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α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death.
Cefpiramide (SM-1652) free acid is a semisynthetic cephalosporin with broad-spectrum antibacterial activity. Cefpiramide free acid shows strong antibacterial effect on both gram-positive bacteria and gram-negative bacteria. Cefpiramide free acid is moderately susceptible to β-lactamase.
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways.
AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base effectively prevents kidney injury.
YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes.
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2.
Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents.
NSC363998 (free base) is an orally active compound. NSC363998 (free base) can suppress rCGG90 induced neurotoxicity. NSC363998 (free base) can be used for the research of neurodegenerative disorder such as Fragile X associated tremor/ataxia syndrome (FXTAS).
JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
FD-1080 free acid is a fluorophore with both excitation and emission in the NIR-II region (Ex=1064 nm, Em=1080 nm). FD-1080 free acid can be used for in vivo imaging.
GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis.
AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity.
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.
CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions.
Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo.
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease.
BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL).
GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and drugs.
PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.
Aviglycine (ABG-3168 free base) is an inhibitor of ethylene biosynthesis. Aviglycine (ABG-3168 (free base)) application delays natural flowering in pineapple.
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKB of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache.
GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
AS2034178 free base, a specific and orally active GPR40 agonist, exhibits glucose-dependent insulin secretion enhancement. AS2034178 free base has potential for type 2 diabetes mellitus research.
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.
AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism.
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs.
Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death.
NCGC00138783 free base is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 free base directly blocks the interaction between CD47 and SIRPα axis.
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity。
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with high affinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit.
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
ERK-IN-2 free base is a ERK2 inhibitor with an IC50 value of 1.8 nM. ERK-IN-2 free base might lead to off-target toxicity and/or off-target activity at dose >10 μM.
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.
Andolast (CR 2039) (free base) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma.
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
TT-OAD2 free base is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC50 of 5 nM. TT-OAD2 free base has the potential for diabetes treatment.
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases.
SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity.
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
Imanixil (HOE-402 free base) is an inducer of the LDL receptor (LDLR). Imanixil (HOE-402 free base) is also a potent cholesterol-lowering compound, which inhibits very low density-lipoprotein (VLDL) production, and consequently attenuates atherosclerosis development.
MK-0941 free base is an orally active glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes.
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex. CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents.
Ganfeborole (GSK656 free base) is a potent, selective and orally active inhibitor of M. tuberculosisleucyl-tRNA synthetase, with an IC50 of 0.20 μM. Ganfeborole can be used for the research of tuberculosis.
Avibactam (NXL-104) free acid is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
FOY 251 free base, an anti-proteolytic active metabolite of Camostate (HY-13512), acts as a proteinase inhibitor. FOY 25 free base inhibits SARS-CoV-2 infection in cells assay.
ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine.
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs.
NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
3'-O-Methylorobol, an antioxidant flavonoid, exhibits moderate antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay.
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.
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent.
AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations.
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.
IGUANA-1 free base (STL5-T-0057) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. IGUANA-1 free base inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. IGUANA-1 free base can be used for the research of cancer.
Dianemycin (Nanchangmycin free acid), a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E.
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS.
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
FFA3 agonist 1 is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3.
Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models.
Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
FR183998 free base is a potent Na +/H +-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.
Fosinopril (SQ28555 free acid) is the ester prodrug of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM.
Fexapotide (NX-1207 free acid) induces apoptosis selectively, reducing prostate volume at a cellular level. Fexapotide can be used in lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH) research.
Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.
Dazostinag (TAK-676 free base) is an agonist of stimulator of interferon genes (STING) protein with antineoplastic activity. Dazostinag can serve as a playload to synthesis Antibody-Drug Conjugates (ADCs).
Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
D-Isofloridoside, one of the polysaccharide precursors, has the activity of scavenging free radicals, inhibiting ROS expression, and inhibiting MMP-2 and MMP-9.
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma.
Antioxidant agent-7 (SD-7) is a benzodiazepine derivative with antioxidant activity with an IC50 value of 470 nM to scavenge DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical.
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor.
Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity.
Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum. Halofantrine blocks HERG potassium channels.
β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active. β-Aminoarteether can be used for inflammation and autoimmune disease research, such as lupus diseases.
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation.
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
Pexiganan (MSI 78 free base) is a synthetic analog of magainin 2. Pexiganan is a potent and orally active broad-spectrum antimicrobial peptide. Pexiganan can be used in the research of infections, such as diabetic foot ulcer infections.
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9 and MMP-13, respectively.
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
Fomivirsen (ISIS-2922 free base) is an antisense 21 mer phosphorothioate oligonucleotide. Fomivirsen is an antiviral agent that is used cytomegalovirus retinitis (CMV) research, incluiding in AIDs. Fomivirsen binds to and degrades the mRNAs encoding CMV immediate-early 2 protein, thus inhibiting virus proliferation.
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
Suc-AAPF-pNA (Suc-Ala-Ala-Pro-Phe-pNA) is a chromogenic p-nitroanilide (pNA) substrate with the Km of 1.7 mM. Suc-AAPF-pNA can be used for the Measurement of free and membrane-bound cathepsin G in human neutrophils.
Apraclonidine (ALO 2145 (free base)), a selective α2 and weak α1 receptor agonist activity, effectively low intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution.
Pentifylline is a vasodilator. Pentifylline inhibits platelet aggregation and thromboxane A2 synthesis, decrease the release of free radicals. Pentifylline has the potential for the research of acute ischaemic stroke.
Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength.
Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes.
Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
Valnivudine (FV-100 free base), a prodrug of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo.
Articaine (Hoe-045 free base) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway.
Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II.
Abetimus (LJP 394 free base) is an immunosuppressant consisting of four double-stranded DNA (dsDNA) oligonucleotides. Abetimus is capable of crosslinking anti-dsDNA antibodies on the surface of B cells, and decreases anti-dsDNA antibodies levels. Abetimus has the potential for research of systemic lupus erythematosus.
Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
Astodrimer (SPL7013 free base) is a large (3-4 nm, ~ 16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties.
Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research.
BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease.
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori.
(±)-Lisofylline ((±)-Lisophylline) is the racemate of Lisofylline. Lisofylline inhibits the generation of phosphatidic acid and free fatty acids. Lisofylline also blocks the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline can be used for Type 1 diabetes research.
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells.
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively.
Riviciclib shows antitumor activity on cisplatin-resistant cells.
Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
Sumatriptan (GR 43175 free base) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research.
Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4 + T cells and CD11b + macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM.
5,5'-Difluoro BAPTA is a difluoro-derivative of BAPTA (HY-100168). 5,5'-Difluoro BAPTA is the most widely used probe for studying cytosolic freeCa 2+ by 19F NMR. 5,5'-Difluoro BAPTA has high selectivity for Ca 2+. 5,5'-Difluoro BAPTA can inhibit the growth of pollen tube.
Alogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes[1][2][3].
(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2.
NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.
Temafloxacin (TMFX) is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin is well tolerated in lower respiratory and genitourinary tract infections.
2'-Acetylacteoside is a phenylethanoid glycoside isolated from Brandisia hancei, inhibits free radical-induced hemolysis of red blood cells and exhibits free radical scavenging activity.
Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes.
Ceftaroline fosamil (TAK-599) inner salt, a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil inner salt can be used for the research of MRSA infection.
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory.
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP2 receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma.
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
Sugammadex is a synthetic γ-cyclodextrin derivative, and acts as a reversal agent for neuromuscular block. Sugammadex shows nephroprotective effect in ischemia-reperfusion injury.
Recoflavone is a synthetic derivative of eupatilin that has a protective effect on gastric mucosa. Recoflavone has the potential to be used to treat peptic ulcer disease.
Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'.
Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively.
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research.
Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.
Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer.
Bifemelane is a nootropic compound. Bifemelan causes the first peak by stimulating release from intracellular Ca 2+ stores and the second by capacitive entry through store–operated Ca 2+ channels. Bifemelane will be provided as a pharmacological tool for basic studies on astrocytes.
Cefcapene pivoxil is an orally active cephalosporin antibiotic. It is a precursor agent that dissociates into free acid and then exerts antibacterial effect.
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Pirmenol is an orally active antiarrhythmic agent. Pirmenol inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol can be used in the research of cardiovascular disease, such as atrial fibrillation.
Tirilazad is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad has antiviral activities against nCoV. Tirilazad is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research.
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.
MK-447 is a free radical scavenger, also a nonsteroidal antiinflammatory agent, and enhances the formation of the endoperoxide, PGH2, and other prostaglandins.
Octadecanedioic acid, an endogenous metabolite, is a long-chain dicarboxylic acid that has been found in serum free fatty acid profile in Reye syndrome.
Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
Quinclorac, an herbicide widely applied in agriculture, induces oxidative stress due to free radical generation and changes in the antioxidant defense system.
Pyrimethanil-d5 is the deuterium labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 µM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 µM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects.
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-freeIC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.
Pyrogallol is a polyphenol compound, which has anti-fungal and anti-psoriatic properties. Pyrogallol is a reductant that is able to generate free radicals, in particular superoxide anions.
MTSEA hydrobromide is a sulfhydryl-reactive compound that modifies free cysteine residues to produce a positively charged side chain approximately the size of lysine.
Beloranib is a fumagillin-class methionine aminopetidase-2 (MetAP2) inhibitor. Beloranib decreases food intake, body weight, fat mass, and the size of adipocytes.
Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research.
Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
Barnidipine (Mepirodipine) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
Erigeroside is as a derivatives of -glucose extracted from Satureja khuzistanica Jamzad. Erigeroside has good ability of anti-oxidation and scavenging oxidation free radical.
Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model.
Urolignoside is an antioxidant with free radical scavenging activity. Urolignoside potently scavenges DPPH radical, and exhibits antioxidant to β-carotene-lineoleate model.
Bacopaside I, a saponin isolated from Bacopa monnieri, exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.
Senecionine acetate (O-Acetylsenecionine) is a pyrrolizidine alkaloid. Senecionine acetate inhibits the sequestration of Ca 2+ in extramitochondrial and mitochondrial compartments possibly by inactivating free sulfhydryl groups.
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
Cy5 DBCO chloride is an azide reaction probe and the addition of DBCO molecules allows the imaging of azide-labelled biomolecules by a copper-free “Click Chemistry” reaction.
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40)(Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
4-Hydroxyestrone- 13C6 is a 13C-labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Cyanine3 DBCO (Cy3-DBCO) hexafluorophosphate is a azide reactive probe, for imaging azide-labeled biomolecules via a copper-free "click-through" reaction.
Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity.
Cephaeline is a phenolic alkaloid in Indian Ipecac roots. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections.
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function.
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
L-Ornithine-d6 (hydrochloride) is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
L-Ornithine-d7 (hydrochloride) is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
L-Ornithine-d2 (hydrochloride) is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
Boc-L-Ala-OH-3- 13C is a 13C-labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
DBCO-NHS ester 2 is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 2 is a derivative of Dibenzylcyclooctyne (DBCO) used in copper-free click chemistry.
Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective.
1,3-Oxazolidine-2-thione, a free oxazolidinethione, increases thyroid size and severely depresses hepatic trimethylamine oxidase activity in the brown-egg layers.
D(+)-Galactosamine- 13C (hydrochloride) is the 13C labeled D(+)-Galactosamine hydrochloride. D(+)-Galactosamine (D-Galactosamine) hydrochloride, which is an established experimental toxin, primarily causes liver injury by the generation of free radicals and
Polyporusterone B is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone B has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
Norbornene-methyl-NHS is a click chemistry reagent containing a TCO group. Dienophile for conjugation via Diels-Alder-reaction, i.e. copper-free click reaction with tetrazines.
Bz-(Me)Tz-NHS is a click chemistry reagent containing an methyltetrazine group. Bz-(Me)Tz-NHS is 3rd generation Click-Linker for Cu-free click conjugation.
TPT-260 Dihydrochloride (NSC55712) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.
Polydeoxyadenylic-thymidylic acid sodium is a synthetic DNA polymer. Polydeoxyadenylic-thymidylic acid sodium can be used to determine the activity of bound and free ribonucleic acid polymerase. Polydeoxyadenylic-thymidylic acid sodium can be used for the research of cancer and virus infection.
L-Ornithine- 15N2 (hydrochloride) is the 15N-labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids.
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
MitoTracker Green FM is a green-fluorescent dye that can selectively accumulate in the mitochondrial matrix. MitoTracker Green FM covalently binds to mitochondrial proteins by reacting with free thiol groups of cysteine residues.
KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases.
Odatroltide, as a nanoscale P-selectin inhibitor, is a nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus.
8-hydroxybergapten is O-methylated by cell-free extracts of Ruta cells to isopimpinellin, in reactions mediated by discrete O-methyltransferases. 8-hydroxybergapten has excellent anti-wrinkle effect.
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
Disufenton sodium (NXY-059) is the disulfonyl derivative of the neuroprotective spin trap phenylbutynitrone(PBN), both NXY-059, its parent PBN and their hydrolysis/oxidation product MNT are very powerful scavengers of free radicals.
TPT-260(TPU260) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.
(Me)Tz-butanoic acid is a click chemistry reagent containing an azide. (Me)Tz-butanoic acid is tetrazine linker for conjugation via Diels-Alder-reaction, i.e. copper-free Click reaction with dienophiles.
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
H-L-Lys(Norbornene-methoxycarbonyl)-OH, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH can be used for the mild and selective modification of proteins in a copper-free click reaction.
L-Ornithine-1,2- 13C2 (hydrochloride) is the 13C-labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
3-Mercapto-3-methylbutan-1-ol-d6 is the deuterium labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Desmethyl Erlotinib-d4 is the deuterium labeled Desmethyl Erlotinib. Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor[1][2].
Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox stimulates leptin releas, inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity.
H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride can be used for the mild and selective modification of proteins in a copper-free click reaction.
CalFluor 488 Azide is a water-soluble fluorogenic azide probe. CalFluor 488 Azide is activated by Cu-catalyzed or metal-free click reaction. CalFluor 488 Azide is not fluorescent until it is reacted with alkynes.
Trimethobenzamide-d6 is deuterium labeled Trimethobenzamide. Trimethobenzamide is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
5-IAF (5-Iodoacetamidofluorescein) is an idoacetamide derivate of fluoresceine. 5-IAF can be used as fluorescent probe that labels proteins and other molecules having free thiols (cysteine side chains).
Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
L-Glutathione reduced- 13C2, 15N is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
Lauric acid- 13C is the 13C labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Fmoc-Tyr(tBu)-OH- 13C9, 15N is a 15N-labeled and 13C-labled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Lauric acid-d5 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Lauric acid-d33 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Lauric acid-d2 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Lauric acid-d233 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Rehmannic acid (lantadene A) is a compound isolated from Lantana camara. Rehmannic acid shows considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner. Rehmannic acid is a promising candidate for use as an antioxidant and hepatoprotective agent.
3-Nitro-L-tyrosine-d3 is the deuterium labeled 3-Nitro-L-tyrosine. 3-Nitro-L-tyrosine is a biomarker of nitrogen free radical species modified proteins in systemic autoimmunogenic conditions[1][2].
Biotin-4-aminophenol is a biotin-phenol analog. Biotin-4-aminophenol generates free radicals and conjugates to tyrosine residues in proteins more efficiently and selectively than the previously reported BP1.
Donepezil-d7 (hydrochloride) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
CYPMPO is a spin-trapping reagent. CYPMPO, a cyclic DEPMPO-type nitrone, is evaluated for spin-trapping capabilities toward hydroxyl and superoxide radicals. anti-oxidant and anti-tumor activity.
Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities. Anticancer activities.
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin II inhibits cell-free protein synthesis, releases adenine from rat liver ribosomes and from DNA, and has no RNase activity.
L-Ornithine-1,2,3,4,5- 13C5 (hydrochloride) is the 13C-labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
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].
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics.
Fmoc-L-Dap(Poc)-OH is a click chemistry reagent containing an azide group. Amino acid building block suitable for side chain Click conjugation with standard protocols and together with tetrazine linkers in copper-free Click conjugation (Diels-Alder).
(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC50 value of 7.49 μM (A549 cells).
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
o-Hydroxybenzylamine (2-HOBA) a selective dicarbonyl scavenger, is an antioxidant and scavanger of free radicals and isolevuglandins (IsoLGs). o-Hydroxybenzylamine can be used in the research of inflammation and cardiovascular disease, such as atherosclerosis, early recurrence of atrial fibrillation (AF) and arrhythmias.
Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor. Dexfadrostat also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..
Bendamustine-d4 is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Lauric acid- 13C-1 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively[1].
Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.
(-)-Isopulegol is prepared directly from the treatment of essential oil of citronella under solid supported acid catalysis and solvent-free microwave assisted ene-cyclisation. (-)-Isopulegol shows high activity in reacting with carbonyl compounds. (-)-Isopulegol can be used for antiviral activity research.
Gallic acid (3,4,5-Trihydroxybenzoic acid) hydrate is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid hydrate has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.
GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption.
GSK2795039 reduces apoptosis.
Acridone-4-carboxylic acid (ACA) (Compound 2c) is a heme-interacting acridone derivatives that prevents free heme-mediated protein oxidation and degradation. Acridone-4-carboxylic acid inhibits protein carbonyl formation with an IC50 of 43 μM.
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
Calcium Orange AM is an intracellular calcium reporter. Specific fluorescence can be detected when free calcium binds to Calcium Orange AM (Ex/Em=549/576 nm). Calcium Orange AM does not enter the vacuoles and does not compartmentalize into acidic vesicles.
ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120.
Cu (II) Protoporphyrin IX is used as a negative control for Zn (II) Protoporphyrin (an inihibitor of heme oxygenase). Heme oxygenase has been implicated in tumor cell resistance to chemotherapy, reduction of free radical formation and inflammation, and associated with vascular repair.
Ombuoside is a glycoside ombuoside isolated from Gynostemma pentaphyllum.Ombuoside has antimicrobial activity against several strains of gram-positive and gram-negative bacteria and the yeast Candida albicans. Ombuoside has antioxidant effects by scavenging free radicals and ROS.
5,5'-Difluoro BAPTA tetrapotassium is a difluoro-derivative of BAPTA (HY-100168). 5,5'-Difluoro BAPTA tetrapotassium shows large 19F NMR chemical shifts upon chelating divalent cations. 5,5'-Difluoro BAPTA tetrapotassium has high selectivity for Ca 2+. 5,5'-Difluoro BAPTA tetrapotassium can inhibit the growth of pollen tube.
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
Dual photoCORM 1 (compound 5) is metal-free, photochemically active dual CORM. Dual photoCORM 1 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach in cancerous B16F10 cells.
Hadogenes Bicolor Venom is a venom that can be obtained from Hadogenes Bicolor (South African flat rock scorpion). Scorpion venoms are Complex mixtures of peptides, enzymes, mucoproteins, free amino acids, nucleotides, lipids, amines, heterocyclic components, inorganic salts, etc.
Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema.
Cholesterol esterase is an enzyme that hydrolyzes cholesterol ester to cholesterol and free fatty acid in the intestinal lumen. Cholesterol synthesized in the acinar cells and is stored in zymogen granules. Cholesterol esterase is also known as bile salt-stimulated lipase and carboxy ester lipasea, acts function for acceleration of cholesterol absorption.
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.
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
Edoxaban impurity 4 is an impurity of Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention.
Phenazine methylsulfate is a free radical generator. Phenazine methylsulfate has been used as an electron transfer reactant in cell viability assays. Phenazine methylsulfate induces ssDNA break formation in the presence of the reducing agent NADPH. Phenazine methylsulfate induces oxidative DNA damage in an alkaline comet assay and apoptosis.
Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is a potent free radical scavenger. Eriodictyol-7-O-glucoside is also an Nrf2 activator, confers protection against Cisplatin-induced toxicity.
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with IC50 of 117 nM. AR420626 inhibits nicotine and serotonin-induced changes in motility of isolated muscle strips from rat colon and suppresses serotonin-induced fecal output in rats.
FWM-1 is a potent SARS-COV-2 NSP13 helicase enzyme inhibitor with binding free energy equals -328.6 kcal/mol. FWM-1 effectively disrupts the binding of ATP to the SARS-COV2 helicase enzyme.
Cy5.5 DBCO is a click chemistry reagent containing an cycloalkynes group. Cy5.5 DBCO is a linker of Cyanine5.5 fluorophore. DBCO group enables copper free biocompatible click chemistry with fast reaction kinetics and good stability.
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
BM635 mesylate is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 mesylate has a MIC50 of 0.6 μM against M. tuberculosis H37Rv. BM635 mesylate significantly improves the bioavailability compared to free-base BM635.
AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6
.
Sodium 2-oxopropanoate- 13C3 is the 13C-labeled Sodium 2-oxopropanoate. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[1][2].
HTHQ (1-O-hexyl-2,3,5-trimethylhydroquinone) is a potent lipophilic phenolic antioxidant. HTHQ has considerable anti-oxidative activity by directly reacting with reactive oxygen species (ROS) and scavenging ROS to form more stable free radicals.
Carboxypeptidase B is a peptide exonuclease that can specifically degrade peptide chains. Carboxypeptidase B is progressively degraded from the C-terminal to release free amino acids. Carboxypeptidase B hydrolyzes only peptide bonds with basic amino acids (such as arginine and lysine) as C-terminal residues.
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
Calcium Green-5N AM is a novel Ca 2+-sensitive fluorescent probe. Calcium Green-5N AM shows enhancement in fluorescence intensity on binding Ca 2+, and can monitor free Ca 2+ in neurons.
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
BM635 hydrochloride is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 hydrochloride has an MIC50 of 0.08 μM against M.tuberculosis H37Rv. BM635 hydrochloride doubles the in vivo exposure with respect to the free base BM635.
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
Isoarjunolic acid (2α,3α,23-Trihydroxyolean-12-en-28-oic acid) is a triterpenoid, can be isolated from the stems of Cornus kousa. Isoarjunolic acid could have free radical scavenging activity and elastase inhibition activity .
5-Dodecanoylaminofluorescein, a lipophilic fluorescent probe, is a free-fatty-acid conjugate of fluorescein. 5-Dodecanoylaminofluorescein has been used in membrane fluidity studies and the determination of critical micelle concentration of detergents. 5-Dodecanoylaminofluorescein can be also used to synthesize hydrophobic nanospheres for drug delivery.
Taurine-d4 is the deuterium labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Emapalumab (NI-0501) is a humanized monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH).
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
Yeast extract is a concentrate of the soluble part of yeast, especially Saccharomyces cerevisiae. The main nutritional components of yeast extract include partly hydrolyzed protein with 35-40% of free amino acid, and it also contain B vitamins and some trace elements. Yeast extract can be used as nutrients for bacterial culture media.
5-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
Methacrylic anhydride is a typical polymerizable 1,6-diolefin. Methacrylic anhydride can form a soluble csyclopolymer by free-radical initiation. Methacrylic anhydride can spontaneously polymerize through the vinyl group and justifies the use of 2-6-di-tert-butyl4-methylphenol as an inhibitor.
Taurine- 13C2 is the 13C-labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase.
Atherosperminine（Atherospermine）is a nature occurring alkaloid, has antiplasmodial activities in vitro, with an IC50 of 5.80 μM. Atherosperminine is a good reductant with the ability to chelate metals. Atherosperminine has scavenging activity towards the free radical DPPH, with an IC50 of 29.56 µg/mL. Atherosperminine exerts a non-specific relaxant effect on the trachealis.
5(6)-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Cyanine3.5 carboxylic acid chloride is an anthocyanin dye. Cyanine3.5 carboxylic acid chloride is Cyanine3.5 free unactivated monofunctional carboxylic acid and can be used as a reference or control for non-reactive dye. Cyanine3.5 also is an analog of Cy3.5 fluorophore.
6-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid.
BDP 581/591 carboxylic acid is a fluorescent dye (Ex=585 nm, Em=594 nm). BDP 581/591 carboxylic acid has a free carboxylic acid group, which can be catalyzed by a catalyst (such as EDC or HATU) to react with primary amines to form stable amide bonds. BDP 581/591 carboxylic acid is highly photostable and can be used for ROS detection.
Fmoc-L-Dap(Pentynoyl)-OH is a click chemistry reagent containing an azide group. Fmoc-L-Dap(Pentynoyl)-OH serves as an amino acid building block for introducing alkyne functions into peptide sequences by standard Fmoc/tBu protocols. The alkyne residue can be engaged for copper catalyzed click reaction with organic azides or with tetrazines for copper-free conjugations.
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD).
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities.
DBCO-PEG4-Biotin is an azadibenzocyclooctyne-biotin derivative containing a biotin group and 4 PEGs. DBCO-PEG4-Biotin is a versatile biotinylation reagent used for the introduction of a biotin moiety to azide-labeled biomolecules via copper-free strain-promoted alkyne-azide click chemistry (SPAAC) reaction.
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis.
Purple-β-D-Gal is a chromogenic β-galactosidase substrate. Intracellular enzymatic hydrolysis of Purple-β-D-Gal generates free indoxyl molecules, which undergo in situ oxidation and subsequent dimerization to produce chromogenic, water-insoluble, indigo precipitates. Purple-β-D-Gal can be used for the detection of β-galactosidase activity.
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.
Dithiodipropionic acid can interact with CPUL1 (HY-151802, a TrxR inhibitor) to form nanoaggregates (CPUL1-DA NAs). CPUL1-DA NAs generates more abundant ROS to induce cell apoptosis than that of free CPUL1, and improves antitumor efficacy against HUH7 cancer cells.
13Z,16Z-Docosadienoic acid, a ω-6 polyunsaturated fatty acid, possesses anti-borreliae effect. 13Z,16Z-Docosadienoic acid, as a long-chain fatty acid (LCFA), is a free fatty acid receptor 4 (FFAR4 or GPR120, a LCFA receptor) agonist.
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
NNMT-IN-3 (compound 14) is a potent and selective nicotinamide N-methyltransferase NNMT inhibitor with IC50 values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. NNMT-IN-3 can be used to research obesity, type 2 diabetes, alcohol-related liver disease, cancer, sarcopenia and so on.
Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
Taurine- 13C2, 15N is the 13C- and 15N- labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research.
Uridine triacetate (Tri-O-acetyl uridine) is an orally active prodrug of Uridine (HY-B1449). Uridine triacetate is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate is used for the research of 5-fluorouracil (5-FU) and capecitabine toxicity, or early-onset cardiac or central nervous system (CNS).
Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine increases free copper and enhances oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria.
Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research.
Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research.
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways.
Tulobuterol-d9 (hydrochloride) is the deuterium labeled Tulobuterol. Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength[1].
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties. Pterostilbene blocks ROS production, also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide.
Edoxaban (DU-176b) tosylate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research.
ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively.
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
Copper tripeptide (GHK-Cu) is a tripeptide. During wound healing, copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a natural modulator of multiple cllular pathways in skin regeneration.
DIMBOA, an antibiotic, is a benzoxazinoid, part of the chemical defense system of graminaceous plants such as maize, wheat, and rye. DIMBOA possess growth inhibitory properties against many strains of studied bacteria and fungi, such as Staphylococcus aureus, Escherichia coli as well as against Saccharomyces cerevisiae. DIMBOA exhibits a potent free-radical scavenging activity and a weaker iron (III) ions reducing activity. Antioxidant activity.
DPPH (2,2-Diphenyl-1-picrylhydrazyl) is a stable free radical that can be used to measure the radical scavenging activity of antioxidants. The odd electron of nitrogen atom in DPPH is reduced by receiving a hydrogen atom from antioxidants to the corresponding hydrazine. DPPH method may be utilized in aqueous and nonpolar organic solvents and can be used to examine both hydrophilic and lipophilic antioxidants.
Tetrahydrofolic acid-d4 is the deuterium labeled Tetrahydrofolic acid. Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid[1][2].
N-Acetyl-DL-serine is a hydrophobic amino acid that is synthesized in the body and can be found as a free form or as a salt with malonate, phosphate, or acetate. N-Acetyl-DL-serine has antimicrobial activity against Bacillus cereus and Staphylococcus aureus. N-Acetyl-DL-serine has also been used for the immobilization of DNA fragments on solid surfaces and can be used for protein synthesis and optical detection of DNA strands.
Hadogenes Gunningi Venom (Gunning's Rock Scorpion Venom) is a venom that can be obtained from Hadogenes Gunningi (South African rock scorpion). Scorpion Venom is known to trigger the release of inflammatory mediators mediated by cytokines. Scorpion venoms are Complex mixtures of peptides, enzymes, mucoproteins, free amino acids, nucleotides, lipids, amines, heterocyclic components, inorganic salts, etc.
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier.
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na + channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.
D(+)-Galactosamine (D-Galactosamine) hydrochloride, which is an established experimental toxin, primarily causes liver injury by the generation of free radicals and depletion of UTP nucleotides. D(+)-Galactosamine hydrochloride intoxication also induces renal dysfunction thus, renal failure is often associated with the end-stage of the liver damage. Lipopolysaccharide/D(+)-Galactosamine-induced acute liver injury is a known animal model of fulminant hepatic failure[1][2].
(R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells.
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
DBCO-PEG2-DBCO is a click chemistry reagent containing an azide group. DBCO-PEG2-DBCO is a PEG linker containing two terminal DBCO groups. The DBCO groups is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. The hydrophilic PEG chain allows for increased water solubility. T Reagent grade, for research use only.
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
Filipin complex is a potent broad spectrum 28-membered ring pentaene macrolide antifungal antibiotic. Filipin complex is also a highly fluorescent polyene. Filipin complex specifically binds free cholesterol and is well established as a histochemical marker for the detection of unesterified cellular cholesterol. Filipin complex consists of four analogues (Filipins I-IV), with Filipin III (HY-N6718) comprising the bulk (>70%) of the complex.
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
Hydroxy-PEG3-DBCO is a click chemistry reagent containing an azide group. Hydroxy-PEG3-DBCO is a PEG linker containing a DBCO moiety and a terminal primary hydroxyl group. The hydroxyl can react with a variety of functional groups and the hydrophilic PEG spacer arm can provide better solubility to labeled molecules. DBCO is commonly used for copper-free Click Chemistry reactions. Reagent grade, for research use only.
Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM.
Lucifer Yellow CH dilithium salt is a high-intensity fluorescent probe containing free hydrazyl groups. Lucifer Yellow CH can react with fatty aldehydes at room temperature. Lucifer Yellow CH serves as a biological tracer to monitor neuronal branching, regeneration, gap junction detection and characterization, and selective ablation of cells after aldehyde fixation. Lucifer yellow CH displays the maximum excitation/emission of 430 nm/540 nm, respectively.
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM.
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
N-decanoyl-L-homoserine lactone (C10-HSL) is a N-acyl-homoserine lactone (AHL) N-decanoyl-L-homoserine lactone can inhibit primary root growth in Arabidopsis. N-decanoyl-L-homoserine lactone triggers a transient and immediate increase in the concentrations of cytosolic free Ca 2+ and reactive oxygen species (ROS), increases the activity of mitogen-activated protein kinase 6 (MPK6), and induces nitric oxide (NO) production in Arabidopsis roots.
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.
Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[1][2][3].
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action.
Lucifer Yellow CH dipotassium is a high-intensity fluorescent probe containing free hydrazyl groups. Lucifer Yellow CH can react with fatty aldehydes at room temperature. Lucifer Yellow CH serves as a biological tracer to monitor neuronal branching, regeneration, gap junction detection and characterization, and selective ablation of cells after aldehyde fixation. Lucifer yellow CH displays the maximum excitation/emission of 430 nm/540 nm, respectively.
ARN1468 (compound 5) is an orally active and potent serpins inhibitor. ARN1468 can inhibit serpins activity would set the protease free to further reduce prion accumulation. ARN1468 shows anti-prion effect in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC50 values of 8.64, 19.3, 11.2, and 6.27 μM.
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
EUK-134, a synthetic superoxide dismutase and catalase mimetic, protects rat kidneys from ischemia-reperfusion-induced damage. EUK-134 is a superoxide dismutase (SOD) mimetics (SODm) with catalase activity. EUK-134 is a mitoprotective antioxidant. EUK-134 reduces the expression of NF-κB, MDA level, and protein carbonylation in H9C2 cells.
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has drug-drug interactions.
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action.
Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects. Antroquinonol can be used for the research of colon cancer. Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice.
TUS-007 is a CANDDY molecular, modified from a proteasome inhibitor. However, TUS-007 hardly inhibits proteasome activity. TUS-007 is also an orally active and potent KRASG12D/V degrader. TUS-007 can be applied in KRAS G12D/V chemical knockdown in cell-free. TUS-007 also exhibits tumor suppression. Note: CANDDY refers to Chemical knockdown with Affinity aNd Degradation DYnamics.
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
DBCO-PEG24-acid is a click chemistry reagent. DBCO-PEG24-acid is an analog of DBCO-Acid with PEG linker and a DBCO group. The DBCO groups is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. The hydrophilic PEG chain allows for increased water solubility. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. Reagent grade, for research use only.
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice.
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.
CFSE is a fluorescent dye that can penetrate the cell membrane. It can react with the free amine group in the cytoskeleton protein inside the cell, and finally form a protein complex with fluorescence. After entering the cell, CFSE locates in the cell membrane, cytoplasm and nucleus, and the fluorescence staining is strongest in the nucleus.
CFSE dye can be uniformly inherited by the cells with cell division and proliferation, and its attenuation is proportional to the number of cell divisions. This phenomenon can be detected and analyzed by flow cytometry under the excitation light of 488nm, and can be used to detect the proliferation of cells.
Sulfo DBCO-PEG3-acid is a click chemistry reagent containing an azide group. Sulfo DBCO-PEG3-acid is an analog of DBCO-Acid with PEG linker and a DBCO group. The DBCO groups is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. The hydrophilic PEG chain and sulfo group increase water solubility. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. Reagent grade, for research use only.
Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent. Brusatol increases cellular apoptosis.
Cyanine5 DBCO (DBCO-Cy5) is a water-soluble, low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm).
Cyprodinil- 13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
Sulfo DBCO-PEG3-NHS ester is a click chemistry reagent containing an azide group. Sulfo DBCO-PEG3-NHS ester is an analog of DBCO-Acid with PEG linker and a DBCO group. The DBCO group is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. The hydrophilic PEG chain and sulfo group increase water solubility. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. Reagent grade, for research use only.
DBCO-PEG24-NHS ester is a click chemistry reagent. DBCO-PEG24-NHS ester is a click chemistry PEG reagent containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation. DBCO is commonly used for copper-free Click Chemistry reactions. Reagent grade, for research use only.
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].
DBCO-PEG2-NHS ester is a click chemistry reagent containing an azide group. DBCO-PEG2-NHS ester is a click chemistry PEG reagent containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation. DBCO is commonly used for copper-free Click Chemistry reactions. Reagent grade, for research use only.
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity.
H-L-Phe(4-NH-Poc)-OH (hydrochloride) is a click chemistry reagent containing an azide group. Used as a modified Phe or Tyr analogue in protein and peptide biosynthesis. Propargyloxycarbonyl, commonly abbreviated as Poc or Pryoc, can either be used as alkyne component for standard Click conjugation or in combination with tetrazine linkers in copper-free Diels-Alder type Click reactions. It also has applications as unusual protecting group for amines, hydroxy functions and as esters. All 3 are stable to neat TFA, but can be cleaved at ambient temperature with Co2(CO)8 in TFA:DCM. Deprotection with other transition metals like palladium have also been reported.
Boc-L-Phe(4-NH-Poc)-OH is a click chemistry reagent containing an azide group. Used as an orthogonally protected building block in peptide synthesis. Propargyloxycarbonyl, commonly abbreviated as Poc or Pryoc, can either be used as alkyne component for standard Click conjugation or in combination with tetrazine linkers in copper-free Diels-Alder type Click reactions. It also has applications as unusual protecting group for amines, hydroxy functions and as esters. All 3 are stable to neat TFA, but can be cleaved at ambient temperature with Co2(CO)8 in TFA:DCM. Deprotection with other transition metals like palladium have also been reported.
(S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
FCH Group Screening Library Collection contains about 2,244,487 lead-like compounds for biological screening. This brand new collection comprises polar molecules with pharmacologically important groups such as free carboxylic and amino groups.
MCE adhesive aluminium foil plate seals are of strong adhesive that can reduce chance of well-to-well contamination and sample evaporation when applied to microplates. This aluminium foil seal is suitable for long-term storage of samples at -80°C. The high integrity sealing materials give the best protection against evaporation and contamination. The aluminium foil seal features excellent chemical resistance to DMSO and DNase- & RNase- free. MCE adhesive foil seal is pierceable, peelable and easy-to-use.
Oxidative stress is an imbalance of free radicals and antioxidants in the body, which can lead to cell and tissue damage. Oxidative stress can be responsible for the induction of several diseases, both chronic and degenerative, as well as speeding up body aging process and cause acute pathologies. Antioxidants are a class of compounds able to counteract oxidative stress and mitigate its effects on individuals’ health, gained enormous attention from the biomedical research community. Antioxidants have long been substantial and amenable therapeutic arsenals for multifarious diseases such as AD and cancer.
MCE Antioxidant Compound Library contains 1214 compounds that act as antioxidants for high throughput screening (HTS) and high content screening (HCS). This library is a useful tool for discovery new antioxidants and oxidative stress research.
Normal mitochondrial function is critical for maintaining cellular homeostasis because mitochondria produce ATP and are the major intracellular source of free radicals. Cellular dysfunctions induced by intracellular or extracellular insults converge on mitochondria and induce a sudden increase in permeability on the inner mitochondrial membrane, the so-called mitochondrial membrane permeability transition (MMPT). MMPT is caused by the opening of pores in the inner mitochondrial membrane, matrix swelling, and outer membrane rupture. The MMPT is an endpoint to initiate cell death because the pore opening together with the release of mitochondrial cytochrome c activates the apoptotic pathway of caspases.
The normal operation of mitochondrial function is important for maintaining normal cell death and treatment of mitochondrial diseases. MCE offers a unique collection of 487 compounds with identified and potential mitochondrial protective activity. MCE Mitochondrial Protection Compound Library is critical for drug discovery and development.
Cy5 DBCO chloride is an azide reaction probe and the addition of DBCO molecules allows the imaging of azide-labelled biomolecules by a copper-free “Click Chemistry” reaction.
Cyanine3 DBCO (Cy3-DBCO) hexafluorophosphate is a azide reactive probe, for imaging azide-labeled biomolecules via a copper-free "click-through" reaction.
MitoTracker Green FM is a green-fluorescent dye that can selectively accumulate in the mitochondrial matrix. MitoTracker Green FM covalently binds to mitochondrial proteins by reacting with free thiol groups of cysteine residues.
CalFluor 488 Azide is a water-soluble fluorogenic azide probe. CalFluor 488 Azide is activated by Cu-catalyzed or metal-free click reaction. CalFluor 488 Azide is not fluorescent until it is reacted with alkynes.
5-IAF (5-Iodoacetamidofluorescein) is an idoacetamide derivate of fluoresceine. 5-IAF can be used as fluorescent probe that labels proteins and other molecules having free thiols (cysteine side chains).
Calcium Orange AM is an intracellular calcium reporter. Specific fluorescence can be detected when free calcium binds to Calcium Orange AM (Ex/Em=549/576 nm). Calcium Orange AM does not enter the vacuoles and does not compartmentalize into acidic vesicles.
Calcium Green-5N AM is a novel Ca 2+-sensitive fluorescent probe. Calcium Green-5N AM shows enhancement in fluorescence intensity on binding Ca 2+, and can monitor free Ca 2+ in neurons.
5-Dodecanoylaminofluorescein, a lipophilic fluorescent probe, is a free-fatty-acid conjugate of fluorescein. 5-Dodecanoylaminofluorescein has been used in membrane fluidity studies and the determination of critical micelle concentration of detergents. 5-Dodecanoylaminofluorescein can be also used to synthesize hydrophobic nanospheres for drug delivery.
5-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
5(6)-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
6-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes.
BDP 581/591 carboxylic acid is a fluorescent dye (Ex=585 nm, Em=594 nm). BDP 581/591 carboxylic acid has a free carboxylic acid group, which can be catalyzed by a catalyst (such as EDC or HATU) to react with primary amines to form stable amide bonds. BDP 581/591 carboxylic acid is highly photostable and can be used for ROS detection.
Purple-β-D-Gal is a chromogenic β-galactosidase substrate. Intracellular enzymatic hydrolysis of Purple-β-D-Gal generates free indoxyl molecules, which undergo in situ oxidation and subsequent dimerization to produce chromogenic, water-insoluble, indigo precipitates. Purple-β-D-Gal can be used for the detection of β-galactosidase activity.
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
Filipin complex is a potent broad spectrum 28-membered ring pentaene macrolide antifungal antibiotic. Filipin complex is also a highly fluorescent polyene. Filipin complex specifically binds free cholesterol and is well established as a histochemical marker for the detection of unesterified cellular cholesterol. Filipin complex consists of four analogues (Filipins I-IV), with Filipin III (HY-N6718) comprising the bulk (>70%) of the complex.
Lucifer Yellow CH dilithium salt is a high-intensity fluorescent probe containing free hydrazyl groups. Lucifer Yellow CH can react with fatty aldehydes at room temperature. Lucifer Yellow CH serves as a biological tracer to monitor neuronal branching, regeneration, gap junction detection and characterization, and selective ablation of cells after aldehyde fixation. Lucifer yellow CH displays the maximum excitation/emission of 430 nm/540 nm, respectively.
Lucifer Yellow CH dipotassium is a high-intensity fluorescent probe containing free hydrazyl groups. Lucifer Yellow CH can react with fatty aldehydes at room temperature. Lucifer Yellow CH serves as a biological tracer to monitor neuronal branching, regeneration, gap junction detection and characterization, and selective ablation of cells after aldehyde fixation. Lucifer yellow CH displays the maximum excitation/emission of 430 nm/540 nm, respectively.
CFSE is a fluorescent dye that can penetrate the cell membrane. It can react with the free amine group in the cytoskeleton protein inside the cell, and finally form a protein complex with fluorescence. After entering the cell, CFSE locates in the cell membrane, cytoplasm and nucleus, and the fluorescence staining is strongest in the nucleus.
CFSE dye can be uniformly inherited by the cells with cell division and proliferation, and its attenuation is proportional to the number of cell divisions. This phenomenon can be detected and analyzed by flow cytometry under the excitation light of 488nm, and can be used to detect the proliferation of cells.
Cyanine5 DBCO (DBCO-Cy5) is a water-soluble, low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm).
Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS.
Superoxide dismutase (SOD) is the only antioxidant enzyme that scavenges the superoxide anion by converting this free radical to oxygen and hydrogen peroxide, thus preventing peroxynitrite production and further damage. Superoxide dismutase is extensively researched and used in anti-inflammatory, antitumor, radiation protection, and antisenility applications.
Endo-β-N-acetylglucosaminidase (Endo S2) is a key enzyme involved in the processing of free oligosaccharides in the cytosol. Endo-β-N-acetylglucosaminidase catalyzes hydrolysis of N-linked oligosaccharides.
CMP-sialic acid synthetase (CSS) is an essential enzyme involved in the biosynthesis of carbohydrates and glycoconjugates containing sialic acids. CMP-sialic acid synthetase activates free Sia, converting it to CMP-Sia, which is the only donor substrate for all sialyltransferases.
Cholesterol esterase is an enzyme that hydrolyzes cholesterol ester to cholesterol and free fatty acid in the intestinal lumen. Cholesterol synthesized in the acinar cells and is stored in zymogen granules. Cholesterol esterase is also known as bile salt-stimulated lipase and carboxy ester lipasea, acts function for acceleration of cholesterol absorption.
Carboxypeptidase B is a peptide exonuclease that can specifically degrade peptide chains. Carboxypeptidase B is progressively degraded from the C-terminal to release free amino acids. Carboxypeptidase B hydrolyzes only peptide bonds with basic amino acids (such as arginine and lysine) as C-terminal residues.
Yeast extract is a concentrate of the soluble part of yeast, especially Saccharomyces cerevisiae. The main nutritional components of yeast extract include partly hydrolyzed protein with 35-40% of free amino acid, and it also contain B vitamins and some trace elements. Yeast extract can be used as nutrients for bacterial culture media.
α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways.
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with high affinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit.
Fexapotide (NX-1207 free acid) induces apoptosis selectively, reducing prostate volume at a cellular level. Fexapotide can be used in lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH) research.
Oxytocin free acid (9-Deamidooxytocin) is an analog of oxytocin in which the glycinamide residue at position 9 in oxytocin has been replaced by a glycine residue. Oxytocin is a pleiotropic, peptide hormone with broad implications for general health, adaptation, development, reproduction, and social behavior.
Pexiganan (MSI 78 free base) is a synthetic analog of magainin 2. Pexiganan is a potent and orally active broad-spectrum antimicrobial peptide. Pexiganan can be used in the research of infections, such as diabetic foot ulcer infections.
Suc-AAPF-pNA (Suc-Ala-Ala-Pro-Phe-pNA) is a chromogenic p-nitroanilide (pNA) substrate with the Km of 1.7 mM. Suc-AAPF-pNA can be used for the Measurement of free and membrane-bound cathepsin G in human neutrophils.
Oxytocin free acid (9-Deamidooxytocin) TFA is an analog of oxytocin in which the glycinamide residue at position 9 in oxytocin has been replaced by a glycine residue. Oxytocin is a pleiotropic, peptide hormone with broad implications for general health, adaptation, development, reproduction, and social behavior.
Cyclosporin A-Derivative 1 (Free base) is a crystalline intermediate derived from the opening of cyclosporin A extracted from patent WO 2013167703 A1. Cyclosporin A is an immunosuppressive agent which can bind to the cyclophilin and inhibit calcineurin.
Astodrimer (SPL7013 free base) is a large (3-4 nm, ~ 16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties.
Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer.
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
Copper tripeptide (GHK-Cu) is a tripeptide. During wound healing, copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a natural modulator of multiple cllular pathways in skin regeneration.
N-Acetyl-DL-serine is a hydrophobic amino acid that is synthesized in the body and can be found as a free form or as a salt with malonate, phosphate, or acetate. N-Acetyl-DL-serine has antimicrobial activity against Bacillus cereus and Staphylococcus aureus. N-Acetyl-DL-serine has also been used for the immobilization of DNA fragments on solid surfaces and can be used for protein synthesis and optical detection of DNA strands.
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
MCE Serum/Protein-Free Cell Freezing Medium is a complete ready-to-use cryopreservation medium. It is suitable for the cryopreservation of conventional mammalian cells and serum-free cultured cells.
MCE Protease Inhibitor Cocktail, Bacteria (EDTA-Free, 100× in DMSO) protects proteins from degradation by endogenous proteases released during protein extraction and purification.
MCE Protease and Phosphatase Inhibitor Cocktail (EDTA-Free, 10× in ddH2O) protects protein from degradation by endogenous proteases released during protein extraction and purification.
Tamtuvetmab (AT-005) is a caninised blontuvetmab against CD52. Tamtuvetmab increases progression-free survival (PFS), exhibits in vivo efficacy in dogs with naïve T-cell lymphoma (LSA). Tamtuvetmab has been approved by veterinary.
Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema.
Emapalumab (NI-0501) is a humanized monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH).
Milatuzumab (hLL1; MEDI-115) is a humanized anti-CD74 monoclonal antibody. CD74, a integral membrane protein, is associated with the promotion of B-cell growth and survival. Milatuzumab causes free radical oxygen generation, and loss of mitochondrial membrane potential. Milatuzumaba also decreases CD20/CD74 aggregates and cell adhesion, to lead to cell death.
3'-O-Methylorobol, an antioxidant flavonoid, exhibits moderate antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay.
Dianemycin (Nanchangmycin free acid), a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E.
D-Isofloridoside, one of the polysaccharide precursors, has the activity of scavenging free radicals, inhibiting ROS expression, and inhibiting MMP-2 and MMP-9.
Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity.
Pexiganan (MSI 78 free base) is a synthetic analog of magainin 2. Pexiganan is a potent and orally active broad-spectrum antimicrobial peptide. Pexiganan can be used in the research of infections, such as diabetic foot ulcer infections.
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4 + T cells and CD11b + macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM.
2'-Acetylacteoside is a phenylethanoid glycoside isolated from Brandisia hancei, inhibits free radical-induced hemolysis of red blood cells and exhibits free radical scavenging activity.
Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively.
Octadecanedioic acid, an endogenous metabolite, is a long-chain dicarboxylic acid that has been found in serum free fatty acid profile in Reye syndrome.
Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 µM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 µM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects.
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
Pyrogallol is a polyphenol compound, which has anti-fungal and anti-psoriatic properties. Pyrogallol is a reductant that is able to generate free radicals, in particular superoxide anions.
Erigeroside is as a derivatives of -glucose extracted from Satureja khuzistanica Jamzad. Erigeroside has good ability of anti-oxidation and scavenging oxidation free radical.
Urolignoside is an antioxidant with free radical scavenging activity. Urolignoside potently scavenges DPPH radical, and exhibits antioxidant to β-carotene-lineoleate model.
Bacopaside I, a saponin isolated from Bacopa monnieri, exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.
Senecionine acetate (O-Acetylsenecionine) is a pyrrolizidine alkaloid. Senecionine acetate inhibits the sequestration of Ca 2+ in extramitochondrial and mitochondrial compartments possibly by inactivating free sulfhydryl groups.
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Cephaeline is a phenolic alkaloid in Indian Ipecac roots. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections.
Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
Polyporusterone B is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone B has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
8-hydroxybergapten is O-methylated by cell-free extracts of Ruta cells to isopimpinellin, in reactions mediated by discrete O-methyltransferases. 8-hydroxybergapten has excellent anti-wrinkle effect.
Rehmannic acid (lantadene A) is a compound isolated from Lantana camara. Rehmannic acid shows considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner. Rehmannic acid is a promising candidate for use as an antioxidant and hepatoprotective agent.
Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities. Anticancer activities.
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin II inhibits cell-free protein synthesis, releases adenine from rat liver ribosomes and from DNA, and has no RNase activity.
(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC50 value of 7.49 μM (A549 cells).
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
o-Hydroxybenzylamine (2-HOBA) a selective dicarbonyl scavenger, is an antioxidant and scavanger of free radicals and isolevuglandins (IsoLGs). o-Hydroxybenzylamine can be used in the research of inflammation and cardiovascular disease, such as atherosclerosis, early recurrence of atrial fibrillation (AF) and arrhythmias.
Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.
Gallic acid (3,4,5-Trihydroxybenzoic acid) hydrate is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid hydrate has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
Ombuoside is a glycoside ombuoside isolated from Gynostemma pentaphyllum.Ombuoside has antimicrobial activity against several strains of gram-positive and gram-negative bacteria and the yeast Candida albicans. Ombuoside has antioxidant effects by scavenging free radicals and ROS.
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
Hadogenes Bicolor Venom is a venom that can be obtained from Hadogenes Bicolor (South African flat rock scorpion). Scorpion venoms are Complex mixtures of peptides, enzymes, mucoproteins, free amino acids, nucleotides, lipids, amines, heterocyclic components, inorganic salts, etc.
Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is a potent free radical scavenger. Eriodictyol-7-O-glucoside is also an Nrf2 activator, confers protection against Cisplatin-induced toxicity.
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
Isoarjunolic acid (2α,3α,23-Trihydroxyolean-12-en-28-oic acid) is a triterpenoid, can be isolated from the stems of Cornus kousa. Isoarjunolic acid could have free radical scavenging activity and elastase inhibition activity .
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase.
Atherosperminine（Atherospermine）is a nature occurring alkaloid, has antiplasmodial activities in vitro, with an IC50 of 5.80 μM. Atherosperminine is a good reductant with the ability to chelate metals. Atherosperminine has scavenging activity towards the free radical DPPH, with an IC50 of 29.56 µg/mL. Atherosperminine exerts a non-specific relaxant effect on the trachealis.
Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid.
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD).
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis.
D-luciferin is the natural substrate of the enzyme luciferase (Luc) that catalyzes the production of the typical yellowgreen light of fireflies. The 560 nm chemiluminescence from this reaction peaks within seconds, with light output that is proportional to luciferase concentration when the substrate luciferin is present in excess. The luciferase (luc) gene is a popular reporter gene for research and drug screening. Chemiluminescent techniques are virtually background-free, making the luc reporter gene ideal for detecting low-level gene expression. As little as 0.02 pg of luciferase can be reliably measured in a standard scintillation counter. In addition to its role as a reporter of gene expression, luciferase is commonly used in an extremely sensitive assay for ATP. We of er the firefly luciferase (HY-P1004), luciferin free acid (HY-12591A), as well as its water-soluble sodium salts (HY-12591) and potassium salts (HY-12591B) .
Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine increases free copper and enhances oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria.
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways.
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties. Pterostilbene blocks ROS production, also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide.
Copper tripeptide (GHK-Cu) is a tripeptide. During wound healing, copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a natural modulator of multiple cllular pathways in skin regeneration.
DIMBOA, an antibiotic, is a benzoxazinoid, part of the chemical defense system of graminaceous plants such as maize, wheat, and rye. DIMBOA possess growth inhibitory properties against many strains of studied bacteria and fungi, such as Staphylococcus aureus, Escherichia coli as well as against Saccharomyces cerevisiae. DIMBOA exhibits a potent free-radical scavenging activity and a weaker iron (III) ions reducing activity. Antioxidant activity.
Hadogenes Gunningi Venom (Gunning's Rock Scorpion Venom) is a venom that can be obtained from Hadogenes Gunningi (South African rock scorpion). Scorpion Venom is known to trigger the release of inflammatory mediators mediated by cytokines. Scorpion venoms are Complex mixtures of peptides, enzymes, mucoproteins, free amino acids, nucleotides, lipids, amines, heterocyclic components, inorganic salts, etc.
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na + channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
D(+)-Galactosamine (D-Galactosamine) hydrochloride, which is an established experimental toxin, primarily causes liver injury by the generation of free radicals and depletion of UTP nucleotides. D(+)-Galactosamine hydrochloride intoxication also induces renal dysfunction thus, renal failure is often associated with the end-stage of the liver damage. Lipopolysaccharide/D(+)-Galactosamine-induced acute liver injury is a known animal model of fulminant hepatic failure[1][2].
(R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells.
Filipin complex is a potent broad spectrum 28-membered ring pentaene macrolide antifungal antibiotic. Filipin complex is also a highly fluorescent polyene. Filipin complex specifically binds free cholesterol and is well established as a histochemical marker for the detection of unesterified cellular cholesterol. Filipin complex consists of four analogues (Filipins I-IV), with Filipin III (HY-N6718) comprising the bulk (>70%) of the complex.
Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM.
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM.
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent. Brusatol increases cellular apoptosis.
Glial-cell-line-derived neurotrophic factor (GDNF), a neurotrophic factor belongs to the GDNF family ligands (GFLs)., promotes survival of dopamine neurons. GDNF demonstrates a variety of neuroprotective roles for mammalian neurons. Animal-Free GDNF Protein, Mouse (His), a recombinant animal-free protein, is produced in E.coil with a C-Terminal His-tag. It consists of 134 amino acids (S78-I211).
CNTF is a pluripotent neurotrophic factor, belonging to the IL-6 cytokine family. CNTF could protect retinal cone and rod photoreceptors. CNTF has neuroprotective effects on a variety of central and also peripheral nervous system neurons. Animal-Free CNTF Protein, Human (His) is produced by E. coli (M1-M200) with C-terminal His-tag.
CNTF is a pluripotent neurotrophic factor, belonging to the IL-6 cytokine family. CNTF could protect retinal cone and rod photoreceptors. CNTF has neuroprotective effects on a variety of central and also peripheral nervous system neurons. Animal-Free CNTF Protein, Mouse (His) is produced by E. coli (M1-M198)with C-terminal His-tag.
FGF-7 Protein, Mouse (His) is a potent mitogen that enhances cell proliferation in various organs, including the skin, intestine, breast, liver, and lung.
Bone morphogenetic protein 4 (BMP-4) is a polymorphic ligand protein belonging to the TGF-β family, which is involved in the circulation of the vascular system and can activate receptors on vascular cells. BMP-4 binds to type I receptors (ALK-2/-3/-6) and type II receptors (BMPR2, ACVR2A) to increase plaque formation and promote oxidative stress, endothelial dysfunction, and osteogenic differentiation through its pro-inflammatory and pro-atherogenic effects. Animal-Free BMP-4 Protein, Human (His) has a total length of 106 amino acids (K303-R408), is expressed in E. coli cells with a C-terminal His-tag.
The TL1A protein (VEGI protein), belongs to the tumor necrosis factor (TNF) family and is a receptor for TNFRSF25 and TNFRSF6B. TL1A is involved in the activation of NF-κB and C-Jun pathways, which can be used as a regulator of mucosal immunity and participate in the immune pathway of inflammatory bowel disease (IBD) pathogenesis. TL1A originates from endothelial cells and inhibits the proliferation of breast cancer, epithelial and myeloid tumor cells. The human TL1A protein has a transmembrane domain (36-56 a.a.) that can be cleaved into membrane-type and soluble peptide fragments. Animal-Free TL1A/TNFSF15 Protein, Human (His) is the extracullar part of TL1A protein (Q58-L251), produced in E.coli with C-terminal His-tag.
Brain Derived Neurotrophic Factor (BDNF) is a neurotrophin that belongs to NGF-beta family. BDNF can bind to its high affinity receptor TrkB and activates signal transduction cascades (IRS1/2, PI3K, Akt). BDNF can also bind to the p75NTR, but the affinity for the p75NTR receptor is lower than for TrkB. BDNF is a neurotransmitter modulator, and is vital in maturation, survival and differentiation of neuronal populations during development. BDNF also participates in neuronal plasticity, which is essential for learning and memory. BDNF is widely expressed in the CNS. Animal-Free BDNF Protein, Human/Mouse (His) is an animal-free recombinant human/muose BDNF (H129-R247) with C-terminal His tag, which is produced in E.coli.
Activin B, a TGFβ superfamily cytokine, is a homodimer of activin βB subunits. Activin B binds to type II transmembrane serine-threonine kinase receptors (ACTRIIA or ACTRIIB) which, in turn, activate type I receptors (ACTRI) that phosphorylate and activate canonical SMAD signaling pathways. Animal-Free Activin B Protein, Human (His), a recombinant animal-free protein, is produced in
E. coli with a C-Terminal His-tag. It consists of 115 amino acids (G293-407A).
Nerve Growth Factor-β (Beta-NGF; NGF) is a neurotrophic factor that regulates neuronal survival and differentiation. NGF is also a seminal plasma protein involved in ovulation and luteinizing. NGF has potential functions in the female reproductive system to help overcome the current problem of early embryo loss. Animal-Free Beta-NGF Protein, Human (His) is produced by E.coli (S122-A241), with C-terminal His-tag.
Bone morphogenetic protein 11 (BMP-11; GDF11), also known as growth/differentiation factor 11, is a polymorphic ligand protein belonging to the TGFβ family. The GDF-11/BMP-11 signal activates the signal through activator receptor types I and II, resulting in the phosphorylation of SMAD2 and SMAD3. GDF-11/BMP-11 is an important regulator of central nervous system (CNS) formation and fate. Exogenous peripheral delivery of GDF-11/BMP-11 may enhance neurogenesis and angiogenesis and improve neuropathological outcomes in the elderly brain. The total length of human GDF-11/BMP-11 protein is 407 amino acids (M1-M407), with a glycosylation domain. Animal-Free GDF-11/BMP-11 Protein, Human (His) has a total length of 109 amino acids (N299-S407), is expressed in E. coli with C-terminal His-tag.
BMP-8 is a pleiotropic ligand protein act as a reproductive system regulator, enriched in the ovary. BMP-8 is encoded by a pair of genes BMP8A and BMP8B, belonging to TNF-β family. BMP-8A activates the SMAD1/5/8 and the SMAD2/3 pathways in granulosa cells, to inhibit gonadotropin-induced progesterone production and steroidogenesis-related gene expression. BMP-8A also involves in Nrf2 phosphorylation in cancer cells to promote survival and drug resistance. BMP-8a Protein, Human is 402 a.a. with 2 glycosylation domains. Animal-Free BMP-8a Protein, Human (His) is a animal free recombinant human protein produced in E. coli cells, with 139 a.a. (A264-H402) and C-terminal His-tag.
FGF-2 is a member of the fibroblast family involved in bone healing, cartilage repair, bone repair, and nerve regeneration. FGF-2 is also a mitotic promoter that accelerates cell proliferation. FGF-2 regulates immune processes by specifically targeting tyrosine kinase receptors and activating the FGF/FGFR signaling pathway. For example, FGF-2 is involved in the JAK-STAT signaling pathway to regulate cartilage metabolism and also activates ERK signaling to promote cartilage regeneration. FGF-2 combined with FGFR1/3 promoted degeneration and repair of articular cartilage, respectively. FGF-2 is also a known carcinogen in GBM, which contributes to glioma growth and vascularization.Animal-Free FGF-2 Protein, Mouse (His), consists of 144 amino acids, produced by E.coli with tag free.
AITRL, a type II transmembrane protein, is a ligand for glucocorticoid-induced TNFR-related protein (GITR). When AITRL binds to GITR, GITR can produce costimulatory signals that regulate T-cell proliferation and effector functions. GITR/AITRL interaction plays a role in the pathogenesis of tumor, inflammation, as well as autoimmune diseases. Besides, AITRL plays a role in endothelial cells (EC)-activation and increases STAT-1 phosphorylation and the expression of adhesion molecules (VCAM-1, ICAM-1). Animal-Free AITRL/TNFSF18 Protein, Human (His) is a recombinant human AITRL (Q49-I174) with C-terminal His tag, which is expressed in E.coli.
Nerve Growth Factor-β (Beta-NGF; NGF) is a neurotrophic factor that regulates neuronal survival and differentiation. NGF is also a seminal plasma protein involved in ovulation and luteinizing. NGF has potential functions in the female reproductive system to help overcome the current problem of early embryo loss. Animal-Free Beta-NGF Protein, Mouse (His) is produced by E.coli (S122-G241), with C-terminal His-tag.
Bone morphogenetic protein 15 (BMP-15; GDF9B), also known as growth differentiation factor 9B (GDF9B), is a polymorphic ligand protein of the TGFβ family and is only expressed in follicular cells. BMP15 is closely related to GDF9 and synergistically regulates the genetic development of follicles. BMP15 is involved in p38 MAPK and HIF-1α/SCF signaling pathway, respectively, and can up-regulate the expression of anti-Mullerian hormone (AMH) and polycystic ovarian syndrome (PCOS) related stem cell factor (SCF) in granulosa cells. The total length of human BMP-15 protein is 392 amino acids (M1-R392), with 4 glycosylation domains. Animal-Free BMP-15 Protein, Human (His) has a total length of 125 amino acids (Q268-R392), is expressed in E. coli cells with a C-terminal His-tag.
Glial-cell-line-derived neurotrophic factor (GDNF), a neurotrophic factor belongs to the GDNF family ligands (GFLs)., promotes survival of dopamine neurons. GDNF demonstrates a variety of neuroprotective roles for mammalian neurons. Animal-Free GDNF Protein, Human (His), a recombinant animal-free protein, is produced in E.coil with a C-Terminal His-tag. It consists of 134 amino acids (S78-I211).
Bone morphogenetic protein 4 (BMP-4) is a polymorphic ligand protein belonging to the TGF-β family, which is involved in the circulation of the vascular system and can activate receptors on vascular cells. BMP-4 binds to type I receptors (ALK-2/-3/-6) and type II receptors (BMPR2, ACVR2A) to increase plaque formation and promote oxidative stress, endothelial dysfunction, and osteogenic differentiation through its pro-inflammatory and pro-atherogenic effects. Animal-Free BMP-4 Protein, Pig (His) has a total length of 182 amino acids (R43-C224), is expressed in E. coli cells with C-terminal His-tag.
FGF-2 is a member of the fibroblast family involved in bone healing, cartilage repair, bone repair, and nerve regeneration. FGF-2 is also a mitotic promoter that accelerates cell proliferation. FGF-2 regulates immune processes by specifically targeting tyrosine kinase receptors and activating the FGF/FGFR signaling pathway. For example, FGF-2 is involved in the JAK-STAT signaling pathway to regulate cartilage metabolism and also activates ERK signaling to promote cartilage regeneration. FGF-2 combined with FGFR1/3 promoted degeneration and repair of articular cartilage, respectively. FGF-2 is also a known carcinogen in GBM, which contributes to glioma growth and vascularization.Animal-Free FGF basic/bFGF Protein, Human (154a.a, His), consists of 154 amino acids, produced by E.coli with tag free.
BMP-8 is a pleiotropic ligand protein act as a reproductive system regulator, enriched in the ovary. BMP-8 is encoded by a pair of genes BMP8A and BMP8B, belonging to TNF-β family. BMP-8B is secreted by brown/beige adipocytes and enhances energy dissipation, serves as a potential targets in obesity. BMP-8B also caspase-3 and -9 activation in pancreatic cancer cell, as well as decreasing mitochondrial membrane potential to induce apoptosis. BMP-8b Protein, Human is 402 a.a. with 2 glycosylation domains. Animal-Free BMP-8a Protein, Human (His) is a animal free recombinant human protein produced in E. coli cells, with 139 a.a. (A264-H402) and N-terminal His-tag.
KGF/FGF-7 Protein, Human (153a.a) is a polypeptide mitogen that belongs to the family of fibroblast growth factors, binds only to a splice variant of FGFR2 (FGFR2 IIIb) and is a highly specific paracrine growth factor for epithelial cells. KGF/FGF-7 Protein and its receptor are important for normal wound healing.
Bone morphogenetic protein 4 (BMP-4) is a polymorphic ligand protein belonging to the TGF-β family, which is involved in the circulation of the vascular system and can activate receptors on vascular cells. BMP-4 binds to type I receptors (ALK-2/-3/-6) and type II receptors (BMPR2, ACVR2A) to increase plaque formation and promote oxidative stress, endothelial dysfunction, and osteogenic differentiation through its pro-inflammatory and pro-atherogenic effects. Animal-Free BMP-4 Protein, Mouse (His) has a total length of 106 amino acids (K303-R408), is expressed in E. coli cells with C-terminal His-tag.
LIGHT/TNFSF14 protein (CD258; TNFRSF14) is a type II transmembrane protein produced by activated T cells. It is a TNFRSF14/HVEM ligand and belongs to the tumor necrosis factor (TNF) family. LIGHT/TNFSF14 is mainly expressed in spleen, with two subtypes: membrane-bound type and soluble type . LIGHT/TNFSF14 protein can be used as immune checkpoint molecule of tumor, and stimulate natural killer cells to produce interferon TFNγ, triggering tumor apoptosis signal . LIGHT/TNFSF14 is also involved in the dominant LTβR-NIK-p52 NF-κB pathway promoting the expression of inflammatory gene. In addition, LIGHT/TNFSF14 protein is a co-stimulatory factor that activates lymphoid cells and has an inhibitory effect on herpes virus infection. Mouse LIGHT/TNFSF14 Protein has 239 amino acids and a transmembrane domain (38-58 a.a.). Animal-Free LIGHT/TNFSF14 Protein, Mouse (His) is the extracellular part (R58-V239) of mouse LIGHT/TNFSF14 Protein, produced by E.coli, with C-terminal His-tag.
TWEAK Protein refers to the cytokine tumor necrosis factor-like weak inducer of apoptosis, belongs to tumor necrosis factor (TNF) superfamily. TWEAK protein binds to FN14 and TNRFSF12/APO3, is a weak inducer of apoptosis. TWEAK does have pro-apoptotic activity for tumor cell, mediates NF-kappa-B activation, promotes angiogenesis and the proliferation of endothelial cells (ECs). TWEAK also increases IL-6 and IL-8 secretion, and could potentiate the pro-inflammatory activities of TNF and IL-1. Human TWEAK protein is a type II transmembrane protein (M1-H249) with a transmembrane domain (22-42 a.a.). Animal-Free TWEAK/TNFSF12 Protein, Human (His) is the extracellular part (K97-H249) of TWEAK protein, produced by E. coli with C-terminal His-tag.
Fas Ligand (CD178; APTL) is a ligand to TNFRSF6/FAS/CD95, transduces the apoptotic signal to regulate cytotoxic T-cell-mediated apoptosis, natural killer cell-mediated apoptosis and in T-cell development. Human Fas Ligand exhibits 4 isoforms, the soluble form (130-281 a.a.) of which plays an important role in the activation-induced cell death (AICD) of T lymphocytes Jurkat cells. However the membrane-bound isoform could be responsible for its inflammatory activity. Animal-Free FasL Protein, Human (His) has a total length of 152 amino acids (Q130-L281), is expressed in E. coli with N-terminal His-tag.
APRIL protein (CD256) is a ligand in the tumor necrosis factor (TNF) family that can induce proliferation, regulate tumor cell growth, and may participate in mononuclear/macrophage-mediated immune process. APRIL protein is produced by myeloid cells and their precursors to accelerate cell maturation and peripheral rupture. APRIL protein has been widely used in the study of lymphatic malignancies. Human APRIL protein is a type II membrane protein with cytoplasmic domain, hydrophobic transmembrane domain and extracellular domain. Animal-Free APRIL/TNFSF13 Protein, Human (His) is produced by E. coli (A105-L250) with C-terminal His-tag.
LIGHT/TNFSF14 protein (CD258; TNFRSF14) is a type II transmembrane protein produced by activated T cells. It is a TNFRSF14/HVEM ligand and belongs to the tumor necrosis factor (TNF) family. LIGHT/TNFSF14 is mainly expressed in spleen, with two subtypes: membrane-bound type and soluble type . LIGHT/TNFSF14 protein can be used as immune checkpoint molecule of tumor, and stimulate natural killer cells to produce interferon TFNγ, triggering tumor apoptosis signal . LIGHT/TNFSF14 is also involved in the dominant LTβR-NIK-p52 NF-κB pathway promoting the expression of inflammatory gene. In addition, LIGHT/TNFSF14 protein is a co-stimulatory factor that activates lymphoid cells and has an inhibitory effect on herpes virus infection. Human LIGHT/TNFSF14 Protein has 240 amino acids and a transmembrane domain (38-58 a.a.). Animal-Free LIGHT/TNFSF14 Protein, Human (His) is the extracellular part (R64-V240) of human LIGHT/TNFSF14 Protein, produced by E. coli, with C-terminal His-tag.
FGF-2 is a member of the fibroblast family involved in bone healing, cartilage repair, bone repair, and nerve regeneration. FGF-2 is also a mitotic promoter that accelerates cell proliferation. FGF-2 regulates immune processes by specifically targeting tyrosine kinase receptors and activating the FGF/FGFR signaling pathway. For example, FGF-2 is involved in the JAK-STAT signaling pathway to regulate cartilage metabolism and also activates ERK signaling to promote cartilage regeneration. FGF-2 combined with FGFR1/3 promoted degeneration and repair of articular cartilage, respectively. FGF-2 is also a known carcinogen in GBM, which contributes to glioma growth and vascularization.Animal-Free FGF-2 Protein, Pig (His), consists of 1 amino acids, produced by E.coli with tag free.
RANKL (TNFSF11), a type II transmembrane protein, is a receptor ligand for NF-κB (RANK). RANKL is an activator of NF-κB. When binding to NF-κB, it induces the differentiation of monocyte/macrophage-lineage cells into osteoclasts and leads to osteoclast precursor maturation. RANKL is critical for osteoclasts maturation, bone modeling, and bone remodeling, as well as the development of lymph nodes (LNs). Animal-Free RANK L/TNFSF11 Protein, Mouse (His) is a recombinant mouse RANKL (P143-D316) with C-terminal His tag, which is produced in E.coli.
rHu72 kDa type IV collagenase/MMP-2, His ; 72 kDa Type IV Collagenase; 72 kDa Gelatinase; Gelatinase A; Matrix Metalloproteinase-2; MMP-2; TBE-1; MMP2; CLG4A
BAFF/TNFSF13B, is the B cell-activating cytokine belonging to the tumor necrosis factor family. BAFF is involved in cancer immunity and is mainly expressed in myeloid cells. Its overexpression can lead to autoimmune diseases such as systemic lupus erythematosus (SLE). In addition, BAFF is also involved in adipogenesis, atherosclerosis, neuroinflammatory process and ischemia/reperfusion (I/R) injury . Mouse BAFF protein has two glycosylated domains and one transmembrane domain (48-68 a.a.), and can be cleaved into membrane-type peptide fragments and soluble peptide fragments. Animal-Free BAFF/TNFSF13B Protein, Mouse (His) is the extracullar part of BAFF protein (A127-L309), produced in HEK293 cells with C-terminal His-tag.
CXCL12 (stromal cell-derived factor-1, SDF-1) is a homeostatic chemokine that binds CXCR4 and CXCR7 receptors and physiologically functions in hematopoiesis, leucocyte trafficking, cardiogenesis, and neurogenesis. CXCL12 is constitutively expressed in several organs including lung, liver, skeletal muscle, brain, kidney, heart, skin, and bone marrow. CXCL12 has an essential role in neural and vascular development, hematopoiesis, cancer and in immunity. CXCL12 Protein, Mouse is produced in E. coli, and consists of 68 amino acids (K22-K89).
