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BDCRB is a selective Human cytomegalovirus (HCMV) inhibitor through blocking the maturational cleavage of high-molecular-weight DNA. BDCRB shows a mean IC50 of 0.03 μM for viral yield at 72 h postinfection .
Demethyl bleomycin A2 is a Bleomycin (HY-108345) congener. The DNA cleavage of demethyl bleomycin A2 is insensitive to the presence of 5-Methylcytidine (HY-113135) .
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site .
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/cleavage .
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent .
DNase I (EC 3.1.21.1) is an enzyme that degrade DNA, it plays a key role in the cleavage of extracellular DNA is crucial for limiting the inflammatory response and maintaining homeostasis. Exogenous deoxyribonuclease shows beneficial effects in inflammatory diseases and cancer .
CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent .
KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
PAR4 antagonist 2 (Compound 31) is a protease activated receptor 4 (PAR4) antagonist, with IC50 values of 95 nM and 367 nM for human PAR4 and mouse PAR4. PAR4 antagonist 2 is active against PAR4 activation by the native protease thrombin cleavage but not the synthetic PAR4 agonist peptide AYPGKF .
6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively .
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects .
UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [ 3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro .
Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections .
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections .
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor .
Kuguaglycoside C is a triterpene glycoside that can be isolated from the leaves of Momordica charantia. Kuguaglycoside C induces caspase‐independent DNA cleavage and cell death of neuroblastoma cells. Kuguaglycoside C also significantly increases the expression and cleavage of apoptosis-inducing factor (AIF) .
Hyaluronidase (Hyaluronate 4-glycanohydrolase; Hyaluronoglucosaminidase) is a naturally occurring enzyme that depolymerizes hyaluronic acid by cleavage of glycosidic bonds .
Glucocerebrosidase (Glucosylceramidase; GBA) is a lysosomal enzyme that catalyzes the cleavage of β-glucosidic linkage of glucocerebroside (GC) into glucose and ceramide .
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
Isocaproaldehyde is a product of side-chain cleavage of cholesterol. Isocaproaldehyde is an endogenous specific substrate of mouse vas deferens protein (MVDP) .
Nucleoside hydrolase (IAGNH) is a glycosidase. Nucleoside hydrolase (IAGNH) catalyzes the cleavage of the N-glycosidic bond in nucleosides to enable the recycling of the nucleobases and Rib .
[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes .
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 .
Bacitracin Zinc (Zinc bacitracin) is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.
SBP-3 is a sulfite bioluminescent probe (SBP). The recognition of SBP-3 towards sulfite is based on the mechanism of a sulfite-mediated intramolecular cleavage reaction .
SBP-2 is a sulfite bioluminescent probe (SBP). The recognition of SBP-2 towards sulfite is based on the mechanism of a sulfite-mediated intramolecular cleavage reaction .
Feruloyl esterase plays a major role in the degradation of plant biomass. Feruloyl esterase catalyzes the cleavage and formation of ester bonds between plant cell wall polysaccharide and phenolic acid .
2-Oxobutanoic acid (Standard) is the analytical standard of 2-Oxobutanoic acid. This product is intended for research and analytical applications. 2-Oxobutanoic acid is a product in the enzymatic cleavage of cystathionine.
FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
Enterostatin (human,mouse,rat) TFA is a pentapeptide mainly formed in the intestine by the cleavage of secreted pancreatic procolipase. Enterostatin selectively reduces fat intake, bodyweight, and body fat in vivo .
FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
2-Hydroxytetradecanoic acid is a hydroxy fatty acid that inhibits cleavage between the enterovirus capsid proteins VP4 and VP2. 2-Hydroxytetradecanoic Acid has anti-virus activity .
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .
Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC) .
Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC) .
Phleomycin is an anticancer glycopeptide antibiotic found in Streptomyces verticillus, which cause DNA cleavage. Phleomycin binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A) .
Ac-EEVVAC-pNA is a chromogenic substrate for a continuous spectrophotometric assay of HCV NS3 protease. The sequence EEVVAC is derived from the 5A-5B cleavage junction of the HCV polyprotein .
Dynorphin B (1-9) is a neuropeptide and N-terminal cleavage product of dynorphin B. The formation of dynorphin B (1-9) is blocked by N-ethylmaleimide (NEM), a non-selective inhibitor of cysteine peptidases .
LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells .
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy .
Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9 .
AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay .
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR) . Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage .
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage . Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes .
Distamycin A (NSC-82150), an oligopeptide antibiotic, is a minor groove binder which binds to B-form DNA, preferentially at A/T rich sites.Distamycin A can change Enediyne-induced DNA cleavage sites and enhances apoptosis .
PNGase F, a glycosidase, catalyzes the cleavage of an internal glycoside bond in an oligosaccharide. PNGase F removes nearly all N-linked oligosaccharides from glycoproteins. PNGase F can release N-glycans from glycoproteins in glycoanalytical workflows .
HSV-1 Protease substrate is a peptide substrate for HSV-1 (Herpes Simplex Virus Type 1) protease, and the specificity constant (kcat/Km) at pH 7.5 for cleavage is 5.2 M -1 s -1 .
Recombinant DNase I (RNase-free) is a recombinant deoxyribonuclease that degrades DNA. Recombinant DNase I is essential for limiting inflammatory responses and maintaining homeostasis .
Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
Avacincaptad pegol (ARC1905) is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. Avacincaptad pegol is being used for the study of age-related macular degeneration (AMD).
Methyl (+/-)-2-hydroxystearateis a hydroxylated fatty acid methyl ester that broadens phase transitions in dimyristoylphosphatidylcholine (DMPC) lipid membranes. It has been used in the synthesis of lipid-nucleotide conjugated anti-HIV agents to increase the cleavage of phosphodiester bonds and the number of released intracellular nucleotides.
α-Secretase Substrate II, Fluorogenic is an internally quenched fluorogenic peptide substrate for α-Secretase that contains the α-secretase cleavage site of β-Amyloid precursor protein (APP) .Ex/Em = 340/490 nm
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells .
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
G3-CNP is an α-amylase substrate. The absorbance of G3-CNP cleavage product 2-chloro-4-nitrophenol is measured at 405 nm, which can be used to detect enzyme activity .
Bacitracin (Zinc) (Standard) is the analytical standard of Bacitracin (Zinc). This product is intended for research and analytical applications. Bacitracin Zinc (Zinc bacitracin) is a dephosphorylated product of C55-isoprenyl pyrophosphate and inhibits Tyr cleavage from Met-enkephalin with an IC50 of 10 μM.
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .
Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
5-Fluorouridine, a metabolite of 5-fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis .
Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Tesidolumab (LFG316) is a fully-human IgG1/λ anti-C5 monoclonal antibody of 143 kDa (without glycosylation). Tesidolumab (LFG316) blocks cleavage of C5 and prevents subsequent formation of the membrane attack complex .
6-Chloro-3-indolyl-β-D-glucuronide cyclohexylammonium salt is a chromogenic substrate for β-glucuronidase. 6-Chloro-3-indolyl-β-D-glucuronide cyclohexylammonium salt produces a salmon colored precipitate upon cleavage .
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research .
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems . Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln) .
RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property .
Antitumor agent-72 (compound 6w) is a potent anticancer agent. Antitumor agent-72 has anticancer activity and induces apoptosis through activation of caspase-3 and cleavage of PARP. Antitumor agent-72 can be used for cancer research .
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly .
3-Cyano-7-ethoxycoumarin is a fluorogenic cytochrome P-450 substrate that generates blue fluorescent product upon enzyme cleavage
Target: Cytochrome P450
3-Cyano-7-ethoxycoumarin is a fluorescent probe useful in microsomal dealkylase studies.
4-Methylumbelliferyl-α-D-galactopyranoside (4MU-α-Gal), a substrate for α-galactosidase A (GLA), is a blue pro-fluorogenic substrate. 4-Methylumbelliferyl-α-D-galactopyranoside forms two products, galactose and fluorescent 4MU, upon cleavage by GLA .
Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity .
LHRH (1-5) (free acid) is a polypeptide generated by the cleavage of LHRH at the Tyr 55-Gly 66 site. LHRH (1-5) (free acid) is converted into LHRH (1-3) and LHRH (4-5) fragments under the catalysis of Angiotensin-converting enzyme (HY-P2983) .
8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase .
3-Indolyl-β-D-glucuronide, a chromogenic substrate for β-D-glucuronidase, employs in the detection and enumeration of E. coli, yielding a blue precipitate upon cleavage. 3-Indolyl-β-D-glucuronide in? patients' plasma act as a new indicator of renal failure .
Suc-YVAD-pNA is a substrate of ICE. Interleukin-1β-converting enzyme (ICE) is a cysteine protease responsible for the cleavage of pre-interleukin-1β (pre-IL-1β) to the mature cytokine and a member of a family of related proteases (the caspases) .
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .
Methylene Violet 3RAX is a phenazine dye to stain the mitochondria of cells. Methylene Violet 3RAX can change the molecular structure of DNA, undermine the module of DNA, and induce the generation of the reactive singlet oxygen. Methylene Violet 3RAX shows inhibition for human erythrocyte AChE and human plasma BChE with an Kis of 1.58, 0.51 μM, respectively. Methylene Violet 3RAX has the potential for the research of potential photosensitizers for mitochondrial targeting action in PDT (photodynamic therapy) .
(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a popular weight loss food supplement. (-)-Hydroxycitric acid lactone is a potent inhibitor of ATP-citrate lyase. (-)-Hydroxycitric acid lactone catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA, limits the availability of acetyl-CoA units required for fatty acid synthesis .
8-NH2-ATP, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado is reported to be potent as shown by induction of apoptosis-related cleavage of poly (ADP-ribose) polymerase .
SpCas9 D10A Nickase is a mutant of the Cas9 protein. SpCas9 D10A Nickase retains the function of a cleavage domain of Cas9 nuclease and specifically cleaves the target single strand to form a nick. SpCas9 D10A Nickase reduces off-target effects .
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases .
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research .
HA-IN-1 (compound 5g) is a Hemagglutinin (HA) ligand with high affinity, targeting to the trypsin cleavage site of HA. HA-IN-1 inhibits HA-mediated membrane fusion and reduces the pulmonary virus titer in vivo. HA-IN-1 is a potential influenza A virus (IAV) inhibitor, and an anti-influenza agent .
N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA .
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). Free 4MβNA can be captured by 5-nitrosalicylaldehyde to produce an insoluble yellow fluorescent and marks the site of thrombin activity .
TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
Evybactin is a DNA gyrase inhibitor. Evybactin is a selective inhibitor of Mycobacterium tuberculosis with a MIC value of 0.25 µg/mL. Evybactin is the first antimicrobial compound found to employ this unusual mechanism of selectivity .
CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-1 is a dual inhibitor of CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-1 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research .
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage .
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM .
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparumcleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections .
USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate .
Zilovertamab vedotin (VLS-101) is a novel antibody-drug conjugate comprising the humanized monoclonal antibody zilovertamab and and the anti-microtubule cytotoxin monomethyl vedotin. Zilovertamab vedotin binding to tumor cell ROR1 results in rapid internalization, trafficking to lysosomes, antibody–agent conjugate cleavage, and monomethyl vedotin release. Zilovertamab vedotin induces apoptosis. Zilovertamab vedotin can be used in research of cancer .
JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces Apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) .
SRE-II, an amide derivative, is an activatable photosensitizer for photodynamic cancer research with decreased fluorescence and photosensitizing capabilities. SRE-II can be further converted into the active photosensitizer SDU Red via carboxylesterase-catalyzed amide bond cleavage. SRE-II induces DNA damage and cell apoptosis in the presence of light. SRE-II can act as a promising theranostic agent for triple-negative breast cancer .
D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice .
Antibacterial agent 113 (compound 3) is a potent antibacterial agent. Antibacterial agent 113 shows antibacterial activity against P.aeruginosa, S.mutans, B.subtilis, E.coli, E.faecalis, S.typhimuriumand, and S.aureus microorganisms, with MIC values all of 156.25 μM .
Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has the potential for soft tissue sarcoma and ovarian cancer research .
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
Bacterial Sortase Substrate III, Abz/DNP is an internally quenched fluorescent peptide substrate. Staphylococcus aureus transpeptidase sortase A (SrtA) reacts with its native substrate Bacterial Sortase Substrate III, Abz/DNP, cleaving it and catalyzing the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Cleavage of this substrate can be monitored at Ex/Em=320 nm/420 nm.
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage . Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME) .
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs .
CCD-2 is a conventional detergent and is readily degraded. CCD-2 can efficiently solubilize and stabilize diverse G protein-coupled receptors (GPCRs). CCD-2 is amenable to the β-barrel protein research. The chemical cleavage of CCD-2 is rapid, complete and biorthogonal and should facilitate a chemical methodology for in situ detergent replacement in diverse membrane proteins (MPs) studies .
3-O-(2'E ,4'Z-Decadienoyl)-20-O-acetylingenol (compound 6) is a diterpene that can be isolated from Euphorbia kansui. 3-O-(2'E ,4'Z-Decadienoyl)-20-O-acetylingenol shows cleavage inhibition activity of individual Xenopus cells at the blastular stage .
Bacterial Sortase Substrate III, Abz/DNP TFA is an internally quenched fluorescent peptide substrate. Staphylococcus aureus transpeptidase sortase A (SrtA) reacts with its native substrate Bacterial Sortase Substrate III, Abz/DNP, cleaving it and catalyzing the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Cleavage of this substrate can be monitored at Ex/Em=320 nm/420 nm.
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects .
RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARPcleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer .
α-Galactosidase, Aspergillus niger (EC 3.2.1.22), that is, α-galactosidase, is a glycoside hydrolase that widely exists in animals, plants and microorganisms, and is often used in biochemical research. α-Galactosidase catalyzes the hydrolysis of α-1,6-linked terminal galactose residues, including galactooligosaccharides, galactomannans, and galactolipids. Catalyzes many catabolic processes including cleavage of glycoproteins, glycolipids and polysaccharides .
Mipsagargin (G-202) is a novel thapsigargin-based targeted proagent consisting of a prostate-specific membrane antigen (PSMA)-specific peptide coupled to an analog of the potent sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump inhibitor Thapsigargin (HY-13433). Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research .
(1R,3S)-Compound E is the isomer of Compound E (HY-14176), and can be used as an experimental control. Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity .
9-cis-Retinal is a natural retinoid. Dietary 9-cis-β-carotene generates 9-cis-retinoids via cleavage into 9-cis-retinal. 9-cis Retinal binds to cellular retinol-binding protein-I (CRBP-I) and CRBP-II with Kds of 8 nM and 5 nM, respectively. 9-cis-Retinal expedites differentiation and maturation of rod photoreceptors in retinal organoids .
GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects .
CTSLCTSB-IN-1 (compound 212-148) is a bispecific inhibitor of host viral spike cleaver proteins CTSL/CTSB and TMPRSS2 with IC50s of 2.13/64.07 nM and 1.38 μM, respectively. CTSLCTSB-IN-1 blocks two relevant SARS-CoV-2 viral entry pathways by inhibiting the viral spike cleavage and can be applied to anti-SARS-CoV-2 research .
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity .
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .
Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma .
N1-Acetylspermidine-d6 (hydrochloride) is the deuterium labeled N1-Acetylspermidine hydrochloride. N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA[1][2][3].
SBP-1 is a sulfite bioluminescent probe (SBP). SBP-1 exhibits the excellent responsivity, selectivity and sensitivity towards sulfite. The recognition of SBP-1 towards sulfite is based on the mechanism of a sulfite-mediated intramolecular cleavage reaction. SBP-1 can be used for detection of exogenous and endogenous sulfite in living animal. SBP-1 also possesses a capability for quantitatively detecting sulfite within a certain concentration range in solution .
(Ser8)-GLP-1 (7-36) amide, human is a glucagon-like peptide 1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. (Ser8)-GLP-1 (7-36) amide, human is an entero-insulinotropic hormone that causes glucose-dependent release of insulin from pancreatic β-cells and affects gastrointestinal motility and secretion .
4-Methylumbelliferyl sulfate (potassium), a fluorescent substrate, is commonly used to detect sulfatase activity in biochemical and biomedical research. It consists of a sulfate group attached to a fluorescent molecule, which can be cleaved by sulfatase enzymes. Upon cleavage, 4-Methylumbelliferyl sulfate releases a highly fluorescent product that can be detected using fluorescence microscopy or spectroscopy. The use of 4-Methylumbelliferyl sulfate as a substrate for sulfatase enzymes allows accurate detection and quantification of these enzymes in a variety of biological samples.
Arachidonoyl Thio-PC is a substrate of many phospholipase A2 (PLA2), including sPLA2, cPLA2 and iPLA2. Cleavage of sn-2 fatty acids by PLA2 results in the production of free thiols, which react with chromogenic reagents such as DTNB (Ellman's reagent) and DTP, allowing quantification of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by depleting or inhibiting sPLA2 and iPLA2 activity in the assay.
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspasescleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
D-Leu-Pro-Arg-Rh110-D-Pro is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro can be used to detect FXIa activity .
D-Leu-Pro-Arg-Rh110-D-Pro acetate is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro acetate consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro acetate can be used to detect FXIa activity .
HDAC-IN-27 (Compound 11h) is a potent, selective and orally active HDAC Class I inhibitor, with IC50 values ranging from 0.43 nM to 3.01 nM for HDAC1-3. HDAC-IN-27 shows anti-acute myeloid leukemia (AML) activity .
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM .
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 .
D-Leu-Pro-Arg-Rh110-D-Pro TFA is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro TFA consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro TFA can be used to detect FXIa activity .
N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine (5'-O-DMT-N4-Bz-dC) can be used for synthesis oligodeoxynucleotides containing a 3'-S-phosphorothiolate (3'-PS) linkage. N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine is an useful tool for probing enzyme-catalyzed cleavage processes in DNA .
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 .
JC2-11 is an inhibitor of inflammatory corpuscles. JC2-11 inhibits domain-containing protein NLRC 4, absent in melanoma 2 (AIM 2) and non-canonical (NC) inflammatory corpuscles. JC2-11 reduces the secretion of caspase-1 (p20), the cleavage of gasdermin D (GSDMD), and the releases of IL-1β and lactate dehydrogenases (LDH) in inflammatory bodies. JC2-11 inhibits the activation of inflammatory bodies by destroying the production of reactive oxygen species and the activity of caspase-1 .
PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and antiviral agent with broad-spectrum anti- Influenza activity. PAN is the N-terminal PA subunit of the polymerase-RNA complex and the dependent endonuclease (CEN) active site. PAN initiates RNA replication by promoting cleavage of the RNA strand and allowing the polymerase to begin synthesizing new RNA molecules. PAN endonuclease-IN-2 targets both the influenza HA and RdRp complexes, thereby interfering with viral entry into host cells and viral replication .
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells .
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers .
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
Caspase-3 activator 1 (compound 4b) is a Ru(III) metal complex that inhibits gastric tumor growth and metastasis. Caspase-3 activator 1 mediates caspase-3 cleavage, which in turn causes Caspase-3 to cleave gasdermin E (GSDME) to produce the GSDME-N terminus, causing gastric tumor cell membrane perforation. Caspase-3 activator 1 is capable of inducing pyroptosis and pyroptosis-induced immune responses and can be assembled with decitabine DCT (HY-A0004) into a 4b-DCT-Lip lipid delivery system .
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
1,8-Dihydroxy-4,5-dinitroanthraquinone (ARDP0006; DHDNE) is a potent inhibitor of serine proteinase NS2B/3, the dengue viral protein. 1,8-Dihydroxy-4,5-dinitroanthraquinone has intermolecular proteinase activity and viral inhibition ability with IC50s of 432 μM and 4.2 μM, respectively. Meanwhile 1,8-Dihydroxy-4,5-dinitroanthraquinone inhibits NS2B/3 cleavage in BHK-21 cells at a dose ranging from 4.2 μM to 432 μM .
Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1 .
Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1 .
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
TNO211 is a biological active peptide. (Matrix Metalloproteinases (MMPs) are a large family of endopeptidases. Collectively, MMPs can degrade all kinds of extracellular matrix proteins, and can also process a number of bioactive molecules. They are known to be involved in the cleavage of cell surface receptors, the release of apoptotic ligands, and chemokine/cytokine inactivation. MMPs are also thought to play a major role in cell behaviors such as cell proliferation, migration (adhesion/dispersion), differentiation, angiogenesis, apoptosis, and host defense.This peptide is a highly soluble fluorogenic MMP substrate for MMP-2, 8, 12, 13 and 14, containing the MMP cleavable Gly-Leu bond and EDANS/DABCYL. Fluorogenic assays using TNO211 are sensitive and can detect MMP activity in culture medium from endothelial cells and untreated synovial fluid from patients. Abs/Em = 340/490 nm.)
3-Cyano-7-ethoxycoumarin is a fluorogenic cytochrome P-450 substrate that generates blue fluorescent product upon enzyme cleavage
Target: Cytochrome P450
3-Cyano-7-ethoxycoumarin is a fluorescent probe useful in microsomal dealkylase studies.
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
Ac-EEVVAC-pNA is a chromogenic substrate for a continuous spectrophotometric assay of HCV NS3 protease. The sequence EEVVAC is derived from the 5A-5B cleavage junction of the HCV polyprotein .
Nucleoside hydrolase (IAGNH) is a glycosidase. Nucleoside hydrolase (IAGNH) catalyzes the cleavage of the N-glycosidic bond in nucleosides to enable the recycling of the nucleobases and Rib .
PNGase F, a glycosidase, catalyzes the cleavage of an internal glycoside bond in an oligosaccharide. PNGase F removes nearly all N-linked oligosaccharides from glycoproteins. PNGase F can release N-glycans from glycoproteins in glycoanalytical workflows .
G3-CNP is an α-amylase substrate. The absorbance of G3-CNP cleavage product 2-chloro-4-nitrophenol is measured at 405 nm, which can be used to detect enzyme activity .
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
Methyl (+/-)-2-hydroxystearateis a hydroxylated fatty acid methyl ester that broadens phase transitions in dimyristoylphosphatidylcholine (DMPC) lipid membranes. It has been used in the synthesis of lipid-nucleotide conjugated anti-HIV agents to increase the cleavage of phosphodiester bonds and the number of released intracellular nucleotides.
4-Methylumbelliferyl sulfate (potassium), a fluorescent substrate, is commonly used to detect sulfatase activity in biochemical and biomedical research. It consists of a sulfate group attached to a fluorescent molecule, which can be cleaved by sulfatase enzymes. Upon cleavage, 4-Methylumbelliferyl sulfate releases a highly fluorescent product that can be detected using fluorescence microscopy or spectroscopy. The use of 4-Methylumbelliferyl sulfate as a substrate for sulfatase enzymes allows accurate detection and quantification of these enzymes in a variety of biological samples.
Arachidonoyl Thio-PC is a substrate of many phospholipase A2 (PLA2), including sPLA2, cPLA2 and iPLA2. Cleavage of sn-2 fatty acids by PLA2 results in the production of free thiols, which react with chromogenic reagents such as DTNB (Ellman's reagent) and DTP, allowing quantification of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by depleting or inhibiting sPLA2 and iPLA2 activity in the assay.
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site .
Big Endothelin-1 (22-38), human is derived from human, is the 22-38 fragment of Big Endothelin-1 (ET-1) (1-38). Big ET-1 (1-38) is a propeptide of ET-1, which has potent and long-lasting vasoconstrictor effects, equips a specific enzymatic cleavage of the 38 amino acid chain to form ET-1 (1-21) and the C-terminal fragment Big ET-1 (22-38) .
[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes .
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 .
FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
Enterostatin (human,mouse,rat) TFA is a pentapeptide mainly formed in the intestine by the cleavage of secreted pancreatic procolipase. Enterostatin selectively reduces fat intake, bodyweight, and body fat in vivo .
Renin FRET Substrate I is a substrate of human renin. Renin FRET Substrate I is designed to incorporate the renin cleavage site that occurs in the N-terminal peptide of human angiotensinogen .
FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
FLAG peptide is an eight amino acids peptide (Asp-Tyr-Lys-Asp-Asp-Asp-Asp-Lys) with an enterokinase-cleavage site; designed for antibody-mediated identification and purification of recombinant proteins.
Ac-EEVVAC-pNA is a chromogenic substrate for a continuous spectrophotometric assay of HCV NS3 protease. The sequence EEVVAC is derived from the 5A-5B cleavage junction of the HCV polyprotein .
Dynorphin B (1-9) is a neuropeptide and N-terminal cleavage product of dynorphin B. The formation of dynorphin B (1-9) is blocked by N-ethylmaleimide (NEM), a non-selective inhibitor of cysteine peptidases .
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
HSV-1 Protease substrate is a peptide substrate for HSV-1 (Herpes Simplex Virus Type 1) protease, and the specificity constant (kcat/Km) at pH 7.5 for cleavage is 5.2 M -1 s -1 .
Glycylglycylcysteine is a Thrombin Activatable Fibrinolysis Inhibitor (TAFI) inhibitor with a Ki of 0.99 μM and a IC50 of 9.4 μM in TAFI substrate assays. TAFI is a basic carboxypeptidase that functions as a fibrinolysis inhibitor through the cleavage of C-terminal lysine on partially degraded fibrin .
α-Secretase Substrate II, Fluorogenic is an internally quenched fluorogenic peptide substrate for α-Secretase that contains the α-secretase cleavage site of β-Amyloid precursor protein (APP) .Ex/Em = 340/490 nm
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
[Glu1]-Fibrinopeptide B is derived from fibrinopeptide B amino acid residues 1-14. Human fibrinopeptide B (hFpB), a thrombin-derived proteolytic cleavage product of the fibrinogen B beta-chain, to stimulate neutrophils (PMN), monocytes, and fibroblasts.
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
LHRH (1-5) (free acid) is a polypeptide generated by the cleavage of LHRH at the Tyr 55-Gly 66 site. LHRH (1-5) (free acid) is converted into LHRH (1-3) and LHRH (4-5) fragments under the catalysis of Angiotensin-converting enzyme (HY-P2983) .
Dabcyl-AGHDAHASET-Edans is a biological active peptide. (This is a type I signal peptidase (SPase1) substrate peptide labeled with EDANS/ DABCYL FRET pair, and contains a crucial cleavage site derived from the C-terminal region of the Staphylococcus epidermidis pre-SceD protein. Abs/Em = 340/490 nm.)
Suc-YVAD-pNA is a substrate of ICE. Interleukin-1β-converting enzyme (ICE) is a cysteine protease responsible for the cleavage of pre-interleukin-1β (pre-IL-1β) to the mature cytokine and a member of a family of related proteases (the caspases) .
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-ψ-(COO)Ala-Ser-Lys(DABCYL)-NH2 (HCV NS3 protease substrate) is a biological active peptide. (This peptide is a HCV protease substrate incorporating an ester bond between residues P1 and P1. Due to ready transesterification of the scissile bond to the acyl-enzyme intermediate, this substrate shows very high kcat/Km values, enabling detection of activity with subnanomolar nonstructural protein 3 (NS3 protease) concentrations. It is widely used for the continuous assay of NS3 protease activity. Substrate cleavage is proportional to the enzyme concentration with a detection limit for NS3 between 1 nM and 250 pM. Upon cleavage of this substrate, fluorescence can be monitored at Abs/Em = 355/500 nm.)
Ac-LEHD-pNA is a biological active peptide. (Caspase-9 substrate; pNA (4-nitroaniline)-derived caspase substrates are widely used for the colorimetric detection of various caspase activities. Cleavage of pNA peptides by caspases generates pNA that is monitored colorimetrically at ~405 nm. pNA has maximum absorption around 408 nm.)
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). Free 4MβNA can be captured by 5-nitrosalicylaldehyde to produce an insoluble yellow fluorescent and marks the site of thrombin activity .
TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
Evybactin is a DNA gyrase inhibitor. Evybactin is a selective inhibitor of Mycobacterium tuberculosis with a MIC value of 0.25 µg/mL. Evybactin is the first antimicrobial compound found to employ this unusual mechanism of selectivity .
X-press Tag Peptide is a tag peptide used for protein purification. X-press Tag is also an N-terminal leader peptide; this N-terminal peptide contains a polyhistidine sequence, the Xpress epitope (part of bacteriophage T7 gene 10 protein) and an enterokinase cleavage site. Anti-Xpress antibodies recognize the Xpress epitope sequence found in this leader peptide.
Suc-AAPF-pNA (Suc-Ala-Ala-Pro-Phe-pNA) is a chromogenic p-nitroanilide (pNA) substrate with the Km of 1.7 mM. Cleavage of Suc-AAPF-pNA releases 4-nitroaniline, which is yellow in colour and can be measured spectrophotometrically. Suc-AAPF-pNA can be used for the measurement of free and membrane-bound cathepsin G in human neutrophils .
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
CLIP (86-100) is amino acids 86 to 100 fragment of class II-associated invariant chain peptide (CLIP). CLIP is a small self-peptide and cleavage product of the invariant chain that resides in the HLA-II antigen binding groove and is believed to play a critical role in the assembly and transport of MHC class II alphabetaIi complexes through its interaction with the class II peptide-binding site .
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
CLIP (86-100) TFA is amino acids 86 to 100 fragment of class II-associated invariant chain peptide (CLIP). CLIP is a small self-peptide and cleavage product of the invariant chain that resides in the HLA-II antigen binding groove and is believed to play a critical role in the assembly and transport of MHC class II alphabetaIi complexes through its interaction with the class II peptide-binding site .
Bacterial Sortase Substrate III, Abz/DNP is an internally quenched fluorescent peptide substrate. Staphylococcus aureus transpeptidase sortase A (SrtA) reacts with its native substrate Bacterial Sortase Substrate III, Abz/DNP, cleaving it and catalyzing the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Cleavage of this substrate can be monitored at Ex/Em=320 nm/420 nm.
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
Bacterial Sortase Substrate III, Abz/DNP TFA is an internally quenched fluorescent peptide substrate. Staphylococcus aureus transpeptidase sortase A (SrtA) reacts with its native substrate Bacterial Sortase Substrate III, Abz/DNP, cleaving it and catalyzing the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Cleavage of this substrate can be monitored at Ex/Em=320 nm/420 nm.
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects .
Mipsagargin (G-202) is a novel thapsigargin-based targeted proagent consisting of a prostate-specific membrane antigen (PSMA)-specific peptide coupled to an analog of the potent sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump inhibitor Thapsigargin (HY-13433). Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research .
HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity .
GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects .
(Ser8)-GLP-1 (7-36) amide, human is a glucagon-like peptide 1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. (Ser8)-GLP-1 (7-36) amide, human is an entero-insulinotropic hormone that causes glucose-dependent release of insulin from pancreatic β-cells and affects gastrointestinal motility and secretion .
DABCYL-LPETG-EDANS is a biological active peptide. (This 5-amino acid peptide is a sortase substrate, C-terminal sorting signal. Sortase cleaves surface proteins at the LPXTG motif and catalyzes the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Sortases are a family of Gram-positive transpeptidases responsible for anchoring surface protein virulence factors to the peptidoglycan cell wall layer. Cleavage of this FRET substrate by sortase reveals the fluorescent signal, Abs/Em = 340/490 nm.)
D-Leu-Pro-Arg-Rh110-D-Pro is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro can be used to detect FXIa activity .
D-Leu-Pro-Arg-Rh110-D-Pro acetate is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro acetate consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro acetate can be used to detect FXIa activity .
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 .
D-Leu-Pro-Arg-Rh110-D-Pro TFA is a substrate for Factor Xa I (FXIa) with binding affinity. D-Leu-Pro-Arg-Rh110-D-Pro TFA consists of Rhodamine 110 (HY-D0817) linked to a peptide chain through a cleavable bond. Cleavable bond cleavage enhances fluorophore intensity. D-Leu-Pro-Arg-Rh110-D-Pro TFA can be used to detect FXIa activity .
TNO211 is a biological active peptide. (Matrix Metalloproteinases (MMPs) are a large family of endopeptidases. Collectively, MMPs can degrade all kinds of extracellular matrix proteins, and can also process a number of bioactive molecules. They are known to be involved in the cleavage of cell surface receptors, the release of apoptotic ligands, and chemokine/cytokine inactivation. MMPs are also thought to play a major role in cell behaviors such as cell proliferation, migration (adhesion/dispersion), differentiation, angiogenesis, apoptosis, and host defense.This peptide is a highly soluble fluorogenic MMP substrate for MMP-2, 8, 12, 13 and 14, containing the MMP cleavable Gly-Leu bond and EDANS/DABCYL. Fluorogenic assays using TNO211 are sensitive and can detect MMP activity in culture medium from endothelial cells and untreated synovial fluid from patients. Abs/Em = 340/490 nm.)
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.)
Tesidolumab (LFG316) is a fully-human IgG1/λ anti-C5 monoclonal antibody of 143 kDa (without glycosylation). Tesidolumab (LFG316) blocks cleavage of C5 and prevents subsequent formation of the membrane attack complex .
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research .
Zilovertamab vedotin (VLS-101) is a novel antibody-drug conjugate comprising the humanized monoclonal antibody zilovertamab and and the anti-microtubule cytotoxin monomethyl vedotin. Zilovertamab vedotin binding to tumor cell ROR1 results in rapid internalization, trafficking to lysosomes, antibody–agent conjugate cleavage, and monomethyl vedotin release. Zilovertamab vedotin induces apoptosis. Zilovertamab vedotin can be used in research of cancer .
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9 .
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/cleavage .
6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively .
Kuguaglycoside C is a triterpene glycoside that can be isolated from the leaves of Momordica charantia. Kuguaglycoside C induces caspase‐independent DNA cleavage and cell death of neuroblastoma cells. Kuguaglycoside C also significantly increases the expression and cleavage of apoptosis-inducing factor (AIF) .
Glucocerebrosidase (Glucosylceramidase; GBA) is a lysosomal enzyme that catalyzes the cleavage of β-glucosidic linkage of glucocerebroside (GC) into glucose and ceramide .
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
Isocaproaldehyde is a product of side-chain cleavage of cholesterol. Isocaproaldehyde is an endogenous specific substrate of mouse vas deferens protein (MVDP) .
2-Oxobutanoic acid (Standard) is the analytical standard of 2-Oxobutanoic acid. This product is intended for research and analytical applications. 2-Oxobutanoic acid is a product in the enzymatic cleavage of cystathionine.
Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC) .
Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC) .
Phleomycin is an anticancer glycopeptide antibiotic found in Streptomyces verticillus, which cause DNA cleavage. Phleomycin binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A) .
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR) . Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage .
Distamycin A (NSC-82150), an oligopeptide antibiotic, is a minor groove binder which binds to B-form DNA, preferentially at A/T rich sites.Distamycin A can change Enediyne-induced DNA cleavage sites and enhances apoptosis .
Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells .
8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase .
3-Indolyl-β-D-glucuronide, a chromogenic substrate for β-D-glucuronidase, employs in the detection and enumeration of E. coli, yielding a blue precipitate upon cleavage. 3-Indolyl-β-D-glucuronide in? patients' plasma act as a new indicator of renal failure .
(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a popular weight loss food supplement. (-)-Hydroxycitric acid lactone is a potent inhibitor of ATP-citrate lyase. (-)-Hydroxycitric acid lactone catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA, limits the availability of acetyl-CoA units required for fatty acid synthesis .
8-NH2-ATP, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado is reported to be potent as shown by induction of apoptosis-related cleavage of poly (ADP-ribose) polymerase .
N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA .
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage .
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has the potential for soft tissue sarcoma and ovarian cancer research .
3-O-(2'E ,4'Z-Decadienoyl)-20-O-acetylingenol (compound 6) is a diterpene that can be isolated from Euphorbia kansui. 3-O-(2'E ,4'Z-Decadienoyl)-20-O-acetylingenol shows cleavage inhibition activity of individual Xenopus cells at the blastular stage .
9-cis-Retinal is a natural retinoid. Dietary 9-cis-β-carotene generates 9-cis-retinoids via cleavage into 9-cis-retinal. 9-cis Retinal binds to cellular retinol-binding protein-I (CRBP-I) and CRBP-II with Kds of 8 nM and 5 nM, respectively. 9-cis-Retinal expedites differentiation and maturation of rod photoreceptors in retinal organoids .
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
GCSH protein, a vital component of the glycine cleavage system, efficiently shuttles the methylamine group of glycine from the P protein (GLDC) to the T protein (GCST), contributing to glycine degradation. GCSH Protein, Human (His) is the recombinant human-derived GCSH protein, expressed by E. coli , with N-His labeled tag. The total length of GCSH Protein, Human (His) is 125 a.a., with molecular weight of ~17 KDa.
Caspase-3/CASP3 protein is a thiol protease critical in apoptosis and is activated by initiating caspases (CASP8, CASP9 and/or CASP10). It catalyzes the cleavage of multiple proteins in sympathetic neurons, including PARP1, SREBP, caspase-6, -7 and -9, huntingtin, and RET. Caspase-3/CASP3 Protein, Human is the recombinant human-derived Caspase-3/CASP3 protein, expressed by E. coli , with tag free. The total length of Caspase-3/CASP3 Protein, Human is 248 a.a., .
Caspase-3/CASP3 protein is a thiol protease critical in apoptosis and is activated by initiating caspases (CASP8, CASP9 and/or CASP10). It catalyzes the cleavage of multiple proteins in sympathetic neurons, including PARP1, SREBP, caspase-6, -7 and -9, huntingtin, and RET. Caspase-3/CASP3 Protein, Human (His, Strep) is the recombinant human-derived Caspase-3/CASP3 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of Caspase-3/CASP3 Protein, Human (His, Strep) is 277 a.a., .
ACLY Protein, Human (His-SUMO) is an important enzyme in the cholesterol biosynthetic pathway. ACLY produces acetyl-CoA (AcCoA) from mitochondrial citrate for cholesterol and fatty acid biosynthesis.
N1-Acetylspermidine-d6 (hydrochloride) is the deuterium labeled N1-Acetylspermidine hydrochloride. N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA[1][2][3].
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
ATP Citrate Lyase Antibody (YA829) is a non-conjugated and Mouse origined monoclonal antibody about 121 kDa, targeting to ATP Citrate Lyase (3D9). It can be used for WB,ICC/IF,FC assays with tag free, in the background of Human, Mouse, Monkey.
CYP11A1 Antibody is an unconjugated, approximately 53/57 kDa, rabbit-derived, anti-CYP11A1 polyclonal antibody. CYP11A1 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, Flow-Cyt, ICC, IF expriments in human, mouse, rat, and predicted: dog, pig, cow, horse, rabbit, sheep background without labeling.
Cleaved-Caspase 3 p12 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 32 kDa, targeting to Cleaved-Caspase 3 p12. It can be used for WB,ICC/IF assays with tag free, in the background of Human, Mouse, Rat.
Deg-1 is a a bifunctional probe with a cleavage group and a covalent binding group. Deg-1 covalently binds to the target nucleic acid, and serves as click-degrader to cleave a nucleic acid molecule. Deg-1 has potential to selectively cleave target nucleic acids in cells .
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