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Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
DSPE-PEG 2000-Mannose is a mannose-containing lipid. DSPE-PEG 2000-Mannose is used to prepare mannose-conjugated Liposome (Man-lipo) for siRNA delivery. Mannose-modified liposomes encapsulating IDO siRNA (Man-lipo-siIDO) preferentially knock down IDO expression in the draining lymph nodes and spleens of melanoma-bearing mice. Man-lipo-siIDO delays the onset time of melanoma and reduces tumor volume .
Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
BiP inducer X, a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78, is an effective ER (endoplasmic reticulum) stress inhibitor. BiP inducer X preferentially induces BiP with slight inductions of GRP94, calreticulin, and C/EBP homologous protein. BiP inducer X protects neurons from ER stress .
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
Rabacfosadine (GS-9219), a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
RU 24969 is a preferential5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion .
Magainin 2 (Magainin II) is an antimicrobial peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
GS-829845 is a is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects .
Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain .
NGI-235 is an STT3A-selective oligosaccharyltransferase complex OST-A inhibitor. NGI-235 preferentially inhibits OST-A catalytic activity, impairing N-glycosylation of OST-A substrates. NGI-235 causes the hypoglycosylation of both TLR4, GLUT1 andinhibits NF-κB signaling. NGI-235 can be used for the research of inflammation .
Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response .
Muscle homing peptide M12 can preferentially bind to surface protein of muscle cells. Muscle homing peptide M12 mediates enhanced cellular uptake of nanoparticles (NPs) in myoblasts in vitro. Muscle homing peptide M12 is covalently conjugated to PLGA-PEG NPs via the N-terminal α-amino groups of peptides using the N-hydroxysuccinimide ester reaction .
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis . D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors . D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor .
Aminopeptidase N (rat) (APN/CD13) is a Zn 2+-dependent membrane-bound exopeptidase that preferentially degrades proteins and peptides with N-terminal neutral amino acids. Aminopeptidase N (rat) is inhibited by angiotensin IV and participates in the regulation of angiotensin IV half-life in the rat striatum .
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis .
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma .
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
PPZ-A10 is an ionizable cationic lipid. PPZ-A10 preferentially delivers mRNA to liver and spleen immune cells. Pi-LNPs containing PPZ-A10 can effectively deliver mRNA/siRNA to solid tumors .
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 .
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia .
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively . Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation .
TTHA is an aminopolycarboxylic acid chelating agent with preferential affinity for lighter (lower atomic number) rare earth element (REE) ions. TTHA binds to REE ions through chelation as the primary coordination mechanism .
NAAA-IN-1 (Compound 1) is a potent and selective inhibitor of NAAA with an IC50 of 7 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-1 has the potential for the research of inflammation and pain .
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels .
m-PEG20000-OH can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Nanoscale micelles can be prepared by using amphiphilic block copolymers to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
Porfiromycin (N-Methylmitomycin C) is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts .
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species .
NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain .
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
CXM102 is an autophagy activator. CXM102 can induce autophagy in aged BMSCs, leading to the rejuvenation of BMSCs and preferential differentiation into osteoblasts. CXM102 promotes the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. CXM102 can stimulate bone synthesis metabolism in middle-aged male mice, reduce bone marrow adipocytes, delay bone loss, lower serum inflammation levels, decrease organ fibrosis, and extend the lifespan of the mice .
NSC 80467, a DNA damaging agent, selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and results in induction of γH2AX and pKAP1, two markers of DNA damage .
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
Rabacfosadine (GS-9219) succinate, a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells .
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation .
GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells .
H-Gly-Arg-pNA hydrochloride (GR-pNA hydrochloride) is a colorimetric substrate for thrombin. H-Gly-Arg-pNA is preferentially bound by thrombin and cleaves the Gly-Arg (GR) peptide sequence, releasing p-nitroaniline (pNA) that can be detected colorimetrically at 405 nm. H-Gly-Arg-pNA hydrochloride is used as a fluorescent dye to measure thrombin activity .
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
Anabaseine-d4 is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Mirogabalin- 13C2,d1 (Mixture of Diastereomers) is a 13C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
Luzindole (Standard) is the analytical standard of Luzindole. This product is intended for research and analytical applications. Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma .
Medifoxamine (Standard) is the analytical standard of Medifoxamine. This product is intended for research and analytical applications. Medifoxamine is a monoamine re-uptake inhibiting antidepressive agent which preferentially inhibits dopamine reuptake .
WAY-PDA 641 is a potent and preferentialPDE-IV inhibitor, with an IC50 of 0.42 μM for canine trachealis PDE-IV. WAY-PDA 641 induces respiratory muscle relaxation and bronchodilation .
G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein .
CSK substrate is a specific substrate for C-terminal Src kinase (CSK), which binds CSK and downregulates the Src family members. CSK substrate preferentially phosphorylates certain amino acid residues that are distinct from the conserved Src C-terminal sequence .
Lyso BD-1, preferentially colocalized in lysosomes and lipid droplets, displays excellent photocytotoxicity (5.57 μM) on triple negative breast cancer cells under white light. Lyso BD-1 displays emission band at 560nm .
BChE-IN-35 (Azo-9) is a BChE inhibitor. BChE-IN-35 has a dynamic cis/trans conformational change, where the cis isomer preferentially binds to BChE. BChE-IN-35 can be used in Alzheimer's disease (AD) research .
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
Midaglizole hydrochloride (DG5128) is a preferentialα2-adrenoceptor antagonist. Midaglizole hydrochloride (DG5128) exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.
Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .
Rp-8-CPT-cAMPS sodium, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS sodium preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
Anabaseine (Standard) is the analytical standard of Anabaseine. This product is intended for research and analytical applications. Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
YM116 is an orally active and competitive CYP17A1 (17,20-lyase) inhibitor (Ki: 0.38 nM). YM116 reduces the synthesis of adrenal androgens by preferentially inhibiting C17-20 lyase activity. YM116 decreases the serum testosterone concentration, reduces dehydroepiandrosterone sulfate levels and decreases prostatic weights .
RU 24969 hemisuccinate is a preferential5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion .
DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes .
Mirogabalin (Standard) is the analytical standard of Mirogabalin. This product is intended for research and analytical applications. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
Lomibuvir (Standard) is the analytical standard of Lomibuvir. This product is intended for research and analytical applications. Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis .
RU 24969 (Standard) is the analytical standard of RU 24969. This product is intended for research and analytical applications. RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion .
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain .
(S)-2-Hydroxy-acid oxidase (EC 1.1.3.15) is a flavoprotein (FMN) . Exists as two major isoenzymes; the A form preferentially oxidizes short-chain aliphatic hydroxy acids; the B form preferentially oxidizes long-chain and aromatic hydroxy acids.
Leucine Aminopeptidase(microsomal), Porcine (EC 3.4.11.2) is an enzyme that preferentially catalyze the hydrolysis of leucine residues at the N-terminus of peptides and proteins.
Achromopeptidase, Bacteria (EC 3.4.21.50) catalyses the following chemical reaction:Preferential cleavage:Lys-, including-Lys-Pro-. Achromopeptidase, Bacteria (EC 3.4.21.50) is isolated from Achromobacter lyticus.
L-703717 is a NMDA receptor antagonist. L-703717 preferentially binds to cerebellar-specific NMDA receptors consisting of a GluRepsilon3 subunit and eventually accumulates in rodent cerebellum. L-703717 can be used for the research of neurological disease .
Anti-PRAME Antibody is a monoclonal antibody that targets the melanoma antigen preferentially/PRAME. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-PRAME Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
ZINC13407541 is a fibroblast growth factor 23 (FGF23) antagonist with an IC50 of 0.45 μM. ZINC13407541 preferentially binds to the FGF23:FGFR interface to disrupt their protein-protein interactions. ZINC13407541 can be used for the research of hypophosphatemia .
Rennin, Mucor miehei (EC 3.4.23.23) hydrolyzes proteins, preferentially hydrolyzing hydrophobic residues at the P1 and P1' positions. Rennin, Mucor miehei (EC 3.4.23.23) can coagulate milk. Because the P1 position cannot accept lysine, it cannot activate trypsinogen.
Chlorophyllase (EC 3.1.1.14) is part of the chlorophyll degradation pathway and is believed to be involved in various plant chlorosis processes, such as fruit ripening, leaf senescence, and flowering, as well as chlorophyll turnover and homeostasis. Chlorophyllase (EC 3.1.1.14) preferentially acts on chlorophyll a, but can also use chlorophyll b and pheophytin as substrates.
NCT-10b (compound 17b) is a selective HDAC6 inhibitor.NCT-10b mediates preferential α-tubulin acetylation without major histone H4 acetylation.NCT-10b can be used for the research of multiple myeloma .
MEDI-2228 Antibody is an anti-human BCMA antibody that preferentially binds to membrane-bound BCMA versus soluble BCMA. MEDI-2228 Antibody can generate antibody drug conjugate (ADC) (MEDI 2228) with a pyrrolobenzodiazepine (PBD) dimer. MEDI-2228 Antibody can be used for the study of multiple myeloma .
ISR activator 2 is a selective ISR activator. ISR activator 2 can preferentially activate the ISR through the binding of the cytosolic pattern recognition receptor RIG-I, which subsequently activates the heme-regulated inhibitor (HRI) ISR kinase independent of an interferon response. ISR activator 2 can be used for the study of pancreatic cancer .
MAF-10L is a membrane-disrupting agent, a cationic amphipathic Mastoparan AF derivative with enhanced α-helicity. MAF-10L preferentially interacts with DOPS lipids in cancer cell membranes, disrupting cancer cell membranes to trigger membrane leakage. MAF-10L can be used for the research of cancer .
SIK2/3-IN-3 (Example 15) is a potent, selective SIK2/3 inhibitor that exhibits preferential inhibitory activity against SIK2 (IC50 = 10.3 nM) and SIK3 (IC50 = 0.8 nM) over SIK1 (IC50 = 801 nM). SIK2/3-IN-3 can be used for the study of inflammatory diseases .
Glyco-3ß,5α,6ß -trihydroxycholanoic acid (NPCBA2) is a bile acid which accumulates preferentially in Niemann-Pick C (NPC) patients. Glyco-3ß,5α,6ß -trihydroxycholanoic acid is a biomarker for the early diagnosis of Niemann-Pick C disease .
IOB-82 is a bifunctional alkylating agent. IOB‑82 induces marked nuclear and cytoplasmic alterations, elicits severe chromatid and chromosome aberrations, and remodels chromosome ploidy. IOB-82 exerts dose-dependent radiomimetic effects and preferentially cytotoxic to large A-type rat ascites cells. IOB-82 can be applied in the research of melanoma‑derived tumors and leukemia .
Aminopurvalanol A (Standard) is the analytical standard of Aminopurvalanol A (HY-104013). This product is intended for research and analytical applications. Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
AG2 is a glucose uptake tracer and two-photon fluorescent probe. AG2 is taken up by cells via glucose-specific transport systems, rather than passive diffusion; it preferentially accumulates in cancer cells and colon cancer tissues compared with normal cells and tissues; it mainly localizes to mitochondria, with a small amount also distributed in the cytoplasm and cell membrane. AG2 can be used for colon cancer research .
Gal-dMor-Gem is a selective senescent cell scavenger, Apoptosis inducer, and a prodrug of Gemcitabine (HY-17026). Gal-dMor-Gem releases Gemcitabine upon activation by Esterases and β-gal. Gal-dMor-Gem reduces SA-β-gal, preferentially induces apoptosis in senescent cells, regulates apoptosis-related proteins, accumulates in senescent tissues, and ameliorates senescence-related organ phenotypes. Gal-dMor-Gem is applicable to research on chemotherapy-induced senescence .
RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS G13D and KRAS G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers .
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
Chaetoglobosin A is a secondary metabolite and nematicide. Chaetoglobosin A is produced by Penicillium aquamarinium. Chaetoglobosin A targets Filamentous actin in cells, thereby inducing cell cycle arrest, and inhibiting membrane ruffle formation and cell migration. Chaetoglobosin A preferentially induces Apoptosis in chronic lymphocytic leukemia cells. Chaetoglobosin A induces dose- and time-dependent death in J2 larvae of the southern root-knot nematode (Meloidogyne incognita). Chaetoglobosin A can be used in studies related to root-knot nematode disease and chronic lymphocytic leukemia .
(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells .
Cyetpyrafen is a pyrazole insecticide/acaricide with broad-spectrum insecticidal activity. Cyetpyrafen binds to DhelOBP4 (Ki = 4.95 μM) and DhelOBP21 (Ki = 5.51 μM) to mediate olfactory recognition in *Cryptolaemus montrouzieri*. Cyetpyrafen induces dose-dependent electroantennogram responses in *Cryptolaemus montrouzieri* and exhibits repellent effects on the species. Cyetpyrafen has bioaccumulative properties, is rapidly and passively absorbed by the roots of lettuce and rice, reaches a steady state within 24 h, preferentially accumulates in roots, and shows limited xylem/phloem translocation .
GMQ is an acid-sensing ion channel modulator, competitive GABAAR antagonist. GMQ preferentially, potently, competitively inhibits GABAARs. GMQ inhibits α1β2, α1β2γ2, α4β2γ2 and α5β2γ2GABAARs. GMQ enhances neuronal excitation through inhibition of GABAergic transmission. GMQ has anti-histamine effects in the enteric system, inhibiting gastric acid secretion .
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .
Rendomab B4 is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity .
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
BD-Oligo is an oligomer-specific fluorescent chemical probe. BD-Oligo preferentially identifies Aβ oligomer assemblies over monomers or fibrils by using diversity-directed fluorescent library (DOFL) screening and computational techniques. BD-Oligo exhibits dynamic oligomer monitoring capabilities during Aβ peptide fibril formation as Aβ is induced to form oligomers and ultimately fibrils over time. BD-Oligo also exhibits blood-brain barrier permeability with the ability to stain Aβ oligomers in vivo .
EAD1 TFA is an aluminum-activated malate transporter with activity in regulating corn ear development. EAD1 TFA is preferentially expressed in the xylem of immature ears and localized across the plasma membrane. The EAD1 TFA transports malic acid in the apical part of developing inflorescences, and its deletion results in reduced malic acid content in this part. The overexpression of EAD1 TFA was significantly positively correlated with ear length and the number of kernels per row. EAD1 TFA serves as a potential genetic resource to help improve grain yield in maize .
ADI-14359 is an antibody that binds to RSV postF, with a KD value of 387 nM, and exhibits non-neutralizing activity. ADI-14359 binds to antigenic site I on RSV postF through interactions of its conserved CDR H3 motif, germline-encoded IGKV1-39 light chain residues and heavy chain residues, where the light chain mediates preferential binding to postF by conflicting with the rearranged preF region. ADI-14359 can be used in studies related to respiratory syncytial virus (RSV) infection .
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine (HY-N6691)-induced Ca 2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy .
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
YM-244769 is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice .
YM-244769 dihydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
YM-244769 hydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Propidium monoazide is a cell-impermeant photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .
AO-176 is a humanized anti-CD47 IgG2 monoclonal antibody. AO-176 induces tumor phagocytosis through blocking the CD47-SIRPα interaction. AO-176 preferentially binds to tumor versus normal cells and directly kills tumor by a cell autonomous mechanism not ADCC (antibody-dependent cell-mediated cytotoxicity). AO-176 demonstrates dose-dependent antitumor activity in tumor xenograft models. AO-176 can be used for the researches of cancer, such as lymphoma .
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) potently binds to type 2 CRF receptors, specifically mCRF2β (Ki = 13.5 nM) and rCRF2α (Ki = 21.7 nM), while demonstrating negligible affinity for hCRF1 (Ki >100 nM). Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion [1][2].
Stachybotramide is a natural fungal metabolite with the property of modulating the activity of cholesteryl ester transfer protein (CETP). Stachybotramide stimulates the transfer of cholesteryl esters (CE) from high-density lipoprotein (HDL) to very-low-density lipoprotein (VLDL) and low-density lipoprotein (LDL), increasing the transfer efficiency by 1.3- to 1.5-fold. Stachybotramide slightly reduced the transfer of cholesteryl esters from LDL and VLDL to HDL at 0.5 mM. The effect of Stachybotramide on the transfer of triglycerides (TG) from HDL was not significant. By these results, Stachybotramide was shown to preferentially stimulate the CETP-mediated transfer of cholesteryl esters from HDL to VLDL and LDL .
Anti-CD11a Antibody (AL-57) is a monoclonal antibody targeting human CD11a. Anti-CD11a Antibody (AL-57) binds to HA cells in a dose-dependent manner but did not bind to LA cells. Anti-CD11a Antibody (AL-57) preferentially binds to the active conformation of LFA-1 and blocks LFA-1-mediated adhesion and lymphocyte proliferation. Anti-CD11a Antibody (AL-57) can be used for the research of inflammatory and autoimmune diseases .
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms .
Urocortin III (human) TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) TFA preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) TFA potently binds to type 2 CRF receptors, specifically mCRF2β (Ki = 13.5 nM) and rCRF2α (Ki = 21.7 nM), while demonstrating negligible affinity for hCRF1 (Ki >100 nM). Urocortin III (human) TFA mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
Ro 09-1428 is a broad-spectrum parenteral cephalosporin. Ro 09-1428 has potent antibacterial activities against Pseudomonas aeruginosa and Acinetobacter caloaceticus, with MIC90s of 0.39 and 6.25 μg/mL, respectively, better than Ceftazidime (HY-B0593). Additionally, Ro 09-1428 shows high activity against Escherichia coli, Kkbsielia pneumoniae, Proteus mirabilis, P. aeruginosa, staphylococci, and more. Ro 09-1428 preferentially attacks PBP 3 for target in E. coli and P. aeruginosa, which is promising for research of septicemias and serious P. aeruginosa infections .
Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells.?I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50?of 1 μM .
Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression .
KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins .
E (c (RGDfK)) 2 is a αvβ3 integrin ligand and tumor-targeting agent. E (c (RGDfK)) 2 binds to αvβ3 integrin, mediates receptor-mediated endocytosis of conjugated payloads, and inhibits integrin-dependent cell adhesion to fibrinogen. E (c (RGDfK)) 2 inhibits the proliferation of cancer cells and endothelial cells. E (c (RGDfK)) 2 preferentially accumulates in orthotopic mouse breast tumors and human ovarian cancer xenograft tumors. E (c (RGDfK)) 2 can be used in research related to glioblastoma, lung cancer, breast adenocarcinoma and ovarian cancer .
PROTAC BET Degrader-16 (Compound A10) is a BETPROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia .
BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=10 μM) with higher affinity for BRDT-BD1 than BRD4-BD1. BRDT-IN-2 preferentially binds BRDT-BD1 without direct interaction with BRDT-BD1’s Arg54 residue. BRDT-IN-2 binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma .
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
cis-Lomibuvir (cis-VX-222) is the cis-isomer of Lomibuvir. Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis . cis-Lomibuvir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferentialNET/SERT inhibition with pIC50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions .
GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator.GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .
(S)-TROX-1 is the S-enantiomer of TROX-1 (HY-120751). TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer .
MRLB-223 is a preferentialHDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma .
SYBR Green I chloride is a highly sensitive fluorescent nucleic acid dye that binds specifically to the minor groove of double-stranded DNA or intercalates between base pairs. SYBR Green I chloride exhibits weak fluorescence in the unbound state but emits bright fluorescence upon binding, and it preferentially binds to large-fragment DNA and DNA with high G+C content. SYBR Green I chloride is suitable for real-time PCR technology; its fluorescence intensity correlates with the amount and size of amplification products, enabling accurate quantification of gene expression and discrimination of amplicons via melting curve analysis without additional post-processing. SYBR Green I chloride is widely used in preclinical in vitro nucleic acid detection .
YM-244769 hydrochloride (Standard) is the analytical standard of YM-244769 (hydrochloride) (HY-107659). This product is intended for research and analytical applications. YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia . .
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD) .
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
3-CPs is a monofunctional furanocoumarin and a photoprotective agent targeting Staphylococcus aureusDNA, possessesing anti-UVB lethal activity. 3-CPs competitively intercalates into DNA, forming exclusively 4',5'-furan-side mono-adducts upon UVB irradiation, and irreversibly inhibits the formation of cyclobutane pyrimidine dimers. 3-CPs prevents UVB-induced DNA damage by preferentially binding to strong (AT)n sites within the DNA, without inducing lethal interstrand DNA cross-links; the limited number of mono-adducts it induces can be efficiently repaired by bacteria. 3-CPs holds potential for use in the development of photoprotective formulations for skin diseases, as well as in studies investigating bacterial DNA photodamage repair mechanisms and the optimization of photochemotherapy safety .
PRAME peptide (425-433) acetate is a proteasome-degraded peptide derived from the cancer-testis antigen PRAME (Preferentially Expressed Antigen in Melanoma). PRAME peptide (425-433) acetate is restricted by HLA-A*02:01 and can serve as a target for bispecific T cell engager therapy in the context of major histocompatibility complex I presentation. PRAME peptide (425-433) acetate shows application potential in various malignant tumors and is widely suitable for research related to solid tumors, melanoma, ovarian cancer, endometrial cancer, and lung cancer (including lung adenocarcinoma and lung squamous cell carcinoma). PRAME peptide (425-433) acetate can be used to explore disease of triple-negative breast cancer, diffuse large B-cell lymphoma, and head and neck squamous cell carcinoma .
TMPyP tetrachloride is a DNA-binding agent, singlet oxygen Sensitizer and photobleaching agent. TMPyP tetrachloride binds to DNA via intercalation or external groove complexation; irradiation induces its photoinduced release from DNA. TMPyP tetrachloride sensitizes the generation of singlet molecular oxygen upon irradiation, and prolonged irradiation leads to photobleaching. TMPyP tetrachloride initially localizes preferentially in neuronal nuclei and cytoplasm, and irradiation triggers its subcellular relocalization. TMPyP tetrachloride binds to K + -free single-molecule G4-DNA nanowires via intercalation, and binds to K + -type variants via non-intercalation. TMPyP tetrachloride can be used in studies related to cancer, HIV infection and bacterial infection .
Edelfosine (ET-18-OCH3) is an orally active lipid raft modulator and apoptosis inducer that alters membrane fluidity and preferentially inserts into tumor cell membranes. Edelfosine recruits death receptor ligands (FasL/CD95L, TRAIL) and Bid to lipid rafts to form death-inducing signaling complexes, thereby initiating mitochondria-dependent apoptosis and inducing cytochrome c release. Edelfosine also exerts anti-inflammatory effects, promotes L-Selectin shedding, and causes no gastrointestinal or organ toxicity. In addition, Edelfosine inhibits nucleic acid and protein synthesis in Leishmania donovani and exhibits antiproliferative activity. Edelfosine can be used in research on multiple myeloma, inflammatory bowel diseases (such as ulcerative colitis and Crohn's disease), and visceral leishmaniasis .
Mocravimod (hydrochloride) is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod (hydrochloride) preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod (hydrochloride) significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod (hydrochloride) retains T cell effector function. Mocravimod (hydrochloride) can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI) .
PAP-1 (Standard) is the analytical standard of PAP-1. This product is intended for research and analytical applications. PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
Z-Leu-Arg-AMC is a fluorogenic peptide substrate for cysteine proteases (e.g., Cathepsin) (Ex=350 nm，Em=460 nm). Z-Leu-Arg-AMC is preferentially cleaved by Cathepsin K and S under weakly acidic conditions, while its hydrolysis relies on residual Cathepsin S activity at neutral pH. Z-Leu-Arg-AMC serves as a substrate for recombinant Sphenophorus levis Cathepsin L, falcipain-2, falcipain-3, berghepain-2, knowlepain-2, vivapain-2, as well as falcipain-2 chimeras and constructs. It enables quantitative detection of cysteine protease activity in human inflammatory bronchoalveolar lavage fluid via fluorescence generation. Z-Leu-Arg-AMC can be used in research related to pulmonary inflammatory diseases and malaria .
Mocravimod (KRP-203 free base) is a sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod retains T cell effector function. Mocravimod can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI) .
EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC50=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis .
SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC .
NAZ2329 (Standard) is the analytical standard of NAZ2329 (HY-103693). This product is intended for research and analytical applications. NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
AZM198 is an orally active myeloperoxidase (MPO) inhibitor. AZM198 irreversibly inactivates MPO (IC50=0.015 μM) via covalent binding to the heme prosthetic group, preferentially targets extracellular MPO activity, and reduces neutrophil extracellular trap formation, reactive oxygen species production and degranulation. AZM198 increases the fibrous cap thickness of atherosclerotic plaques, reduces lesion area, ameliorates hepatic steatosis and fibrosis in non-alcoholic steatohepatitis, and alleviates proteinuria and inflammatory infiltration associated with glomerulonephritis. AZM198 also decreases circulating levels of high-sensitivity Cardiac Troponin I and IL-1β, and mitigates endothelial cell injury. Therefore, AZM198 is suitable for research on various MPO-related diseases, including atherosclerotic cardiovascular disease, myocardial infarction, ischemic stroke, non-alcoholic steatohepatitis and crescentic glomerulonephritis .
Volrustomig (MEDI-5752) is a human IgG1 κ monoclonal antibody targeting CTLA4/PD1. The isotype control for Volrustomig is Human IgG1 kappa, Isotype Control (HY-P99001). Volrustomig anchors to the surface of T cells by binding PD-1, induces PD-1 internalization and degradation, and preferentially inhibits CTLA-4 on activated PD-1 + T cells. Volrustomig binds to tumor-infiltrating lymphocytes and a subset of PD-1 + B cells, enhances T cell function and IFNγ secretion. Volrustomig reduces the activation of non-tumor-infiltrating lymphocytes and exhibits manageable toxicity. Volrustomig can be used in research on various cancers, such as non-small cell lung cancer, gastric cancer, hepatobiliary cancer, and cervical cancer .
EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis .
DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)) .
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma . (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
Anti-Mouse CXCR4 Antibody is a monoclonal antibody that specifically recognizes murine CXCR4 (C-X-C chemokine receptor 4), also known as fusin or CD184. CXCR4 is a seven-transmembrane G protein–coupled receptor whose principal endogenous ligand is CXCL12 (stromal cell–derived factor-1α, SDF-1α) and is widely expressed in hematopoietic cells, endothelial cells, neurons, as well as embryonic and adult stem cells. The CXCR4–CXCL12 signaling axis activates multiple downstream pathways, including ERK1/2, Ras, p38 MAPK, PLC/MAPK, and SAPK/JNK, thereby regulating cell survival, proliferation, migration, and stemness maintenance. Aberrant overexpression of CXCR4 is closely associated with poor prognosis and metastasis in various cancers, with CXCR4-positive tumor cells preferentially home to CXCL12-rich tissues such as the liver, bone marrow, lung, and lymph nodes. Accordingly, CXCR4 and its CXCL12-related antagonists emerge as attractive targets for experimental anticancer therapy. Anti-Mouse CXCR4 Antibody is generated using a cell-based immunization and screening strategy and exhibits high affinity for both endogenous and exogenous murine CXCR4. Anti-Mouse CXCR4 Antibody can be used for thestudy of chronic lymphocytic leukemia and multiple myeloma .
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
Propidium monoazide is a cell-impermeant photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
SYBR Green I chloride is a highly sensitive fluorescent nucleic acid dye that binds specifically to the minor groove of double-stranded DNA or intercalates between base pairs. SYBR Green I chloride exhibits weak fluorescence in the unbound state but emits bright fluorescence upon binding, and it preferentially binds to large-fragment DNA and DNA with high G+C content. SYBR Green I chloride is suitable for real-time PCR technology; its fluorescence intensity correlates with the amount and size of amplification products, enabling accurate quantification of gene expression and discrimination of amplicons via melting curve analysis without additional post-processing. SYBR Green I chloride is widely used in preclinical in vitro nucleic acid detection .
BD-Oligo is an oligomer-specific fluorescent chemical probe. BD-Oligo preferentially identifies Aβ oligomer assemblies over monomers or fibrils by using diversity-directed fluorescent library (DOFL) screening and computational techniques. BD-Oligo exhibits dynamic oligomer monitoring capabilities during Aβ peptide fibril formation as Aβ is induced to form oligomers and ultimately fibrils over time. BD-Oligo also exhibits blood-brain barrier permeability with the ability to stain Aβ oligomers in vivo .
H-Gly-Arg-pNA hydrochloride (GR-pNA hydrochloride) is a colorimetric substrate for thrombin. H-Gly-Arg-pNA is preferentially bound by thrombin and cleaves the Gly-Arg (GR) peptide sequence, releasing p-nitroaniline (pNA) that can be detected colorimetrically at 405 nm. H-Gly-Arg-pNA hydrochloride is used as a fluorescent dye to measure thrombin activity .
Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Lyso BD-1, preferentially colocalized in lysosomes and lipid droplets, displays excellent photocytotoxicity (5.57 μM) on triple negative breast cancer cells under white light. Lyso BD-1 displays emission band at 560nm .
AG2 is a glucose uptake tracer and two-photon fluorescent probe. AG2 is taken up by cells via glucose-specific transport systems, rather than passive diffusion; it preferentially accumulates in cancer cells and colon cancer tissues compared with normal cells and tissues; it mainly localizes to mitochondria, with a small amount also distributed in the cytoplasm and cell membrane. AG2 can be used for colon cancer research .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
PPZ-A10 is an ionizable cationic lipid. PPZ-A10 preferentially delivers mRNA to liver and spleen immune cells. Pi-LNPs containing PPZ-A10 can effectively deliver mRNA/siRNA to solid tumors .
TMPyP tetrachloride is a DNA-binding agent, singlet oxygen Sensitizer and photobleaching agent. TMPyP tetrachloride binds to DNA via intercalation or external groove complexation; irradiation induces its photoinduced release from DNA. TMPyP tetrachloride sensitizes the generation of singlet molecular oxygen upon irradiation, and prolonged irradiation leads to photobleaching. TMPyP tetrachloride initially localizes preferentially in neuronal nuclei and cytoplasm, and irradiation triggers its subcellular relocalization. TMPyP tetrachloride binds to K + -free single-molecule G4-DNA nanowires via intercalation, and binds to K + -type variants via non-intercalation. TMPyP tetrachloride can be used in studies related to cancer, HIV infection and bacterial infection .
TTHA is an aminopolycarboxylic acid chelating agent with preferential affinity for lighter (lower atomic number) rare earth element (REE) ions. TTHA binds to REE ions through chelation as the primary coordination mechanism .
m-PEG20000-OH can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Nanoscale micelles can be prepared by using amphiphilic block copolymers to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Magainin 2 (Magainin II) is an antimicrobial peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
Muscle homing peptide M12 can preferentially bind to surface protein of muscle cells. Muscle homing peptide M12 mediates enhanced cellular uptake of nanoparticles (NPs) in myoblasts in vitro. Muscle homing peptide M12 is covalently conjugated to PLGA-PEG NPs via the N-terminal α-amino groups of peptides using the N-hydroxysuccinimide ester reaction .
E (c (RGDfK)) 2 is a αvβ3 integrin ligand and tumor-targeting agent. E (c (RGDfK)) 2 binds to αvβ3 integrin, mediates receptor-mediated endocytosis of conjugated payloads, and inhibits integrin-dependent cell adhesion to fibrinogen. E (c (RGDfK)) 2 inhibits the proliferation of cancer cells and endothelial cells. E (c (RGDfK)) 2 preferentially accumulates in orthotopic mouse breast tumors and human ovarian cancer xenograft tumors. E (c (RGDfK)) 2 can be used in research related to glioblastoma, lung cancer, breast adenocarcinoma and ovarian cancer .
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) potently binds to type 2 CRF receptors, specifically mCRF2β (Ki = 13.5 nM) and rCRF2α (Ki = 21.7 nM), while demonstrating negligible affinity for hCRF1 (Ki >100 nM). Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion [1][2].
DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species .
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
Urocortin III (human) TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) TFA preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) TFA potently binds to type 2 CRF receptors, specifically mCRF2β (Ki = 13.5 nM) and rCRF2α (Ki = 21.7 nM), while demonstrating negligible affinity for hCRF1 (Ki >100 nM). Urocortin III (human) TFA mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
RGD-targeted Proapoptotic Peptide is a peptide. The C-terminal RGD-4C peptide (ACDCRGDCFC) binds preferentially to integrins at sites of tumor angiogenesis.
PRAME peptide (425-433) is a peptide corresponding to amino acids 425-433 of PRAME (preferentially expressed antigen) in melanoma. PRAME peptide (425-433) can be used to stimulate human PRAME-specific CD8 + T cells .
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein .
CSK substrate is a specific substrate for C-terminal Src kinase (CSK), which binds CSK and downregulates the Src family members. CSK substrate preferentially phosphorylates certain amino acid residues that are distinct from the conserved Src C-terminal sequence .
β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
CLPVASC is a kidney-targeting cyclic peptide that preferentially distributes to kidney tissue, with utility to enhance kidney targeting of nanocarriers.CLPVASC preferentially distributes to the kidney when displayed on PEG-b-PPS micelles. CLPVASC can be used for the research of acute kidney injury .
MAF-10L is a membrane-disrupting agent, a cationic amphipathic Mastoparan AF derivative with enhanced α-helicity. MAF-10L preferentially interacts with DOPS lipids in cancer cell membranes, disrupting cancer cell membranes to trigger membrane leakage. MAF-10L can be used for the research of cancer .
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
PRAME peptide (425-433) acetate is a proteasome-degraded peptide derived from the cancer-testis antigen PRAME (Preferentially Expressed Antigen in Melanoma). PRAME peptide (425-433) acetate is restricted by HLA-A*02:01 and can serve as a target for bispecific T cell engager therapy in the context of major histocompatibility complex I presentation. PRAME peptide (425-433) acetate shows application potential in various malignant tumors and is widely suitable for research related to solid tumors, melanoma, ovarian cancer, endometrial cancer, and lung cancer (including lung adenocarcinoma and lung squamous cell carcinoma). PRAME peptide (425-433) acetate can be used to explore disease of triple-negative breast cancer, diffuse large B-cell lymphoma, and head and neck squamous cell carcinoma .
MCE Oil Red O Staining Kit for Cell Smears effectively stains lipid droplets of various sizes, including smaller lipid droplets, and preferentially adsorbs dye from the solvent. It is suitable for staining oil red O in cell smears, bone marrow smears, fluid smears, blood smears, and other samples. When using the kit, specimens should not be fixed with fixatives containing ethanol. If fixation is required, 10% formalin can be used. The positive staining result for fat typically appears orange-yellow to red, with the exact color varying depending on the lipid concentration.
MCE Weigert Elastin Staining Kit combines Weigert Resorcinol Fuchsin Staining Solution with Van Gieson (VG) Staining Solution. Weigert Resorcinol Fuchsin Solution is mainly used for staining elastic fibers, Van Gieson (VG) Solution is used for collagen fiber staining. The principle of VG staining is based on differences in the size of anionic dye molecules and the permeability of tissues. Picric acid (PA) has the smallest molecular weight and preferentially enters dense structures. Ponceau Red or acid fuchsin has a relatively larger molecular weight and primarily binds to collagen fibers, while light green has the largest molecular weight and stains other tissue components. After VG staining, collagen fibers appear red, while muscle fibers and cytoplasm appear yellow, enabling a clear distinction between tissue components.
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
Volrustomig (MEDI-5752) is a human IgG1 κ monoclonal antibody targeting CTLA4/PD1. The isotype control for Volrustomig is Human IgG1 kappa, Isotype Control (HY-P99001). Volrustomig anchors to the surface of T cells by binding PD-1, induces PD-1 internalization and degradation, and preferentially inhibits CTLA-4 on activated PD-1 + T cells. Volrustomig binds to tumor-infiltrating lymphocytes and a subset of PD-1 + B cells, enhances T cell function and IFNγ secretion. Volrustomig reduces the activation of non-tumor-infiltrating lymphocytes and exhibits manageable toxicity. Volrustomig can be used in research on various cancers, such as non-small cell lung cancer, gastric cancer, hepatobiliary cancer, and cervical cancer .
AO-176 is a humanized anti-CD47 IgG2 monoclonal antibody. AO-176 induces tumor phagocytosis through blocking the CD47-SIRPα interaction. AO-176 preferentially binds to tumor versus normal cells and directly kills tumor by a cell autonomous mechanism not ADCC (antibody-dependent cell-mediated cytotoxicity). AO-176 demonstrates dose-dependent antitumor activity in tumor xenograft models. AO-176 can be used for the researches of cancer, such as lymphoma .
Anti-PRAME Antibody is a monoclonal antibody that targets the melanoma antigen preferentially/PRAME. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-PRAME Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
MEDI-2228 Antibody is an anti-human BCMA antibody that preferentially binds to membrane-bound BCMA versus soluble BCMA. MEDI-2228 Antibody can generate antibody drug conjugate (ADC) (MEDI 2228) with a pyrrolobenzodiazepine (PBD) dimer. MEDI-2228 Antibody can be used for the study of multiple myeloma .
Rendomab B4 is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
ADI-14359 is an antibody that binds to RSV postF, with a KD value of 387 nM, and exhibits non-neutralizing activity. ADI-14359 binds to antigenic site I on RSV postF through interactions of its conserved CDR H3 motif, germline-encoded IGKV1-39 light chain residues and heavy chain residues, where the light chain mediates preferential binding to postF by conflicting with the rearranged preF region. ADI-14359 can be used in studies related to respiratory syncytial virus (RSV) infection .
Anti-CD11a Antibody (AL-57) is a monoclonal antibody targeting human CD11a. Anti-CD11a Antibody (AL-57) binds to HA cells in a dose-dependent manner but did not bind to LA cells. Anti-CD11a Antibody (AL-57) preferentially binds to the active conformation of LFA-1 and blocks LFA-1-mediated adhesion and lymphocyte proliferation. Anti-CD11a Antibody (AL-57) can be used for the research of inflammatory and autoimmune diseases .
Anti-Mouse CXCR4 Antibody is a monoclonal antibody that specifically recognizes murine CXCR4 (C-X-C chemokine receptor 4), also known as fusin or CD184. CXCR4 is a seven-transmembrane G protein–coupled receptor whose principal endogenous ligand is CXCL12 (stromal cell–derived factor-1α, SDF-1α) and is widely expressed in hematopoietic cells, endothelial cells, neurons, as well as embryonic and adult stem cells. The CXCR4–CXCL12 signaling axis activates multiple downstream pathways, including ERK1/2, Ras, p38 MAPK, PLC/MAPK, and SAPK/JNK, thereby regulating cell survival, proliferation, migration, and stemness maintenance. Aberrant overexpression of CXCR4 is closely associated with poor prognosis and metastasis in various cancers, with CXCR4-positive tumor cells preferentially home to CXCL12-rich tissues such as the liver, bone marrow, lung, and lymph nodes. Accordingly, CXCR4 and its CXCL12-related antagonists emerge as attractive targets for experimental anticancer therapy. Anti-Mouse CXCR4 Antibody is generated using a cell-based immunization and screening strategy and exhibits high affinity for both endogenous and exogenous murine CXCR4. Anti-Mouse CXCR4 Antibody can be used for thestudy of chronic lymphocytic leukemia and multiple myeloma .
Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Magainin 2 (Magainin II) is an antimicrobial peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis . D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors . D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor .
Chaetoglobosin A is a secondary metabolite and nematicide. Chaetoglobosin A is produced by Penicillium aquamarinium. Chaetoglobosin A targets Filamentous actin in cells, thereby inducing cell cycle arrest, and inhibiting membrane ruffle formation and cell migration. Chaetoglobosin A preferentially induces Apoptosis in chronic lymphocytic leukemia cells. Chaetoglobosin A induces dose- and time-dependent death in J2 larvae of the southern root-knot nematode (Meloidogyne incognita). Chaetoglobosin A can be used in studies related to root-knot nematode disease and chronic lymphocytic leukemia .
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
Glyco-3ß,5α,6ß -trihydroxycholanoic acid (NPCBA2) is a bile acid which accumulates preferentially in Niemann-Pick C (NPC) patients. Glyco-3ß,5α,6ß -trihydroxycholanoic acid is a biomarker for the early diagnosis of Niemann-Pick C disease .
Stachybotramide is a natural fungal metabolite with the property of modulating the activity of cholesteryl ester transfer protein (CETP). Stachybotramide stimulates the transfer of cholesteryl esters (CE) from high-density lipoprotein (HDL) to very-low-density lipoprotein (VLDL) and low-density lipoprotein (LDL), increasing the transfer efficiency by 1.3- to 1.5-fold. Stachybotramide slightly reduced the transfer of cholesteryl esters from LDL and VLDL to HDL at 0.5 mM. The effect of Stachybotramide on the transfer of triglycerides (TG) from HDL was not significant. By these results, Stachybotramide was shown to preferentially stimulate the CETP-mediated transfer of cholesteryl esters from HDL to VLDL and LDL .
APEG1 Isoform 3 potentially regulates the growth and differentiation of arterial smooth muscle cells. APEG1 Protein, Human (His) is the recombinant human-derived APEG1 protein, expressed by E. coli , with C-His labeled tag.
PRAME is located in the CRL2 E3 ubiquitin-protein ligase complex and directs ubiquitination and degradation, specifically targeting the truncated MSRB1/SEPX1 selenoprotein.It is recruited to active promoter regions and is involved in chromatin regulation.Melanoma antigen preferentially/PRAME, Human (His) is the recombinant human-derived Melanoma antigen preferentially/PRAME, expressed by E.coli , with N-6*His labeled tag.
Anabaseine-d4 is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
Mirogabalin- 13C2,d1 (Mixture of Diastereomers) is a 13C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain .
Propidium monoazide is a cell-impermeant photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
DSPE-PEG 2000-Mannose is a mannose-containing lipid. DSPE-PEG 2000-Mannose is used to prepare mannose-conjugated Liposome (Man-lipo) for siRNA delivery. Mannose-modified liposomes encapsulating IDO siRNA (Man-lipo-siIDO) preferentially knock down IDO expression in the draining lymph nodes and spleens of melanoma-bearing mice. Man-lipo-siIDO delays the onset time of melanoma and reduces tumor volume .
Edelfosine (ET-18-OCH3) is an orally active lipid raft modulator and apoptosis inducer that alters membrane fluidity and preferentially inserts into tumor cell membranes. Edelfosine recruits death receptor ligands (FasL/CD95L, TRAIL) and Bid to lipid rafts to form death-inducing signaling complexes, thereby initiating mitochondria-dependent apoptosis and inducing cytochrome c release. Edelfosine also exerts anti-inflammatory effects, promotes L-Selectin shedding, and causes no gastrointestinal or organ toxicity. In addition, Edelfosine inhibits nucleic acid and protein synthesis in Leishmania donovani and exhibits antiproliferative activity. Edelfosine can be used in research on multiple myeloma, inflammatory bowel diseases (such as ulcerative colitis and Crohn's disease), and visceral leishmaniasis .
PPZ-A10 is an ionizable cationic lipid. PPZ-A10 preferentially delivers mRNA to liver and spleen immune cells. Pi-LNPs containing PPZ-A10 can effectively deliver mRNA/siRNA to solid tumors .
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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