1 (485-501) is the carboxyl terminal of BACE1 (Beta-site APP cleaving enzyme 1). BACE1 (485-501) can be used as antigen to produce anti-BACE1-C antibody .
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- HY-P10668
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Dengue virus
Flavivirus
|
Infection
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Ac-EVKKQR-pNA is a competitive chromogenic para-nitroanilide substrate corresponding to the P6-P1 segment amino-terminal to the NS2B-NS3 cleavage site but with a more reactive, hydrolytically cleavable, para-nitroanilide at the P1’ position. Ac-EVKKQR-pNA is promising for research of dengue 2 virus and flavivirus virus infection .
|
-
- HY-P5415
-
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HIV
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Others
|
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-kD protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99238
-
|
ADC Antibody
|
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) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
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Classification |
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- HY-128774
-
|
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Alkynes
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AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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