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SIK1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Sik1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Sik1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Utrophin activator-1 (compound 3) is an utrophin upregulator with an EC50 of 1.8 μM. Utrophin activator-1 can be used for Duchenne muscular dystrophy research [1].
KCNQ1activator-1 (compound 3) is a potent activator of KCNQ1 channel. KCNQ1activator-1 has the potential for the research of long QT syndrome (LQTS) [1].
Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1) [1].
RyRs activator 1 (compound 7f) is a potent activator of ryanodine receptors (RyRs). RyRs activator 1 at 0.5 mg/L displays 100% larvicidal activity. The larvicidal activity of RyRs activator 1 is 90% at 0.01 mg/L [1].
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment [1].
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail [1].
SIRT1activator 1(compound 3) is a derivative of marine compound xyloallenoide A isolated from the mangrove fungus Xylaria sp.SIRT1 activator 1 shows angiogenic activities in zebrafish. SIRT1activator 1 protects hEPC against AngII-induced senescence by increasing SIRT1 expression levels and balancing the AMPK/Akt signaling pathway [1].
SIRT3 activator 1 (Compound 5v) is a SIRT3 activator. SIRT3 activator 1 selectively elevates SIRT3 expression, leading to the upregulation of SOD2 and OPA1 expression, effectively preventing mitochondrial dysfunction, mitigating oxidative stress, and preserving cardiomyocyte viability. SIRT3 activator 1 can be used for research of cardiovascular diseases [1].
EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently [1].
Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist (EC50 ∼ 1 μM) with promising in vivo pharmacokinetic properties [1].
Caspase-3 activator 1 (compound 4b) is a Ru(III) metal complex that inhibits gastric tumor growth and metastasis. Caspase-3 activator 1 mediates caspase-3 cleavage, which in turn causes Caspase-3 to cleave gasdermin E (GSDME) to produce the GSDME-N terminus, causing gastric tumor cell membrane perforation. Caspase-3 activator 1 is capable of inducing pyroptosis and pyroptosis-induced immune responses and can be assembled with decitabine DCT (HY-A0004) into a 4b-DCT-Lip lipid delivery system [1].
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure [1].
GPR40 Activator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively [1].
Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability [1].
EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively [1].
SOS1activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS [1].
20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases [1].
Procaspase-3/6 activator 1 (compound 1541) is a highly specific and robust activator of executioner procaspases-3 and -6, with EC50 values of 2.4 ± 0.2 and 2.8 ± 0.3 μM, respectively. Procaspase-3/6 activator 1 does not activate procaspases-1 or -7 [1].
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor with an IC50 of 2.12 nM/1.40 nM/2.86 nM for SIK1, SIK2 and SIK3, respectively [1].
Nrf2/HO-1activator 1 (Compound 24) is a potent Nrf2/HO-1 activator, neuroprotective agent. Nrf2/HO-1activator 1 shows neuroprotective and antioxidant activities. Nrf2/HO-1activator 1 can be used in Parkinson's disease (PD) research [1].
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease [1].
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM [1].
YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively [1].
Nav1.1activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2,Nav1.5, and Nav1.6[1].
ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity [1] .
PI3K/Akt/CREB activator 1 (compound AE-18) is a potent, orally active PI3K/Akt/CREB activator. PI3K/Akt/CREB activator 1 promotes neuronal proliferation, induced differentiation of Neuro-2a cells into a neuron-like morphology, and accelerated the establishment of axon-dendrite polarization of primary hippocampal neurons through upregulating brain-derived neurotrophic factor via the PI3K/Akt/CREB pathway. PI3K/Akt/CREB activator 1 can be used in research of vascular dementia (VaD) [1].
YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM) [1].
AMPK-α1β1γ1activator 1 (M1) is an acyl glucuronide metabolite of Indole-3-carboxylic Acid-based AMPK activator. AMPK-α1β1γ1activator 1 can selectively activated human β1 isoforms with an EC50 value of 38.1nM. AMPK-α1β1γ1activator 1 can direct binding with human AMPK α1β1γ1 isoform. AMPK-α1β1γ1activator 1 can be used for the research of diabetic nephropathy [1].
GLPG3312 (Compound 28) is a selective pan-SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases [1].
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively [1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A) [1].
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potent ferroptosis regulator glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 increases GPX4 activity to 150% at 20 μM in the cell-free assay and 61 μM in cell extracts [1].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator .
Asteltoxin is an inhibitor for extracellular vesicles (EV), which exhibits inhibitory effects towards mitochondrial ATP synthase and mTORC1activation .
Oleoylcarnitine, the metabolite which accumulates through suppression of fatty acid β-oxidation, can enhance hepatocarcinogenesis via STAT3activation .
Safironil is an antifibrotic compound. Safironil is a competitive inhibitor of collagen protein synthesis. Safironil reduces liver fibrogenesis by inhibiting HSC activation .
ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κBactivation . Sinomenine also is an activator of μ-opioid receptor .
Methyl vanillate, one of the ingredients in Oryza sativa Linn., is a Wnt/β-catenin pathway activator . A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation .
Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPKactivation .
Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virusactivation .
Minumicrolin is a plant growth inhibitor. Minumicrolin can be isolated from Murraya paniculata. Minumicrolin inhibits Epstein-Barr virus early antigen (EBV-EA) activation .
VnP-16 can promote bone formation by accelerating osteoblast differentiation and activity through direct interaction with β1 integrin followed by FAKactivation .
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation .
INX-SM-56 is a cytotoxin that can be used for the synthesis of anti-VISTA antibody agent conjugate. VISTA: V-region Immunoglobulin-containing Suppressor of T cell Activation .
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κBactivation .
α-Toxicarol is a potent inhibitor of EBV.α-Toxicarol significantly inhibits mouse skin tumor in vivo. α-Toxicarol inhibits the TPA-induced EBV-EA activation .
Compound 48/80 (trimer) is a trimer of Compound 48/80 (HY-115768). Compound 48/80 is widely used in animal and tissue models as a "selective" mast cell activator .
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 .
Etilefrine (3-[2-(ethylamino)-1-hydroxyethyl]phenol) is an α adrenergic agonist . Etilefrine also is an AMPKactivator . Etilefrine can be used for the research of postural hypotension .
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζactivation .
Angiotensin amide ((Asn1,Val5)-Angiotensin II) is a potent vasoconstrictor. Angiotensin amide is a derivative of angiotensin II. Angiotensin amide can be used as a cardiac activator .
GKK1032B is an alkaloid compound that can be found in endophytic fungus Penicillium sp. GKK1032B can induce the apoptosis of human osteosarcoma MG63 cells through caspase pathwayactivation .
LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation .
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagyactivator .
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPRactivation .
Guaiacol (Standard) is the analytical standard of Guaiacol. This product is intended for research and analytical applications. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κBactivation . Anti-inflammatory activity [1].
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity [1]. Phortress free base leads to DNA damage and cell cycle arrest .
Tetrapeptide-30 is a skin-brightening peptide consisting of four amino acids. Tetrapeptide-30 can act as a tyrosinase inhibitor, lightening hyperpigmentation and evening out skin tone by reducing the amount of tyrosinase and inhibiting melanocyte activation .
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation .
Salicylic acid (Standard) is the analytical standard of Salicylic acid. This product is intended for research and analytical applications. Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation .
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspaseactivation .
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3activation .
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2Aactivator .
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1(NPC1L1) inhibitor, and is a potent Nrf2activator .
Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1(NPC1L1) inhibitor, and is a potent Nrf2activator .
Octanal-d4 is deuterated labeled Methyl vanillate (HY-75342). Methyl vanillate, one of the ingredients in Oryza sativa Linn., is a Wnt/β-catenin pathway activator . A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation .
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
CGP 53716 is a potent protein tyrosine kinase inhibitor. CGP 53716 has selective activity of platelet-derived growth factor (PDGF) receptor. CGP 53716 can be used in the study of disease induced by abnormal cell proliferation induced by PDGF receptor activation .
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation .
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPKactivation .
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a human monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKTactivation .
Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation . Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle .
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation .
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Quercetin GMP is Quercetin (HY-18085) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Quercetin is a flavonoid antioxidant, a PI3K inhibitor and a SIRT1Activator .
(±)5-HETE lactone is the racemate of 5-HETE lactone. 5-HETE lactone is a metabolite generated by a series of enzymatic reactions of arachidonic acid, and is also a substrate of paraoxonase-1 (PON1). 5-HETE lactone can be used in the study of B cell activation .
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation .
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κBactivation .
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC)activator . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38activation . SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
Tylvalosin (Acetylisovaleryltylo?sin) is an orally active, broad-spectrum macrolide antibiotic with antimicrobial activity. Tylvalosin is an antiviral agent used to study PRRSV infection. Tylvalosin induces apoptosis. Tylvalosin also has anti-inflammatory activity, alleviates oxidative stress, and alleviates acute lung injury by inhibiting NF-κB activation .
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of Thromboxane A2 (HY-113350) (TXA2) and acts as a potent TXA2 (TP) agonist. U-46619 also is a RhoA agonist. U-46619 stimulates the activation of RhoA through TXA2 receptor activation .
Tylvalosin (Acetylisovaleryltylosin) tartrate is an orally active, broad-spectrum macrolide antibiotic with antimicrobial activity. Tylvalosin tartrate is an antiviral agent useful in studying PRRSV infection. Tylvalosin tartrate induces apoptosis. Tylvalosin tartrate also has anti-inflammatory activity, relieves oxidative stress, and alleviates acute lung injury by inhibiting NF-κBactivation .
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) sodium, a potent bioactive phospholipid, is a LPA receptoractivator. 1-Oleoyl lysophosphatidic acid sodium can promote mitosis by inducing DNA synthesis. 1-Oleoyl lysophosphatidic acid sodium is also involved in normal and pathological emotional responses, including anxiety and depression [1] .
α-Conotoxin PeIA is an analgesic α-conotoxin.α-Conotoxin PeIA inhibits the α6β4, α9α10 and α3β2nAChR.α-Conotoxin PeIA is also a potent inhibitor of N-type calcium channel via GABAB receptor activation .
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7activation .
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1activation .
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated .
o-Vanillin (2-Vanillin) is a nature product, could be extracted from Vanilla planifolia, Pinus koraiensis fruit. o-Vanillin is a potent antifungal agent. o-Vanillin inhibits the growth of mycelia by disrupting the integrity of cell walls and cell membranes. o-Vanillin inhibits Doxorubicin (HY-15142A)- and 4-hydroperoxycyclophosphamide-induced NF-κB activation .
Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate(S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1activator .
Fenoprofen- 13C6 (sodium hydrate) is the 13C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].
ICy-Q is a quinone oxidoreductase 1 (NQO-1)-activated near-infrared (NIR) reagent which can react with NQO-1 to release the reduction product ICy-OH. ICy-OH selectively induces pancreatic cancer cell death through the pyroptosis pathway. ICy-Q can be used as an effective tool for rapid and accurate diagnosis of intraoperative pathological sections [1].
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation .
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation .1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity .
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosisactivator .
Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosisactivator .
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation . P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts .
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation .
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1activation .
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
Fingolimod (hydrochloride) (Standard) is the analytical standard of Fingolimod (hydrochloride). This product is intended for research and analytical applications. Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate(S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1activator .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation .
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagyactivator .
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation .
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagyactivator .
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epacactivator .
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation .
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Quercetin GMP is Quercetin (HY-18085) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Quercetin is a flavonoid antioxidant, a PI3K inhibitor and a SIRT1Activator .
Reteplase (BM 06.022) is a recombinant plasminogen activator, consists of the kringle 2 and protease domains of human tissue-type plasminogen activator .
Quercetin GMP is Quercetin (HY-18085) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Quercetin is a flavonoid antioxidant, a PI3K inhibitor and a SIRT1Activator .
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
VnP-16 can promote bone formation by accelerating osteoblast differentiation and activity through direct interaction with β1 integrin followed by FAKactivation .
Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca 2+ pump in liver plasma membranes independently of adenylate cyclase activation .
Angiotensin amide ((Asn1,Val5)-Angiotensin II) is a potent vasoconstrictor. Angiotensin amide is a derivative of angiotensin II. Angiotensin amide can be used as a cardiac activator .
Tetrapeptide-30 is a skin-brightening peptide consisting of four amino acids. Tetrapeptide-30 can act as a tyrosinase inhibitor, lightening hyperpigmentation and evening out skin tone by reducing the amount of tyrosinase and inhibiting melanocyte activation .
α-Conotoxin PeIA is an analgesic α-conotoxin.α-Conotoxin PeIA inhibits the α6β4, α9α10 and α3β2nAChR.α-Conotoxin PeIA is also a potent inhibitor of N-type calcium channel via GABAB receptor activation .
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
γ-Fibrinogen377-395 is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in mice in vivo. γ-Fibrinogen377-395 can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
γ-Fibrinogen377-395 TFA is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 TFA blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in mice in vivo. γ-Fibrinogen377-395 TFA can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation .
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a human monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKTactivation .
SIRT1activator 1(compound 3) is a derivative of marine compound xyloallenoide A isolated from the mangrove fungus Xylaria sp.SIRT1 activator 1 shows angiogenic activities in zebrafish. SIRT1activator 1 protects hEPC against AngII-induced senescence by increasing SIRT1 expression levels and balancing the AMPK/Akt signaling pathway [1].
Oleoylcarnitine, the metabolite which accumulates through suppression of fatty acid β-oxidation, can enhance hepatocarcinogenesis via STAT3activation .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κBactivation . Sinomenine also is an activator of μ-opioid receptor .
Methyl vanillate, one of the ingredients in Oryza sativa Linn., is a Wnt/β-catenin pathway activator . A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation .
Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPKactivation .
Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virusactivation .
Minumicrolin is a plant growth inhibitor. Minumicrolin can be isolated from Murraya paniculata. Minumicrolin inhibits Epstein-Barr virus early antigen (EBV-EA) activation .
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κBactivation .
α-Toxicarol is a potent inhibitor of EBV.α-Toxicarol significantly inhibits mouse skin tumor in vivo. α-Toxicarol inhibits the TPA-induced EBV-EA activation .
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζactivation .
GKK1032B is an alkaloid compound that can be found in endophytic fungus Penicillium sp. GKK1032B can induce the apoptosis of human osteosarcoma MG63 cells through caspase pathwayactivation .
Guaiacol (Standard) is the analytical standard of Guaiacol. This product is intended for research and analytical applications. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κBactivation . Anti-inflammatory activity [1].
Salicylic acid (Standard) is the analytical standard of Salicylic acid. This product is intended for research and analytical applications. Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation .
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspaseactivation .
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3activation .
Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation . Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle .
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation .
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC)activator . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation .
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation .
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
C11orf59; LAMTOR1; Late endosomal/lysosomal adaptor and MAPK and MTOR activator 1; Lipid raft adaptor protein p18; LTOR1_HUMAN; p18; p27Kip1-releasing factor from RhoA; p27RF-Rho; PDRO; PP7157; Protein associated with DRMs and endosomes; Ragulator complex protein LAMTOR1; ragulator complex protein PDRO; Ragulator1; RhoA activator C11orf59
The LAMTOR1 protein is an important component of the Ragulator complex and plays dual roles in amino acid sensing and mTORC1 activation. It acts as a guanine nucleotide exchange factor (GEF) for Rag GTPases and mediates their recruitment to the lysosomal membrane. LAMTOR1 Protein, Human (His) is the recombinant human-derived LAMTOR1 protein, expressed by E. coli , with N-His labeled tag. The total length of LAMTOR1 Protein, Human (His) is 160 a.a., with molecular weight of ~24 kDa.
The UBE2V1 protein does not have intrinsic ubiquitin ligase activity and can cooperate with UBE2N to synthesize non-canonical polyubiquitin chains linked through Lys-63. This type of polyubiquitination activates IKK and mediates NF-kappa-B activation, thereby affecting transcriptional activation, cell cycle progression, and DNA repair. UB2V1 Protein, Human (Sf9) is the recombinant human-derived UB2V1 protein, expressed by Sf9 insect cells , with tag free. The total length of UB2V1 Protein, Human (Sf9) is 146 a.a., .
The UBE2V1 protein does not have intrinsic ubiquitin ligase activity and can cooperate with UBE2N to synthesize non-canonical polyubiquitin chains linked through Lys-63. This type of polyubiquitination activates IKK and mediates NF-kappa-B activation, thereby affecting transcriptional activation, cell cycle progression, and DNA repair. UB2V1 Protein, Human (Sf9, His, Strep) is the recombinant human-derived UB2V1 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of UB2V1 Protein, Human (Sf9, His, Strep) is 146 a.a., .
The UBE2V1 protein does not have intrinsic ubiquitin ligase activity and can cooperate with UBE2N to synthesize non-canonical polyubiquitin chains linked through Lys-63. This type of polyubiquitination activates IKK and mediates NF-kappa-B activation, thereby affecting transcriptional activation, cell cycle progression, and DNA repair. UBE2V1 Protein, Human (His) is the recombinant human-derived UBE2V1 protein, expressed by E. coli , with C-6*His labeled tag. The total length of UBE2V1 Protein, Human (His) is 146 a.a., with molecular weight of ~17.0 kDa.
In the Hippo signaling pathway, MOB4A/MOB1B, a crucial activator, controls organ size and suppresses tumors by regulating proliferation and promoting apoptosis. This pathway involves a kinase cascade where STK3/MST2 and STK4/MST1, with the regulatory protein SAV1, activate LATS1/2. In partnership with its regulator MOB1B, LATS1/2 phosphorylates and inactivates YAP1 and WWTR1/TAZ, influencing gene expression. MOB4A/MOB1B stimulates STK38L and interacts with LATS1 and LATS2, contributing to the complex regulatory network within the Hippo signaling pathway. MOB4A/MOB1B Protein, Human (His) is the recombinant human-derived MOB4A/MOB1B protein, expressed by E. coli, with N-6*His labeled tag. The total length of MOB4A/MOB1B Protein, Human (His) is 216 a.a., with molecular weight of 43-48 kDa.
GCAP1 Proteinas, a pivotal regulator in the visual system, modulates retinal guanylyl cyclase activity based on intracellular calcium concentrations. Under low calcium, GCAP1 stimulates retinal guanylyl cyclase for dark state recovery in rod photoreceptors. Elevated calcium inhibits guanylyl cyclase activity, a crucial aspect of rod photoreceptor phototransduction. Additionally, GCAP1 may contribute to light response and recovery in cone photoreceptors under bright light. The protein's homodimeric structure enhances its regulatory capabilities in the visual signaling pathway. GCAP1 Protein, Human (sf9) is the recombinant human-derived GCAP1 protein, expressed by Sf9 insect cells , with tag free. and with residual Gly-Pro in N-terminal (not related to functional changes) mutation. The total length of GCAP1 Protein, Human (sf9) is 201 a.a., with molecular weight of ~20 kDa.
The GCAP1 protein is a key regulator in the visual system, regulating retinal guanylyl cyclase activity in response to intracellular calcium concentration. Under low calcium conditions, GCAP1 stimulates retinal guanylyl cyclase to return rod photoreceptors to the dark state. GCAP1 Protein, Human (sf9, His-GST) is the recombinant human-derived GCAP1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of GCAP1 Protein, Human (sf9, His-GST) is 201 a.a., with molecular weight of ~42 kDa.
In the Hippo signaling pathway, MOB1A serves as a vital activator, governing organ size and suppressing tumors by modulating proliferation and apoptosis. Acting in a kinase cascade, MOB1A, along with STK3/MST2 and STK4/MST1, phosphorylates and activates LATS1/2, influencing the YAP1 oncoprotein and WWTR1/TAZ. This orchestrated phosphorylation controls gene expression pivotal for cell processes. Additionally, MOB1A stimulates STK38 and STK38L kinase activity, cooperating with STK3/MST2 and forming intricate interactions with key pathway components, contributing to its complex regulatory network. MOB1A Protein, Human (His) is the recombinant human-derived MOB1A protein, expressed by E. coli, with C-6*His labeled tag. The total length of MOB1A Protein, Human (His) is 215 a.a., with molecular weight of ~29.0 kDa.
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
Octanal-d4 is deuterated labeled Methyl vanillate (HY-75342). Methyl vanillate, one of the ingredients in Oryza sativa Linn., is a Wnt/β-catenin pathway activator . A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
Fenoprofen- 13C6 (sodium hydrate) is the 13C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].