AN-AZ

Bioactive Small Molecules

Product #

Image

Product Name

Biochem/physiol Actions

Gene Symbol (ID)

Add to Cart

SML1424 Ac-YVAD-pNA ≥98% (HPLC) Ac-YVAD-pNA is a very selective chromogenic substrate for caspase-1, a key mediator of inflammatory processes formerly known as interleukin (IL)-1-converting enzyme. Ac-YVAD-pNA is used to determine caspase-1 activity. Cleavage of Ac-YVAD-pNA by caspase-1 releases pNA (p-nitroanilide), which can be quantified spectrophotometrically at 405 nm.
 
A8236 AN-9 ≥95% (HPLC) HDAC Inhibitor tested as an anti-cancer drug; butyric acid pro-drug
 
SML0209 ANA-12 ≥98% (HPLC) The neurotrophin brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) have emerged as key mediators in the pathophysiology of several mood disorders, including anxiety and depression. ANA-12 is a TrkB ligand that prevents activation of the receptor by BDNF with a high potency. It binds selectively to TrkB and inhibits processes downstream of TrkB without altering TrkA and TrkC functions. In adult mice model ANA-12 decreases TrkB activity in the brain without affecting neuronal survival. Mice dosed with ANA-12 show reduced anxiety- and depression related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans. ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders. There is also N-T19, which is less potent.
 
A7236 Anacardic acid Anacardic acid is a HAT (Histone Acetyltransferase) inhibitor.
 
SML0846   Anagrelide hydrochloride ≥98% (HPLC) Anagrelide is a phosphodiesterase inhibitor with antiplatelet activity (IC50 = 36 nM for inhibition of phosphodiesterase-III). Anagrelide inhibits the maturation of megakaryocytes into platelets, reducing both megakaryocyte hyperproliferation and differentiation. As a drug, anagrelide is antithrombocythemic used for the treatment of overproduction of blood platelets.
 
A2736 Anastrozole ≥98% (HPLC) Anastrozole, which contains a triazole functional group, reversibly binds to the cytochrome P-450 component of aromatase. Binding interferes with the catalytic properties of aromatase, which results in inhibition of estrogen synthesis.
 
A8598 Ancitabine hydrochloride Antineoplastic
 
A7505 1,4-Androstadiene-3,17-dione   human ... CYP19A1(1588)
A7755 5α-Androstane-3α,17β-diol Dihydroandrosterone is a testosterone metabolite; affects sperm maturation and survival.
rat ... Ar(24208)
A2480 5α-Androstan-3β-ol powder mCAR (constitutive androstane receptor) inverse agonist; testosterone metabolite.
 
A8380 5α-Androstan-17β-ol-3-one ≥97.5% Androstanolone is an anabolic steroid. Testosterone secreted by the testis is converted to dihydrotestosterone in the target tissues where it appears to mediate many of the biological actions of testosterone. Androgens direct the development of the male phenotype during embryogenesis and at puberty.
human ... AR(367), ESR1(2099), PGR(5241), SERPINA6(866), SHBG(6462)
mouse ... Esr1(13982)
rat ... Ar(24208), Esr1(24890), Nr3c1(24413), Nr3c2(25672), Pgr(25154)
A7883 5α-Androst-16-en-3α-ol 5alpha-androst-16-en-3alpha-ol (androstenol), is an androgen believed to act as a pheromone.
 
A3009 4-Androsten-11β-ol-3,17-dione 11β-Hydroxy-4-androstene-3,17-dione is a naturally occurring steroid that is primarily, if not strictly, produced in adrenal tissue. In diseases such as Cushing′s syndrome, adrenal-originated hyperandrogenism, and congenital adrenal hyperplasia, plasma 11β levels are very high. Plasma 11β concentration is very low in congenital 11-hydroxylase deficiency and adrenal insufficiency.
 
A8008 5α-Androst-16-en-3-one    
E3375 trans-Androsterone   human ... HSD17B3(3293)
A0612   Anemone Toxin II recombinant from Escherichia coli >95% (HPLC) rATX II is a 47 amino acid peptidyl toxin, originally isolated from Anemonia sulcata sea anemone venom. It is a potent neurotoxin, which modulates voltage-gated Na+ channel gating kinetics by delaying its inactivation and prolonging the action potential of excitable membranes. ATX II has been used as a powerful activator of TTX-sensitive and insensitive Na+ channels in various excitable tissue and cell types (at concentration range of 10-100nM).
 
SML1373 Angiotensin A trifluoroacetate salt ≥98% (HPLC) Angiotensin A (Ang A) is an endogenous vasoconstrictor octapeptide. It is a derivative of angiotensin II (Ang II) that differs from Ang II in having alanine instead of aspartic acid as the first amino acid. Angiotensin A has similar affinity as Angiotensin II for AT1 and AT2 receptors with Ki values of 1.6 and 2.3 nM at AT1 and AT2 receptors.
 
A0773 Angiotensin Converting Enzyme Inhibitor ≥95% (TLC)    
10385 Angiotensin III trifluoroacetate salt hydrate ≥98.0% (HPCE) Angiotensin III is an AT1 and AT2 agonist, with higher sensitivity for the AT2 receptor. Ang III has been shown to be a main effector peptide in RAS-controlled vasopresin release and a stimulator for aldosterone release.
 
A0230 Angiotensin IV trifluoroacetate salt ≥95% (HPLC), powder AT4 angiotensin receptor agonist. The AT4 receptor appears to be important in synaptic plasticity and thus in learning and memory.
 
SML1813 Ani9 Ani9 is a potent and highly selective anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A) inhibitor that completely inhibited ANO1 chloride current with submicromolar potency. Ani9 does not affect the intracellular calcium signaling and CFTR chloride channel activity.
 
A6563 6-Anilinoquinoline-5,8-quinone ≥95% (TLC), solid Blocks cGMP production; inhibits intracellular Ca2+ release; blocks the effects of nitric oxide. Inhibits antigen-induced leukotriene release.
 
A9950 Aniracetam ≥98% Cognition enhancer (nootropic) that potentiates AMPA receptor mediated ion conductance and potentiates metabotropic glutamate receptor activity.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM4(2914), GRM5(2915), GRM6(2916), GRM7(2917), GRM8(2918)
rat ... Gria1(50592)
SML0252 Anisodamine ≥98% (HPLC) Anisodamine is a muscarinic receptor antagonist. Anisodamine is a naturally occurring atropine derivative isolated from Scopolia Tangutica Maxim plant indigenous to Tibet.
 
A9789 Anisomycin from Streptomyces griseolus ≥98% (HPLC), solid Antibiotic isolated from Streptomyces griseolus that inhibits protein synthesis. Acts by inhibiting peptidyl transferase activity in eukaryote ribosomes. Reported to induce apoptosis in a variety of cells including promyelocytic leukemia cells, Jurkat cells, ventricular myocytes, and colon adenocarcinoma cells. Initiates intracellular signals and immediate early gene induction. Selective signaling agonist. Potent Jun-NH2 terminal kinase (JNK) agonist. Activates mitogen-activated protein (MAP) kinases (JNK/SAPK and p38/RK). Antiprotozoal agent.
 
SML1515 Anle138b ≥98% (HPLC) Anle138b is a fluorescent inhibitor of α-synuclein and prion-protein (PrPSc) aggregation that reduces the progression of prion and Parkinson′s disease in animal models. Anle138b extends the survival of mice infected with prions. Anle138b strongly inhibits BSE-derived and human prions. The fluorescence strongly increases upon binding with α-synuclein fibrils. Apparently, Anie138b binds to hydrophobic pockets in the fibrils.
 
SML0728   ANR-94 ≥98% (HPLC) ANR-94 is a potent antagonist of the adenosine A2A receptor (AA2AR). The Ki for human AA2AR is 46 nM. ANR-94 displays neuroprotective properties in rat models of Parkinson′s disease. ANR-94 reverses GABA-A receptor desensitization in oocyte and neuronal electrophysiological preparations.
 
A8727 Antalarmin hydrochloride ≥98% (HPLC), solid Antalarmin hydrochloride is a non-peptide CRF1 corticotropin-releasing factor receptor antagonist.
 
A9899 Antazoline hydrochloride Imidazoline agonist; more potent than efaroxan in inducing insulin release from β cells; H1 histamine receptor antagonist.
human ... HRH1(3269)
A7475   Anthopleurin-A >88% (HPLC) Shown to have inotropic effects and not chronotropic effects on mammalian heart preparations.
 
A8674 Antimycin A from Streptomyces sp. Inhibitor of electron transfer at complex III. Induces apoptosis.
 
SML0250 anti-3-OS HS peptide trifluoroacetate salt ≥98% (HPLC) MPRRRRIRRRQK is an anti-3-OS HS peptide that binds 3-O sulfated heparan sulfate (3-OS HS) and prevents HSV-1 infection in vivo and in cell culture. It also prevents entry of other members of herpesviruses family including cytomegalovirus (CMV) and human herpesvirus-8 (HHV-8). MPRRRRIRRRQK exhibits protective effects against HSV-1 infection of the mouse cornea.
 
SML0568   3-AP ≥98% (HPLC) 3-Aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) is a ribonucleotide reductase inhibitor and iron chelator with anti-tumor activity.
 
A7232 AP-18 ≥98% (HPLC), solid AP-18 is a selective TRPA1 channel blocker. Transient receptor potential A1 (TRPA1) plays a central role for chemical sensing in the pain pathway. AP-18 is a novel TRPA1 channel blocker. It reduces cinnamaldehyde-induced nociception in vivo and blocks cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation demonstrating selectivity vs. TRPV11. AP-18 reverses CFA-induced mechanical hyperalgesia in mice.
 
SML1503 Apcin ≥98% (HPLC) Apcin is an inhibitor of the anaphase-promoting complex/cyclosome (APC/C), a large multimeric complex that functions as a ubiquitin ligase, initiating the metaphase–anaphase transition and regulating ordered transitions through the cell cycle by controlling the ubiquitin-mediated proteolysis of cell cycle proteins. Apcin prevents substrate recognition and inhibits APC/C-dependent ubiquitylation by binding to the D-box binding site of Cdc20, a coactivator required for full activation of APC/C and substrate recognition. The effectiveness of apcin in blocking mitotic exit was synergistically amplified by co-addition of TAME (tosyl-L-arginine methyl ester) or its cell permeable prodrug proTAME, which block Cdc20 binding to the APC/C at a different site than apcin.
 
A7361 2R, 4R-APDC monohydrate ≥98% (HPLC) 2R,4R-APDC is a Group II mGluR metabotropic glutamate receptor.
 
A0781 Aphidicolin from Nigrospora sphaerica ≥98% (HPLC), powder Aphidicolin is an antibiotic, a potent antiviral and antimitotic agent and DNA polymerase inhibitor.
human ... POLA1(5422), POLD1(5424), POLG(5428)
SML1342 API-1 API-1 is a potent and specific Akt/PKB inhibitor. API-1 binds to pleckstrin homology (PH) domain of Akt and blocks Akt membrane translocation. The compound inhibits all three members of the family Akt1/PKBa, Akt2/PKBb and Akt3/PKBg. API-1 does not inhibit the activation of PKC, SGK, PKA, STAT3, Erk-1/2 or JNK.
 
A8851 Apicidin ≥98% (HPLC), from microbial Apicidin is a cyclic tetrapeptide that inhibits histone deacetylase. Apicidin has antiproliferative activity on various cancer cell lines and HeLa cells, accompanied by cell arrest at the G1 phase. It has been shown to induce selective changes in the expression of p21 and gelsolin, induce apoptosis in HL60 cells, and exhibit antiprotozoal, antiparasitic, and potential antimalarial properties.
 
SML1055 3-AP-Me ≥98% (HPLC) 3-AP-Me is a dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me is a potent inducer of ER stress and the unfolded protein response in cancer cell lines, incuding IRE1, PERK and ATF6 activity. Treatment with 3-AP-Me induces CHOP expression, phosphorylation of eIF2α, up-regulation of ATF4 and Bim, and causes mitochondrial membrane depolarization and apoptosis.
 
A7785 Apolipoprotein C-I from human plasma ≥95% (SDS-PAGE), lyophilized powder Interferes directly with fatty acid uptake and is the major plasma inhibitor of cholesterol ester transfer protein.
human ... APOC1(341)
A7910   Apolipoprotein C-II from human plasma ≥95% (SDS-PAGE) Activates lipoprotein lipase
human ... APOC2(344)
A4393 R-(−)-Apomorphine hydrochloride hemihydrate calcined, ≥98.5% Nonselective dopamine agonist; causes nausea and emesis.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
SML0907 Apoptolidin A Ready Made Solution 1 mg/mL in DMSO Apoptolidin A is a 20-membered macrolide shown to be selectively cytotoxic against several cancer cell lines and noncytotoxic against normal cells. The molecule was originally produced by Nocardiopsis species, and its target site was identified as mitochondrial F0F1-ATPase.
Apoptolidin induces apoptosis selectively in rat glia cells transformed with the adenovirus oncogene E1A. Several minor apoptolidin congeners were isolated, known as Apoptolidins A-D. All apoptolidins were reported to inhibit growth of H292 cancer cells (lung carcinoma) in the submicromolar range. Recently, a stereo-selective synthesis of the Apoptolidin disaccharide was reported.
 
B3055   Apoptosis PCR Primers Bad primers    
F8425   Apoptosis PCR Primers FAS primer set    
F8300   Apoptosis PCR Primers Fas-Ligand primers    
SML1543 Apratastat ≥98% (HPLC) Apratastat (TMI-005) is an orally active, potent and selective dual inhibitor of disintegrin metalloenzyme 17 (ADAM17/ TACE) and matrix metalloprotease (MMP).
 
A7606 Aprindine hydrochloride ≥98% (HPLC), solid Aprindine hydrochloride is a class Ib antiarrhythmic and hERG channel blocker. Aprindine shows structure similarities to lidocaine and procainamide and is effective in treatment of patients with ventricular premature depolarizations, ventricular tachycardia, and supraventricular arrhythmias. Aprindine inhibits the activation of bovine brain cyclic 3′:5′-nucleotide phosphodiesterase (EC 3.1.4.17) by calmodulin and inhibits calmodulin-stimulated Ca-ATPase (ATP phosphohydrolase EC 3.6.1.3) activity.
 
SML1805 APS-2-79 hydrochloride ≥98% (HPLC) APS-2-79 is a stabilizer of the Kinase suppressor of Ras (KSR) inactive state, resulting in inhibition of oncogenic Ras signaling, antagonizing the Ras–MAPK pathway. KSR is a MAPK scaffold that is regulated allosterically by dimerization with RAF. APS-2-79 was found to bind to the KSR active site with an IC50 value of 120 nM, antagonizing MEK (MAPKK) phosphorylation by RAF. In Ras mutant cell lines, APS-2-79 increased the potency of several MEK inhibitors..
 
A9236 AQ4 ≥98% (HPLC) AQ4 is a chemically stable cytotoxic agent which acts as a topoisomerase II inhibitor and DNA intercalator. The compound is a potent cytotoxic agent in many human tumor lines, including those derived from human pancreatic adenocarcinomas. The compound N-oxide is a hypoxia activated prodrug of topoisomerase-targeting.
 
SML1339 AR420626 ≥98% (HPLC) AR420626 is a selective agonist of Free Fatty Acid 3 receptor FFA3 (previously called GPR41). FFA3 is expressed in adipose tissue, gut, and the peripheral nervous system and normally activated by short chain fatty acids (SCFAs) produced in the body through the fermentation of complex carbohydrates by the gut microbiota. There is increasing interest in the role of the various free fatty acid receptors and SCFAs as chemical messengers in energy regulation and regulation of inflammatory processes and as therapeutic targets in the treatment of various metabolic and inflammatory conditions. AR420626 has an EC50 value of 117 nM for FFAR3 and did not activate FFAR2 in concentrations up to 100 μM.
 
SML0921   AR7 ≥98% (HPLC) AR7 is an atypical retinoic acid receptor α (RARα) antagonist. There is high interest in retinoic acid receptors for cancer and for differentiation studies. Recently, it has been found that signaling through retinoic acid receptor α (RARα) inhibits chaperone-mediated autophagy (CMA). Disruption of RARα signaling has a stimulatory effect on CMA, but can lead to inhibition of macroautophagy. AR7 antagonizes only the CMA inhibitory effect without affecting macroautophagy, allowing the two RARα effects on autophagy to be studied independently.
 
A4233 Ara-G hydrate ≥98% (HPLC), solid Ara-G is an inducer of apoptosis; inhibitor of DNA synthesis; antineoplastic; and antimetabolite. Ara-G is converted by cellular kinases to the active 5′-triphosphate, Ara-GTP. Incorporation of Ara-GTP into DNA leads to inhibition of DNA synthesis and apoptosis.
 
A3230 AR-A014418 ≥98% (HPLC), solid Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.
 
A8798 Arachidonic acid sodium salt from porcine liver, ≥99% (capillary GC), waxy solid Released arachidonic acid (AA) reacts with molecular oxygen nonenzymatically, through oxidative stress, and enzymatically through the action of oxygenase enzymes. AA is oxidized to prostaglandins and thromboxanes by at least two cyclooxygenase (COX) isoforms, to leukotrienes and lipoxins by lipoxygenases, and to epoxyeicosatrienoic acids via cytochrome p450-catalyzed metabolism. Cellular uptake of AA is energy dependent and involves protein-facilitated transport across the plasma membrane.
 
SML1395 Arachidonic acid sodium salt from Mortierella alpina ≥98.5% (GC) Released arachidonic acid (AA) reacts with molecular oxygen nonenzymatically, through oxidative stress, and enzymatically through the action of oxygenase enzymes. AA is oxidized to prostaglandins and thromboxanes by at least two cyclooxygenase (COX) isoforms, to leukotrienes and lipoxins by lipoxygenases, and to epoxyeicosatrienoic acids via cytochrome p450-catalyzed metabolism. Cellular uptake of arachidonic acid is energy dependent and involves protein-facilitated transport across the plasma membrane.
 
A8848 Arachidonoyl dopamine ≥98% (HPLC), ethanol solution AA-DA competitively inhibits fatty acid amide hydrolase (IC50 = approx. 22 μM) from N18TG2 neuroblastoma cells and inhibits binding (Ki = 0.25 μM) of the selective cannabinoid receptor subtype 1 (CB1) ligand, [3H]SR141716A, to rat brain membrane. AA-DA also inhibits the anandamide membrane transporter in BL-2H3 basophilic leukemia and C6 glioma cells. AA-DA has at least a 40 fold greater selectivity for CB1 than CB2 receptors in rat brain membranes and has been shown to be more potent than anandamide as a CB1 agonist in undifferentiated N18TG2 neuroblastoma cells. AA-DA induces hypothermia and immobility, and decreases spontaneous activity and pain perception in mice and rats, which supports its action as a CB1 agonist in vivo. AA-DA has been shown to inhibit (IC50 = 0.25 μM) proliferation of human breast MCF-7 cancer cells.
 
A7357 Arachidonoylserotonin ≥98% (HPLC), oil Arachidonoylserotonin is a Fatty Acid Amide Hydrolase (FAAH) Inhibitor and Transient Receptor Potential Vanilloid-Type I (TRPV1) Antagonist. FAAH and TRPV1 are targets for chronic pain treatment. Arachidonylserotonin is a dual target agent and is analgesic in rodents.
 
A9719 Arachidonyl-2′-chloroethylamide hydrate ≥97% (HPLC), oil Potent and selective neuronal CB1 cannabinoid receptor agonist.
mouse ... Cnr1(12801), Cnr2(12802)
rat ... Cnr1(25248)
A8973 2-Arachidonyl glycerol ~10 mg/mL, ≥98% (HPLC) Endogenous cannabinoid receptor agonist.
human ... FAAH(2166)
rat ... Cnr1(25248), Cnr2(57302)
A2984 N-Arachidonylmaleimide ≥98% (HPLC) N-Arachidonylmaleidmide (NAM) is structurally similar to the MAGL substrate 2-AG and displays a high potency for inhibition of MAGL. It is thought that NAM binds MAGL at the substrate binding site and inhibits enzyme activity through the Michael addition reaction at the Cys201, and to a lesser extent Cys242, residue of MAGL. In cerebellar rat membranes, NAM inhibits MAGL-like activity with an IC50 of 140 nM.
 
A231 Arachidonyl trifluoromethyl ketone oil, ≥97% (NMR) Inhibits anandamide hydrolysis in vitro; inhibits phospholipase A2.
human ... PLA2G1B(5319)
SML0860   Arbidol hydrochloride ≥98% (HPLC) Arbidol is a broad-spectrum antiviral that has demonstrated activity against a number of enveloped and non-enveloped viruses, and is used clinically to treat influenza. Arbidol inhibits viral entry into host cell and stimulates immune response. Arbidol inhibits fusion between the viral capsid and the cell membrane of the target cell, thus preventing viral entry.

































































































































































































































































































































































































Arbidol is a broad-spectrum antiviral that has demonstrated activity against a number of enveloped and non-enveloped viruses, and is used clinically to treat influenza. Arbidol inhibits viral entry into host cell and stimulates immune response. Arbidol inhibits fusion between the viral capsid and the cell membrane of the target cell, thus preventing viral entry.
 
A5736 ARC 239 dihydrochloride hydrate ≥98% (HPLC) ARC 239 is a selective α-2B adrenergic blocker. Although ARC-239, like prazosin, also has some alpha-1 antagonist activity, it is used most commomly to differentiate alpha-2A/D from alpha-2B and alpha-2C subtypes rather than for any alpha-1 inhibition..
 
A0384 Arcaine sulfate salt Potent antagonist at the polyamine site of the NMDA glutamate receptor.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRINA(2907)
A140 Arecaidine propargyl ester hydrobromide solid Potent muscarinic acetylcholine receptor agonist exhibiting slight selectivity for M2 receptors; inactive at nicotinic receptors.
human ... CHRM2(1129)
SML1667 Arformoterol tartrate ≥98% (HPLC) Arformoterol is the active isomer of formoterol. Arformoterol is a selective β2-adrenergic receptor agonist, a long-acting beta adrenergic agonist (LABA). Arformoterol is a bronchodilator used clinically as an anti-asthmatic and for treatment of chronic obstructive pulmonary disease (COPD).
 
A4602 Arg-Arg-Ala-pSer-Pro-Val-Ala ≥95% (HPLC) The phosphoseryl peptide RRApSPVA can provide a sensitive evaluation of the majority of acid and alkaline phosphatases, while being refractory to protein phosphatases.
 
A0487   Argatroban monohydrate ≥98% (HPLC) Argatroban is a potent, seletive, univalent direct inhibitor of thrombin. It directly inhibits thrombin by binding only to its active site (thus univalent) as compared to Bivalent DTIs (hirudin and analogs) which bind both to the active site and exosite 1.
 
A6757 D-Arginine monohydrochloride ≥98% (TLC)    
SML1570   Arglabin ≥98% (HPLC) Arglabin is a natural product with antitumor and anti-inflammatory activity. Arglabin competitively inhibits the binding of farnesyl diphosphate to farnesyl transferase (FTase), preventing the activation of RAS proto-oncogene by preventing the incorporation of farnesyl pyrophosphate into human H-ras proteins. Arglabin is also an inhibitor of the NLRP3 inflammasome. Arglabin reduces inflammation and plasma lipids and has shown a marked reduction in atherosclerotic lesions.
 
SML0935   Aripiprazole ≥98% (HPLC) Aripiprazole is a second generation atypical antipsychotic and anti-depressant with partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors. Ki values are 0.34 nM, 0.8 nM, 1.7 nM, and 3.4 nM, respectively, for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors.
 
A5512 Aristolochic acid I powder Potent phospholipase A2 inhibitor, including calcium ionophore-induced phospholipase A2 activity in neutrophils. Kidney tumor initiator in experimental animal model.
 
SML0178 ARL-17477 dihydrochloride hydrate ≥98% (HPLC) ARL-17477 is an nNOS specific inhibitor. The IC50 against rat nNOS is 35 nM and it has 100-fold selectivity over endothelial and inducible isoforms. ARL-17477 penetrates the brain, and reduces infarct size and reduces cerebral blood flow in several different rodent models of ischemic brain injury.
 
A265 ARL 67156 trisodium salt hydrate ≥98% (HPLC), solid ecto-ATPase inhibitor; prevents metabolism of P2 purinoceptor agonists.
human ... ENTPD2(954)
SML0039 Armodafinil ≥98% (HPLC) Armodafinil has affinity for dopamine transporters and inhibits the uptake of dopamine in brain areas that are involved in the cognitive performances. It is beneficial for the patients of substance abuse and mental disorders.
Armodafinil is the R isomer and longer-lasting isomer of racemic modafinil. It is a psychostimulant wake-promoting agent developed for the treatment of narcolepsy, shift work sleep disorder and excessive daytime sleepiness associated with obstructive sleep apnea
 
A8356 ARP 101 ≥98% (HPLC), solid ARP 101 is a MMP-2 selective inhibitor (Gelatinase A, EC 3.4.24.24; TBE-1; LG4A; MONA; Type IV Collagenase). ARP 101 has diverse physiological roles including wound healing, cancer metastasis, angiogenesis, tissue remodeling in development and embryogenesis. IC50 = 0.81 nM on MMP-2.
 
A9361 Artemether ≥98% (HPLC) Artemether is a methyl ether derivative of artemisinin. It is used against multi-drug resistant strains of the malaria parasite, Plasmodium falciparum, and shows potential in treatment of schistosomiasis.
 
SML1093 Articaine hydrochloride ≥98% (HPLC) Articaine is an amide local anesthetic widely used in dentistry. Articaine acts by inhibition of nerve impulse conduction by blockade of sodium channels.
 
SML0520 Arvanil ≥98% (HPLC), solution (in ethanol) Arvanil is an activator of cannabinoid and vanilloid receptors, and a potent inhibitor of anandamide accumulation. Arvanil inhibits growth of astrocytoma xenograft tumors in mice, mimicing the effect of neural precursor cells, that have been shown to kill TRPV1-expressing tumor cells by secreting endovanilloids.
 
SML1263 Arylquin 1 ≥98% (HPLC) Arylquin 1 is a potent secretagogue of the tumor suppressor protein prostate apoptosis response-4 (Par-4), selectively inducing apoptosis in a variety of cancer cells. Arylquin 1 acts by binding to vimentin, displacing Par-4 from vimentin for secretion. Arylquin 1 produced a dose-dependent secretion of Par-4 at nanomolar concentrations.
 
A6486 AS-136A ≥98% (HPLC) AS-136A is a potent measles virus RdRp inhibitor. Measles virus (MV) is a member of the paramyxovirus family. Ribavirin (R9644) is the only drug available for treatment of paramyxoviruses, and it has limited efficacy against MV. A series of small molecules has been developed to inhibit viral RNA-dependent RNA polymerase (RdRp), a protein vital to infection leading to the development of AS-136A, a very potent RdRp inhibitor. AS-136A has high stability and continues to decrease virus titer after 24 hours in physiologic conditions. AS-136A is now used as a positive control in experiments assaying MV inhibition. This compound is a product of the NIH Probes effort, also known as SID 24769845.
 
SML1906 AS1517499 ≥98% (HPLC) AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor (IC50 = 21 nM against IL-4-dependent reporter activity) that selectively prevents anti-CD3- & IL-4-induced T-helper cell 2 (Th2) differentiation of mouse spleen T cells (IC50 = 2.3 nM), without affecting anti-CD3- & IL-12-induced Th1 differentiation. AS1517499 in vivo effecicacy is demonstrated in various animal models of immunological disorders, including the autoimmune Graves’ disease, antigen-induced bronchial hypercontractility (10 mg/kg i.p.). AS1517499 treatment (10 mg/kg/day i.p.) following early gliomagenesis blockage by a CSF-1R inhibitor is also shown to greatly prolong the survival rate when compared with CSF-1R inhibition alone in a murine model of PDGF-driven glioma (PDG).
 
SML1022   AS1949490 ≥98% (HPLC) AS1949490 is a potent, selective SHIP2 phosphatase inhibitor. AS1949490 activates insulin signaling pathways in liver and lowers glucose levels in diabetic mice.
 
SML1643 AS2444697 ≥98% (HPLC) AS2444697 is a potent and selective inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK-4) that suppresses the progression of chronic renal failure via anti-inflammatory action.
 
A8981 AS-252424 ≥98% (HPLC), solid AS-252424 is a potent and selective phosphoinositide 3-kinase PI3Kγ inhibitor with IC50 = 30 nM in a mouse model.
 
A0231 AS 604850 ≥98% (HPLC), solid AS 604850 is a selective PI3Kγ inhibitor
 
A0233 AS605240 ≥98% (HPLC) AS605240 is a potent and selective PI3Kγ inhibitor.
 
SML1692 AS8351 ≥98% (HPLC) AS8351 is an iron chelator that has been found to inhibit of histone demethylase KDM5B (JARID1B), a histone H3K4 demethylase involved in regulation of cell proliferation and stem cell self-renewal and differentiation. AS8351 is thought to inhibit KDM5B by competing with a-ketoglutarate for chelating iron that KDM5B requires as a co-factor.
 
SML1913 ASB14780 ≥98% (HPLC) ASB14780 is an indole-based selective and potent cytosolic phospholipase A2α inhibitor (IC50 = 20 nM/cPLA2α and >10 μM/sPLA2α). ASB14780 inhibits cPLA2α-dependent inflammatory responses both in cultures and in animals in vivo, including LPS-induced PGE2 production (IC50 = 0.5 μM; mouse peritoneal exudate cells), A23187-induced TXB2 production (IC50 = 0.54 and 0.64 μM using guinea pig and human whole blood, respectively), TPA-induced ear edema (50 mg/kg, p.o.; mice), OVA-induced asthma (5 - 20 mg/kg/d, p.o.; guinea pig), CCl4-induced hepatic fibrosis and high-fat cholesterol diet-induced fatty liver (0.1-0.3 g/kg/d, p.o.; mouse). SB14780 bioavailability is also demonstrated in dog and monkey, albeit at a lower value (F = 34.3%/dog and 30.9%/monkey vs. 89.6%/mouse).
 
SML0104   Ascochlorin ≥98% (HPLC), from Verticillium hemipterigenum Ascochlorin is an isoprenoid antibiotic produced by Verticillium hemipterigenum, initially identified as an antiviral and antitumor agent. Research also indicates that ascochlorin inhibits the Qi and Qo quinone binding sites of the mitochondria cytochrom bc1 complex. Moreover, ascochlorin activates p53, probably as a result of its inhibitory effect on mitochondrial respiration. In addition, ascochlorin has the ability to suppress the nuclear subscription enzyme protein-1, a nuclear transcription factor activator, which leads to suppression of the extra-cellular enzyme, matrix metalloproteinase-9 (MMP9). The regulation of MMP is implicated in renal development, macrophage differentiation, atherosclerosis, inflammation, rheumatoid arthritis, and tumor invasion. Ascochlorin was also found to be effective against Mx-1, an estrogen lacking breast cancer cell line.
 
A3835 Ascomycin from Streptomyces hygroscopicus var. ascomyceticus Green Alternative Strong immunosuppressant; inhibits allogenic T-lymphocyte proliferation. It binds with high affinity to FKBP and inhibits calcineurin phosphatase in the nM range.
 
A7861 Asenapine maleate ≥98% (HPLC) Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.
 
G3018   Asialoganglioside GM1 from bovine brain ~98%, lyophilized powder Removing the sialic acid from monosialoganglioside GM1 inhibits its ability to bind cholera toxin. Asialoganglioside GM1 does not block the binding of cholera toxin to cellular GM1.
 
G9398   Asialoganglioside-GM2 from bovine brain ~95%, lyophilized powder Degraded form of Asialoganglioside-GM1 ganglioside.
 
SML1261 Asimadoline hydrochloride ≥98% (HPLC) Asimadoline is a potent and selective κ-opioid agonist that does not penetrate the blood-brain barrier. Asimadoline produces both analgesic and antidiarrheal effects.
 
SML1690 ASMI ≥98% (HPLC) ASMI is a cell-permeable, non-toxic, biocompatible, photostable, positively charged, mitochondria targeting styryl-methylpyridinium based compound that acts as a rapid, cysteine selective, sensitive, and ratiometric (F 518 /F 452  nm) fluorescent turn-on probe (0.5 - 40 μM of [Cys]). Under physiological conditions, cysteine thiol reacts with the ASMI acrylate moiety in a time-dependent manner, and induces a facile intramolecular cyclization to release fluorogenic oxystyryl methylpyridinium. ASMI displays high selectivity over other biothiols (Kobs  = 0.75, 0.038, 0.011 & 0.012 min -1  for Cys, Hcy, GSH & Na 2 S, respectively) and with no interference from other biologically relevant amino acids, essential metal ions, and anions, including Na2S. Shown to monitor mitochondrial Cys levels in HeLa cells and in deep tissues (150 μm of penetration depth) by two-photon excited fluorescence microscopy.
 
11260 L-Aspartic acid hemimagnesium salt dihydrate ≥98.0% (KT)    
A6558 L-Aspartic acid potassium salt ≥98% (HPLC) Principal neurotransmitter for fast synaptic excitation.
 
11230 L-Aspartic acid potassium salt puriss. p.a., ≥99.0% (anhydrous basis) Aspartic acid is a non-essential amino acid. It is involved in the Urea cycle, Krebs cycle and in DNA metabolism.
Principal neurotransmitter for fast synaptic excitation.
 
SML0982   Astaxanthin ≥97% (HPLC), from Haematococcus pluvailis Astaxanthin is a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin protects against oxidative stress, inhibiting NF-KB, suppressing pro-inflammatory genes and suppressing production of pro-inflammatory compounds nitric oxide, prostaglandin E2, TNF-α, and interleukin-1β. Astaxanthin′s protection of cells from oxidative stress generated by TNF-α and palmitate has been shown to ameliorate insulin resistance. Astaxanthin has also been shown to be an inhibitor of PPARγ.
 
A2861 Astemizole ≥98% (HPLC) Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.
 
SML0856   AT-56 ≥98% (HPLC) AT-56 is a selective orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. PGD2 is a lipid signaling molecule, which activates two receptors, DP1 involved in centrally mediated processes such as sleep and pain, and DP2 involved and inflammation. The two PGD synthases involved in its synthesis are hematopoietic (H-PDGS) and lipocalin-type (L-PGDS), which acts to form PGD2 in the CNS and other systems but not in inflammatory cells/tissues. AT-56 binds competitively at the enzyme′s catalytic pocket, and has no effect on the production of other PGs or H-PDGS-catalyzed PDG2. AT-56 inhibited PGD2 production by L-PGDS-expressing human TE-671 cells with an IC50 value of 3 μM without affecting production of PGE2 and PGF2, but had no effect on the PGD2 production by H-PGDS-expressing human megakaryocytes.
 
SML0433   AT101 ≥98% (HPLC) AT101 [R-(-)-enantiomer of gossypol] is an orally available and well-tolerated natural BH3-mimetic that activates Bax and also induces mitochondrial Smac release. AT101 has shown anti-tumor activity as a single agent and in combination with standard anticancer drugs in a variety of tumor models. AT101 induced apoptosis in chemoresistant ovarian cancer cells.
 
SML1796 Atazanavir ≥98% (HPLC) Atazanavir is an antiviral HIV protease inhibitor.
 
A3355 ATC0175 ≥98% (HPLC), solid ATC0175 is a non-peptide, orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.
Non-peptide, orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.
 
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
human ... ADRB1(153)
rat ... Adrb1(24925)
A143 (S)-(−)-Atenolol powder β1-Adrenergic receptor antagonist; active enantiomer of atenolol.
human ... ADRB1(153)
SML1720   ATI-2341 trifluoroacetate salt ≥95% (HPLC) ATI-2341 is a potent and selective allosteric agonist of chemokine CXC-type receptor 4 (CXCR4) that functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 does not promote β-arrestin recruitment. ATI-2341 promotes the mobilization of PMNs and HSPCs in the peripheral circulation of both mice and monkeys.
 
A9611 Atipamezole ≥98% (HPLC) Atipamezole is a selective α2 adrenergic blocker. Atipamezole is more potent than yohimbine; it is very selective for α2 adrenergic vs α1 sites, but not selelctive for α2 subtypes.
 
PZ0001 Atorvastatin calcium salt trihydrate ≥98% (HPLC) Atorvastatin calcium salt trihydrate is a specific inhibitor of HMG-CoA reductase. HMG-CoA reductase is the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. Atorvastatin is used in the treatment of hypercholesterolemia.
 
A3480 Atosiban ≥98% (HPLC) Atosiban is a peptide oxytocin receptor antagonist.
human ... AVPR1A(552), OXTR(5021)
rat ... Oxtr(25342)
A7986 Atovaquone ≥98% (HPLC) Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor; Antimalarial; Antipneumocystic, and has also been used to treat toxoplasmosis. It is an analog of protozoan mitochondrial protein ubiquinone, and acts by inhibiting the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket.
 
A263 ATPA solid Selective kainate receptor agonist.
human ... GRIK1(2897)
rat ... Gria1(50592), Grik1(29559), Grin2a(24409)
SML1041   Atreleuton ≥98% (HPLC) Atreleuton is a reversible 5-lipoxygenase inhibitor. Atreleuton exhibits potent and selective inhibition of leukotriene formation both in vitro and in vivo.
 
A0132 Atropine ≥99% (TLC), powder Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM4(1132), CHRM5(1133), LOC730413(730413)
mouse ... Chrm1(12669)
rat ... Chrm1(25229), Chrm2(81645), Chrm3(24260), Drd2(24318), Htr1a(24473)
SML0732   Atropine methyl nitrate ≥98% (HPLC) Atropine methyl nitrate is a muscarinic acetylcholine receptor antagonist that does not cross the blood brain barrier. Atropine methyl nitrate has been used for its peripheral muscarinic effects (bladder, respiratory, to block parasympathetic signaling to the heart, etc.) and to separate central from peripheral effects or protect against peripheral side effects when using muscarinics that do cross the blood brain barrier.
 
A0981   ATX II recombinant, expressed in E. coli, ≥98%, lyophilized powder rATX II is a 47 amino acid peptidyl toxin, originally isolated from Anemonia sulcata sea anemone venom. It is a potent neurotoxin, which modulates voltage-gated sodium channel gating kinetics by delaying its inactivation and prolonging the action potential of excitable membranes. ATX II has been used as a powerful activator of TTX-sensitive and insensitive sodium channels in various excitable tissue and cell types (at concentration range of 10-100 nM).
 
SML0177 AUDA ≥98% (HPLC) AUDA is a potent inhibitor of soluble epoxide hydrolase
Inhibition of soluble epoxide hydrolase by AUDA inhibits the metabolism of epoxyeicosatrienoic acids (EETs) and protects end-organs against the damaging effects of salt-sensitive hypertension. AUDA also renders protection against myocardial ischemia-reperfusion injury and cerebral ischemia.
 
A6733 Auranofin ≥98% (HPLC) Auranofin inhibits various leukocyte activation pathways at multiple sites. Auranofin inhibits the release of inflammatory mediators from human macrophages, basophils, and pulmonary mast cells. The compound also inhibits 5-lipoxygenase in human neutrophils. Auranofin is a disease-modifying antirheumatic drug (DMARD). The compound is a potent inhibitor of selenoenzyme thioredoxin reductase (TrxR), which is involved in defense against oxidative stress. Auranofin is an efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions related to its inhibition of mitochondrial thioredoxin reductase. Auranofin inhibits IKB kinase (IKK) by modifying Cys-179 of the IKKβ subunit 5.
 
A9861 Auraptene ≥98% (HPLC) Auraptene is an estrogen receptor modulator that also acts as an ACAT inhibitor. It displays anti-tumor effects in several xenograft and chemically-induced murine tumor models. Auraptene induces apoptosis and is anti-proliferative in cancer cell lines. It has agonistic properties against PPARs, and interferes with lipid and cholesterol production by inhibiting ACAT (IC50 = 4 uM).
 
SML0882   Aurora-A Inhibitor I ≥98% (HPLC) Aurora-A Inhibitor I is a potent inhibitor of Aurora kinase A with an IC50 of 3.4 nM and 1000-fold selectivity for Aurora A over Aurora B (better than VX-680) and even higher for CDKs. Antiproliferative IC50 values were in the vicinity of 1 μM against the human colorectal cancer cell line HCT116.
 
A0606 Aurothioglucose hydrate ≥96% (titration) Aurothioglucose, a gold compound used clinically to treat rheumatoid arthritis, has recently been found to be a potent PKCiota-Par6 interaction inhibitor, with an IC50 approximately 1 μM. Disruption of this interaction disrupts a rac1 signaling pathway that is required for transformed growth in non-small-cell lung cancer.
 
BM0005 Avagacestat ≥98% (HPLC) Avagacestat (BMS-708163) is a potent γ-secretase inhibitor selective for amyloid precursor protein (APP) over Notch cleavage. Avagacestat inhibits Aβ40 and Aβ42 production with IC50 values of 0.3 nM and 0.27 nM, respectively, compared to IC50 values of 41, 10, 33, and 38 nM respectively for signaling inhibition of the human Notch 1-4 proteins. At higher concentrations BMS-708163 has been found to reverse sensitivity to the EGFR tyrosine kinase inhibitor gefitinib, thought to be by Notch inhibition.
 
PZ0190 Avasimibe ≥98% (HPLC) Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor. It was originally developed as an antilepic drug, and was shown to significantly reduce plasma total triglyceride and VLDL-cholesterol, but later clinical trials were disappointing. ACAT has also been investigated as a potential therapeutic target for Alzheimer′s disease. Recent studies have looked at the effects of avasimibe in reducing amyloid pathology by limiting generation and increasing clearance of diffusible amyloid-beta (Abeta).
 
BM0009   Avitriptan fumarate ≥98% (HPLC) Avitriptan fumarate is a serotonin 5HT-1B/1D-receptor agonist with anti-migraine activity.
 
PZ0123 Avridine ≥97% (HPLC) Avridine is a potent synthetic adjuvant that can induce arthritis in most rat strains; immunomodulator and interferon-inducing.
 
PZ0193 Axitinib ≥98% (HPLC) Axitinib (AG-013736) is an orally available, potent (picomolar) and selective tyrosine kinase inhibitor that blocks VEGF receptors 1, 2 and 3. The drug blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase.
 
A7231   AZ11645373 ≥98% (HPLC), solid AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
 
SML1429 AZ12216052 ≥98% (HPLC) AZ 12216052 is positive allosteric modulator of mGluR8 receptors that reduced measures of anxiety in wild-type male mice.
 
SML1089 AZ191 ≥98% (HPLC) AZ191 is a cell permeable, potent and selective inhibitor of DYRK1B that promotes a G1 cell cycle arrest.
 
SML1328 AZ20 ≥98% (HPLC) AZ20 is cell penetrant potent and selective ATR (ataxia telangiectasia and Rad3-related protein) kinase inhibitor that potently inhibits the growth of LoVo colorectal adenocarcinoma xenografts in mice.
 
SML1427 AZ3146 ≥98% (HPLC) AZ3146 is a potent and specific inhibitor of monopolar spindle 1 kinase (Mps1; IC50 = 35 nM), an important regulator of Spindle Assembly Checkpoint (SAC). AZ3146 treated HeLa cells override SAC, and quickly enter mitosis, with a reduced mitosis completion time of 32 minutes. 50% of treated cells entered anaphase without complete chromosomal alignment.
 
SML0452 AZ513 ≥98% (HPLC) AZ513 is a reversible, noncompetitive FAAH inhibitor. It also binds non-competitively at a site distinct from the catalytic site. AZ513 is 20-fold more potent against rat FAAH (IC50 27 nM) than the human form (IC50 551 nM).
 
SML0785   AZ628 ≥98% (HPLC) AZ628 is a potent Raf kinase inhibitor with IC50 values of 105 nM for wild-type B-raf, 34 nM for Raf-B V600E and 29 nM for wild-type c-Raf-1. AZ628 is a type II inhibitor that binds to the catalytically inactive Asp-Phe-Gly (DFG)-out configuration.
 
A2385 5-Azacytidine ≥98% (HPLC) A potent growth inhibitor and cytotoxic agent; inhibits DNA methyltransferase, an important regulatory mechanism of gene expression, gene activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes.
human ... DNMT1(1786), DNMT3A(1788), DNMT3B(1789)
A3656 5-Aza-2′-deoxycytidine ≥97% 5′-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression.
 
A3734 1-Azakenpaullone ≥97% (HPLC) 1-Azakenpaullone is a cell permeable, potent, selective inhibitor of glycogen synthase kinase 3β (GSK3β) with 100-fold less cross-reactivity against CDKs. 1-Azakenpaullone can be used together with BIO and CHIR99021 as "gold standards" for GSK3 inhibition.
 
SML0485 Azamulin ≥98% (HPLC) Azamulin is a derivative of the antibiotic pleuromutilin. The compound is a very specific inhibitor of the CYP3A family (IC50 = 0.03-0.24 μM). Azamulin is 15 and 13 fold more active against CYP3A4 compared to CYP3A5 or CYP3A7, respectively, and is at least 100 fold selective over other CYP isoforms, with the exception of CYP2J2 (approximately 50-fold).
 
SML0268 AZD1152-HQPA ≥98% (HPLC) AZD1152-HQPA is the active metabolite of AZD-1152, a potent selective Aurora Kinase B inhibitor. AZD1152 is 50-fold selective for Aurora kinase B over Aurora kinase C and over 1000-fold selective for Aurora kinase B over Aurora Kinase A. (IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L). It is converted in plasma to the active form AZD1152-HQPA, which has been shown to have antineoplastic activity in a variety of animal models and human cancer cell lines.
 
SML1505 AZD1480 ≥98% (HPLC) AZD1480 is an orally active, potent and selective inhibitor of Janus kinases JAK1 and JAK 2 with selectivity for JAK2 as evidenced by IC50 values of 1.3 nM for JAK1 and <0.4 nM for JAK2 in enzyme assays. AZD1480 inhibits endogenous as well as IL-6 induced STAT3 activation. AZD1480 reduces myeloid cell-mediated angiogenesis and metastasis. AZD1489 is an effective anticancer agent in bot adult and pediatric human tumors.
 
SML1858 AZD2461 ≥98% (HPLC) AZD2461, an olaparib analog, is an orally available, potent and selective PARP1 and PARP2 inhibitor that is a poor substrate for drug transporters. AZD2461 exhibits a high efficacy in olaparib-resistant tumors that overexpress P-glycoprotein.
 
SML1855   AZD5438 ≥97% (HPLC) AZD5438 is an orally active, potent and reversible inhibitor against cyclin-dependent kinases (IC50 = 6 nM/Cyc E-CDK2, 14 nM/p25-CDK5, 16 nM/Cyc B1-CDK1, 20 nM/Cyc T-CDK9, 21 nM/Cyc D3-CDK6, 45 nM/Cyc A-CDK2, 449 nM/Cyc D1-CDK4, 821 nM/Cyc H-CDK7; [ATP] = Km) and glycogen synthase kinase GSK-3β≤ (IC50 = 17 nM) without significant inhibitory potency toward 30 other kinases (≤75% inhibition at 10 μM). AZD5438 effectively inhibits cellular CDK substrates phosphorylation and displays antiproliferation activity against a broad spectrum of human cancer cultures (IC50 from 0.2 μM/MCF to 1.7 μM/ARH-77) by inducing cell cycle arrest at G2-M, S, and G1. Oral administration (50 mg/kg/12 h or 75 mg/kg/day) is efficacious against human tumor xenograft growth in mice in vivo.
 
SML0635   AZD6765 dihydrochloride ≥97% (HPLC) AZD6765 is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist and fast-acting antidepressant. In a recent study AZD6765 relieved depression within 80 minutes, unlike most antidepressants acting on serotonin or dopamine systems which can take several weeks to work. The effects lasted from about an hour up to 2 weeks. AZD6765 has an IC50 value of 1.3 μM. Unlike more potent drugs such as ketamine, which also has rapid antidepressant activity, AZD6765 has no dissociative side-effects such as hallucinations. Earlier studies inidcated the compound has neuroprotective and anticonvulsant effects.
 
SML0350 AZD-7762 hydrochloride ≥98% (HPLC) AZD-7762 is a potent, ATP-competitive inhibitor of Chk1 and Chk2 that enhanced cytotoxicity DNA-damaging agents.
 
SML1764 AZD9272 ≥98% (HPLC) AZD9272 is a long acting, CNS penetrant, potent and selective mGluR5 antagonist.
 
A6850 Azelaoyl PAF 10 mg/mL in ethanol Potent PPARγ agonist.
 
A7611 Azelastine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist; NF-kB activator.
 
A7106 Azelnidipine ≥98% (HPLC), powder Azelnidipine, a novel dihydropyridine derivative, is a L-type calcium channel blocker and antihypertensive. Unlike other L-type calcium channel blockers, azelnidipine causes minimal stimulation of the sympathetic nervous system despite its significant depressor effect. Azelnidipine may have a protective role in inflammation in atherosclerosis.
 
A2169 3′-Azido-3′-deoxythymidine ≥98% (HPLC) Azidothymidine (AZT), a thymidine analogue, is a reverse transcriptase inhibitor against the HIV-1 virus. Azidothymidine has been shown to decrease CRISPR-mediated homology-directed repair (HDR) efficiency.
Reverse transcriptase inhibitor active against HIV-1 virus.
human ... HIVE1(3095)
mouse ... Slc29a1(63959)
SML0432 Azilsartan ≥98% (HPLC) Azilsartan is a highly potent and slowly dissociating Angiotensin II type 1 (AT1) receptor blocker (ARB) with an IC50 of 2.6 nM. It is the active form of Azilsartan medoxomil, used for treatment of hypertension. Azilsartan may also have potentially beneficial effects on metabolic syndrome including insulin sensitizing activity that may involve more than just blockade of AT(1) receptors.
 
SML0353 Azimilide dihydrochloride ≥97% (HPLC) Azimilide is an investigational class III anti-arrhythmic drug that blocks fast and slow components of the delayed rectifier cardiac potassium channels. It inhibits KV7.1 and KV11.1 potassium channels. Azimilide′s block of K+ currents is relatively selective for IKr over IKs: It potently blocks the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 mM), and inhibits IKs (IC50 3 mM) with nearly 10-fold less potency. At 10 mM, it does not block the inward rectifier K+ current. It blocks (10 mM) the L-type Ca2+ current (ICa) in a use-dependent manner.
 
75199 Azithromycin analytical standard    
PZ0007 Azithromycin dihydrate ≥98% (HPLC) Azithromycin dihydrate is a macrolide antibiotic, azalide subclass. It binds to the 50S subunit of the 70S bacterial ribosomes and inhibits RNA-dependent protein synthesis in bacterial cells. Azithromycin also has anti-immunomodulatory/anti-inflammatory properties, which make it useful in treating cystic fibrosis.
 
SML0242 AZ-MTAB ≥98% (HPLC) AZ-MTAB is a potent, short acting κ-opioid receptor (KOR) selective antagonist.