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NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo .
N-[4-(2-Benzimidazolyl)phenyl]maleimide is a potent fluorescent probe with excitation maximum of 315 nm and emission maximum of 360 nm. N-[4-(2-Benzimidazolyl)phenyl]maleimide can be used for fluorometry of thiol compounds .
Dnp-PLGLWA-DArg-NH2 TFA is a fluorogenic substrate for MMP-1 and MMP-9. Dnp-PLGLWA-DArg-NH2 TFA can be used to quantify the activity of MMPs (Ex=280 nm, Em=360 nm) .
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction .
Suc-Leu-Tyr-AMC is a fluorometric peptide substrate for µ-calpain and m-calpain. The excitation wavelength is 360 nm and the emission wavelength is 460 nm .
SGA360 suppress inflammatory SAA1 signaling in an AHR-dependent manner through a mechanism that does not require AHR binding to its cognate response element (partial antagonist) .
NPEC-caged-dopamine is a caged version of dopamine. NPEC-caged-Dopamine was used by applying focal photolysis with UV light (360 nm) to releases dopamine, which leads to D1 receptor activation .
Phenamacril (JS399-19) inhibits activity of myosin I non-competitively with an IC50 of 360 nM through suppression of the ATPase activity, exhibits therefore an antifungal efficacy towards Fusarium species .
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activated potassium channel. Noxiustoxin plays an important role in neuroinflammatory disease .
1,4-PBIT (1,4-PB-ITU) dihydrobromide (compound 46) is a potent nitric oxide synthases (NOS) inhibitor, with Ki values of 7.6 nM, 360 nM, and 16 nM for the inducible (iNOS), endothelial (eNOS), and neuronal (nNOS) isozymes, respectively .
Z-LRGG-AMC (Z-Leu-Arg-Gly-Gly-AMC) is a fluorescent substrate that hydrolyzes and releases free fluorescent 7-amino-4-methylcoumarin (AMC). Detection wavelength of AMC: Ex/Em=360/460 nm .
Mag-Fura-2 tetrapotassium is a UV excitable rational fluorescent Mg 2+/Ca 2+ indicator (Ex=334-360 nm, Em=510 nm). Mag-Fura-2 tetrapotassium can be used for the determination of Mg 2+ and Ca 2+ concentrations .
Sp-8-Br-cAMPS sodium is a cAMP analog, which performs a protein kinase A (PKA) activating activity with EC50 of 360 nM. Sp-8-Br-cAMPS sodium inhibits proliferation of T cells and the haemocyte non-self response in Lepidoptera larve .
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
Dnp-PYAYWMR is a peptide substrate that selectively targets MMP3. Dnp-PYAYWMR is cleaved by MMP3 to produce Dnp-PYA (nonfluorescent) and YWMR (fluorophore detectable at 360 nm). After incubation of MMP3 with Dnp-PYAYWMR for 2 h, MMP3 fluorescence intensity was measured. Ex/Em=328/350 nm .
Fluoflavine (ML-090) is a selective NOX1 inhibitor with an IC50 of 90 nM. Fluoflavine has >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50>10 μM). ML-090 has an IC50 of 360 nM in HEK293 cells .
UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
Antitumor agent-122 (Compound 5j) is an antitumor agent with good efficacy, limited toxicity and low resistance. Antitumor agent-122 has antiproliferative activity for MGC-803 cell, HepG2 cell, SKOV3 cell and T24 cell with IC50 values of 5.23 μM, 3.60 μM, 1.43 μM, 3.03 μM, respectively .
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research .
These compounds have strong hdac and hsp90 inhibitory activities. Compound 20 (HDAC ic50 = 194 nm; Hsp90 α < b> Ic50 = 153 nm) and compound 26 ((HDAC ic50= 360 nm; Hsp90 α < b> Ic50 = 77 nm) shows the strongest HDAC and HSP90 α Inhibitory activity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.
PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research .
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
SLC26A3-IN-2 is an orally active inhibitor of anion exchanger protein SLC26A3(IC50=360 nM). SLC26A3 belongs to solute carrier (SLC) proteins, and the SLC26 family. SLC26 family has broad anion specificity for chloride, bicarbonate, sulfate and oxalate. SLC26A3 down-regulates in adenoma, DRA, involves in in intestinal absorption of chloride and oxalate. The loss of SLC26A3 function mutations is associated with chloride-losing diarrhea .
Dnp-PLGLWA-DArg-NH2 TFA is a fluorogenic substrate for MMP-1 and MMP-9. Dnp-PLGLWA-DArg-NH2 TFA can be used to quantify the activity of MMPs (Ex=280 nm, Em=360 nm) .
Mag-Fura-2 tetrapotassium is a UV excitable rational fluorescent Mg 2+/Ca 2+ indicator (Ex=334-360 nm, Em=510 nm). Mag-Fura-2 tetrapotassium can be used for the determination of Mg 2+ and Ca 2+ concentrations .
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
Dnp-PLGLWA-DArg-NH2 TFA is a fluorogenic substrate for MMP-1 and MMP-9. Dnp-PLGLWA-DArg-NH2 TFA can be used to quantify the activity of MMPs (Ex=280 nm, Em=360 nm) .
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction .
Suc-Leu-Tyr-AMC is a fluorometric peptide substrate for µ-calpain and m-calpain. The excitation wavelength is 360 nm and the emission wavelength is 460 nm .
IRAK-4 Peptide substrate (IRAK-1 (360-380)) is a biological active peptide. (This is a substrate peptide for Interleukin-1 Receptor-Associated Kinase (IRAK) 4)
Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activated potassium channel. Noxiustoxin plays an important role in neuroinflammatory disease .
Z-LRGG-AMC (Z-Leu-Arg-Gly-Gly-AMC) is a fluorescent substrate that hydrolyzes and releases free fluorescent 7-amino-4-methylcoumarin (AMC). Detection wavelength of AMC: Ex/Em=360/460 nm .
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
Dnp-PYAYWMR is a peptide substrate that selectively targets MMP3. Dnp-PYAYWMR is cleaved by MMP3 to produce Dnp-PYA (nonfluorescent) and YWMR (fluorophore detectable at 360 nm). After incubation of MMP3 with Dnp-PYAYWMR for 2 h, MMP3 fluorescence intensity was measured. Ex/Em=328/350 nm .
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
IL-21R protein, a receptor for interleukin-21, forms a heterodimer with the common gamma subunit and associates with Janus kinase 1 (JAK1). These interactions are pivotal for transducing the cellular responses initiated by interleukin-21, regulating immune processes and inflammatory pathways. IL-21R Protein, Human (217a.a, HEK293, Fc) is the recombinant human-derived IL-21R protein, expressed by HEK293 , with C-hFc labeled tag. The total length of IL-21R Protein, Human (217a.a, HEK293, Fc) is 217 a.a., with molecular weight of 60-70 kDa.
IL-21R protein, a receptor for interleukin-21, forms a heterodimer with the common gamma subunit and associates with Janus kinase 1 (JAK1). These interactions are pivotal for transducing the cellular responses initiated by interleukin-21, regulating immune processes and inflammatory pathways. IL-21R Protein, Human (217a.a, HEK293, His) is the recombinant human-derived IL-21R protein, expressed by HEK293 , with C-6*His labeled tag. The total length of IL-21R Protein, Human (217a.a, HEK293, His) is 217 a.a., with molecular weight of 40-55 kDa.
The IL-21R protein is specifically designed for IL-21 and forms a heterodimeric complex with the common γ subunit, which is critical for signal transduction. This receptor complex promotes interaction with Janus kinase 1 (JAK1), initiating downstream signaling events in response to interleukin-21. IL-21R Protein, Mouse (217a.a, HEK293, His) is the recombinant mouse-derived IL-21R protein, expressed by HEK293 , with C-6*His labeled tag. The total length of IL-21R Protein, Mouse (217a.a, HEK293, His) is 217 a.a., with molecular weight of 34-38 kDa.
CHI3L1 Protein, a carbohydrate-binding lectin with a preference for chitin, participates in tissue remodeling and cellular adaptation to environmental changes. It is involved in Th2 inflammation, IL-13-induced inflammation, allergen sensitization, inflammatory cell apoptosis, dendritic cell accumulation, M2 macrophage differentiation, and pathogenic enteric bacteria invasion. In colonic epithelial cells, it activates the AKT1 signaling pathway, leading to IL8 production. It also enhances antibacterial responses in the lung and regulates hyperoxia-induced injury and inflammation. CHI3L1 exists as a monomer. CHI3L1 Protein, Mouse (360a.a, HEK293, His) is the recombinant mouse-derived CHI3L1 protein, expressed by HEK293 , with C-His labeled tag. The total length of CHI3L1 Protein, Mouse (360a.a, HEK293, His) is 360 a.a., with molecular weight of 42-50 kDa.
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