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SML0197 4E1RCat ≥97% (HPLC) 4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc.
 
E8534 E3330 ≥98% (HPLC) E3330 is a specific inhibitor of AP endonuclease 1 redox domain. E3330 inhibits APE-1 regulation of transcription factors, but does not affect Ape1 DNA repair activity. AP endonuclease 1 (APE1; also known as REF-1) is a multifunctional protein with dual functions in DNA repair and redox regulation of transcription factors. It is involved in apurinic/apyrimidinic endonuclease DNA base excision repair activity, in proofreading exonuclease activity, and in modulating DNA binding activity of several transcription factors including NF-κB, Egr-1, p53, AP-1, CREB, HIF-α, and members of the Pax family. APE1 is overexpressed in several human cancers, and disruption of APE1 function has detrimental effects on cancer cell viability. E3330 significantly reduces the growth of human pancreatic cancer cells in vitro and inhibits pancreatic cancer cell migration.
 
M5060 E-4031 ≥98% (HPLC), solid E-4031 selectively blocks hERG K+ channels.
 
SML0206 EAA-090 ≥98% (HPLC) EAA-090 inhibits the binding of ligands to glutamate receptors and blocks NMDA-induced currents. It is neuroprotective against glutamate and ischemia-induced toxicity.
EAA-090 is a potent NMDA receptor antagonist with neuroprotective properties. In isoflurane-anesthetized dogs, EAA-090 reduces the minimum alveolar concentration (MAC) of isoflurane and increases systolic, mean, and diastolic arterial blood pressure.
 
SML1157 Eact ≥98% (HPLC) Eact activates the Calcium-activated Chloride channel (CaCC) TMEM16A CaCC. Eact stimulates CaCC conductance in salivary gland cells and submucosal airway epithelial cells. The compound Eact also stimulates submucosal gland secretion in human bronchial tissue and smooth muscle contraction in mouse intestine.
 
E8405 EB-47 ≥98% (HPLC), solid Potent inhibitor of poly (ADP-ribose) polymerase (PARP).
 
SML1727 EB1089 ≥98% (HPLC) EB1089 is a Vitamin D analog 50 to 200 times more potent than Vitamin D in inhibiting growth and inducing differentiation with half the hypercalcemic activity. Studies have found EB1089 to be more potent than vitamin D in inhibiting growth and inducing differentiation of some cancer cell lines. EB1089 enhances radio sensitivity of H460 and A549 non-small cell lung cancer (NSCLC) cells.
 
E9531 Ebastine ≥98% (HPLC), solid Ebastine is a non-sedating histamine H1 receptor antagonist, which inhibits allergen-induced bronchospasm in conscious guinea pigs. Unlike other compounds in this category, ebastine does not prolong the QT interval at up to five times the recommended therapeutic dose.
 
SML0034 1-EBIO ≥98% (HPLC) 1-EBIO is an activator of epithelial Ca2+-activated K+ channel also known as the intermediate-conductance Ca(2+)-activated K(+) channel (IK-1) or KCa3.1.
1-EBIO potentiates the secretion of CFTR-mediated Cl ion secretion by activating the basolateral KCNN4 K+ channels in native human colonic tissues. It stimulates the apical Cl channels and Ca+2-dependent basolateral K+ channels to stimulate fluid transport in lacrimal glands.
 
PZ0140 EBPC ≥98% (HPLC) EBPC is an aldose reductase inhibitor; anti-cancer.
 
SML0419 Ebselen Oxide ≥98% (HPLC) Ebselen oxide is a potent inhibitor of a-Methylacyl coenzyme A racemase (AMACR).
 
E9004 α-Ecdysone ≥90%    
SML0477   Echinomycin ≥98% (HPLC) Echinomycin is an antitumor antibiotic and potent hypoxia inducible factor 1α (HIF-1α) inhibitor. It binds to DNA via bifunctional intercalation, blocking the binding of HIF-1α, a transcription factor important in tumor growth. Echinomycin selectively eliminated cancer stem cells in a study with mouse lymphoma and human AML xenogeneic models, eradicating the lymphomas. Recently, echinomycin was also found to act as an antibiotic adjuvant having synergistic effects with novobiocin in gram negative bacteria.
 
SML0332 Edelfosine ≥95% (HPLC) Edelfosine is a synthetic alkyl-lisophospholipid with anti-tumor activity. The compound induces apoptosis in a variety of cancer cells. Edelfosine accumulates in the cell membrane, where it alters lipid composition and induces the co-clustering of lipid rafts and Fas/CD95 death receptor.
 
E1286   Eeyarestatin I ≥98% (HPLC) Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination. Also inhibits Sec61-mediated protein translocation at the ER. Displays cytotoxic activity preferentially against cancer cells; induces cell death via the proapoptotic protein NOXA.
Eeyarestatin I or Eer1 promotes transcriptional activation of the pro-apoptotic protein NOXA by inducing activation of the NOXA transcription factors ATF3 and ATF4 and by inhibiting the degradation of histone H2A by blocking its ubiquitination.
 
E8409 EF-24 ≥98% (HPLC) EF-24 is a IKK inhibitor and curcumin analog. EF-24 is more potent and bioavailable than curcumin, with 10-fold greater potency in cell death induction. It is also more efficacious in anti-cancer screens and less toxic than Cisplatin. EF-24 inhibits HIF-1alpha posttranscriptional activity and induces microtubule stabilization, in contrast to Curcumin. EF-24 up-regulates PTEN expression via inhibition of ubiquitination. EF-24 induces cell death through direct inhibition of IkappaB kinase (IKK), resulting in suppression in NFκB activity.
 
E3263 Efaroxan hydrochloride ≥98% (HPLC) (+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand that induces insulin secretion, mediated by the blockade of ATP-sensitive potassium channels in pancreatic β cells; I1 imidazoline binding site antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
SML0536 Efavirenz ≥98% (HPLC) Efavirenz is a nonnucleoside reverse transcriptase inhibitor (NNRTI). It is an anti-HIV drug, commonly used in combination therapy for AIDs treatment. It is part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.
 
SML1244   Efinaconazole ≥98% (HPLC) Efinaconazole is a triazole antifungal drug approved clinically for the treatment of nail fungus (Onychomycosis). It inhibits sterol biosynthesis by inhibition of cytochrome P450 14α-demethylase, an enzyme in the sterol biosynthesis pathway that leads from lanosterol to ergosterol. Efinaconazole has better nail penetration, so is more effective than other topical agents and as effective as oral medication for nail fungus.
 
E0159 Efonidipine hydrochloride monoethanolate ≥98% (HPLC) Racemic efonidipine has both L-type and T-type calcium channel blocking activity. The R(−)-isomer appears to be very selective for T-type calcium channel. The S(+)-isomer inhibits the expressed Ca(V)1.2, Ca(V)1.3 and Ca(V)3.1 channel currents almost equally.
 
SML1367 EG00229 ≥98% (HPLC) EG00229 is an antagonist of the VEGF-A receptor neuropilin 1 (NRP1), which decreases viability of A549 lung carcinoma cells. EG00229 impairs VEGFA induced migration of HUV-EC-C endothelial cells.
 
SML1006   EGA ≥98% (HPLC) EGA is a small molecule that blocks the entry of anthrax lethal toxin by inhibiting trafficking pathways in acidified endosomes, without affecting endosome pH. EGA blocks trafficking of other toxins, including diphtheria toxin, but does not inhibit trafficking of ricin. The compound EGA attenuates lysosomal targeting and degradation of the EGF receptor, but does not block does not block endosomal recycling of transferrin.
 
E114 EHNA hydrochloride ≥98% (HPLC) Adenosine deaminase inhibitor.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
SML0526 EHop-016 ≥98% (HPLC) EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration. EHop-016 inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation.
 
E1657 EHT 1864 ≥98% (HPLC) EHT 1864 inhibits Rac function. It prevents Aβ40 and Aβ42 production in vitro without direct inhibition of g-secretase.
 
E2011 cis-5,8,11,14,17-Eicosapentaenoic acid ≥99% 5-Lipoxygenase inhibitor; reduces thromboxane A2 production.
human ... ALOX5(240)
mouse ... ALOX5(11689), Pparg(19016)
rat ... ALOX5(25290)
E6627   cis-5,8,11,14,17-Eicosapentaenoic acid sodium salt ≥99% (capillary GC) 5-Lipoxygenase inhibitor; reduces thromboxane A2 production.
human ... ALOX5(240)
mouse ... ALOX5(11689)
rat ... ALOX5(25290)
SML0384 Eicosapentaenoyl ethanolamide 5 mg/mL in absolute ethanol, ≥98% (HPLC) Eicosapentaenoyl ethanolamide (EPEA) is a lipid mediator that has been found to suppress lifespan extension resulting from dietary restriction in C. elegans and also to have antiproliferative and anti-inflammatory actions. In C. elegans, it is believed to act as a metabolic signal that couples nutrient availability with growth and lifespan. EPEA is a member of the N-acylethanolamines (NAEs), lipid-derived signaling molecules that include the mammalian endocannabinoid arachidonoyl ethanolamide (AEA). In mammals, NAEs are believed to act primarily through cannabinoid receptors, although they can also interact with a variety of other targets, and EPEA has been shown to act as a CB1 and CB2 receptor agonist. However, C. elegans does not possess clear orthologues of the mammalian cannabinoid receptors which suggests that there are unidentified NAE receptors in nematodes that are possibly conserved mediators of NAE signaling.
 
E1768 5,8,11,14-Eicosatetraynoic acid ≥97% Cyclooxygenase and lipoxygenase inhibitor.
human ... ALOX15(246)
E3285 EIINFEKL trifluoroacetate salt ≥95% (HPLC) EIINFEKL is an antagonist variant of SIINFEKL [OVA (257-264)] [it induces positive selection T-cells].
 
SML0486 Elacridar ≥98% (HPLC) GF120918 (Elacridar) is a very potent inhibitor of the ABC transporters MDR-1 (P-gp) and BCRP. GF120918 increases the bioavailability of cytotoxic anti-tumor drugs, and also leads to increased levels of anti-HIV drugs in the brain and CNS.
 
PZ0011 Eletriptan hydrobromide ≥98% (HPLC) Eletriptan hydrobromide is a serotonin 5-HT1B/1D receptor agonist; second generation anti-migraine drug.
 
E2031 Eliprodil ≥98% (HPLC), powder NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
human ... GRIN2B(2904)
rat ... Adra1a(29412)
E2250 Ellagic acid ≥95% (HPLC), powder, from tree bark A naturally occurring plant phenol that is a potent antioxidant presumably by acting as a scavenger of oxygen species produced by hydrogen peroxide treatment, and as a protector of the DNA double helix from alkylating agent injury. It therefore has anti-mutagenic and anti-carcinogenic properties. Also reported to inhibit topoisomerases I and II and gyrase.
Commonly occurring plant polyphenol, inhibitor of glutathione S-transferase. Used for the assay of factor XIIa in plasma. Contact activation in blood coagulation.
human ... CSK(1445), DYRK1A(1859), GSK3B(2932), SRC(6714)
rat ... Lyn(81515), Syk(25155)
SML1137 ELN484228 ≥98% (HPLC) ELN484228 is a cell penetrant α-synuclein ligand that rescues of α-synuclein induced disruption of vesicle trafficking and dopaminergic neuronal loss and neurite retraction. ELN484228 reverses a-synuclein induced impairment of phagocytosis and protects dopaminergic neurons against the toxic effects of α-synuclein A53T over-expression.
 
SML1526 Eltoprazine hydrochloride ≥98% (HPLC) Eltoprazine hyrochloride is a serotonin 5-HT1A/1B receptor agonist that has been shown to reduce L-DOPA-induced dyskinesias in in experimental models of Parkinson′s Disease and in human patients. It has Ki values for 5-HT1A, 5-HT1B and 5-HT1C receptors of 40 nM and 52 nM, respectively.
 
SML0183 EM20-25 ≥98% (HPLC) EM20-25 disrupts the BCL-2/BAX interactions and activates caspase-9 in cells overexpressing BCL-2. It sensitizes the BCL-2 expressing leukemic cells to the effects of chemotherapy involving staurosporine and chlorambucil.
EM20-25 is an analog of HA14-1 that antagonizes the effects of the anti-apoptotic protein BCL-2, and causes opening of the mitochondrial permeability transition pore. Unlike HA14-1, EM20-25 does not effect mitochondrial respiration.
 
E1406 Embelin ≥98% (HPLC), powder Embelin is an inhibitor of XIAP (X-linked inhibitor-of-apoptosis protein); in vivo antitumor and anti-inflammatory activity.
human ... XIAP(331)
SML0139 EMD386088 ≥98% (HPLC) EMD-386088 is a potent serotonin 5-HT6-specific agonist. The IC50 for competition of LSD from 5-HT6 expressed in HEK cells is 7.4 nM, and the EC50 for stimulating cAMP production is 1 nM. EMD-386088 is inactive against other HT receptors except 5-HT3 (IC50 = 34 nM).
EMD386088 effectively reverses cholinergic and glutataminergic-induced deficits in cognitive functions. It may be a therapeutic option in improving associated learning in Alzheimer′s disease and schizophrenia. EMD386088 also exhibits anti-depressant and anxiolytic effects in rats.
 
SML1828 EMD-87580 ≥98% (HPLC) EMD-87580 is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. EMD-87580 has shown cardioprotective effects, and has been investigated as a possible treatment for Duchenne′s muscular dystrophy.
 
E2375 Emetine dihydrochloride hydrate    
E7881 Emodin from Frangula bark, ≥90% (HPLC) Inhibitor of NF-κB activation and adhesion molecule expression. Casein Kinase 2 (CK2) inhibitor.
human ... CSNK2A1(1457), CSNK2B(1460), ELA2(1991), NFKB1(4790), NKAP(79576), NKRF(55922)
SML0864   EMPA ≥98% (HPLC) EMPA is a potent, selective OX2R antagonist (IC50 = 2.3 nM). EMPA binds reversibly to OX2R and inhibits orexin-a and -b-evoked intracellular calcium flux in cells expressing recombinant OX2R, but not OX1R.
 
E6888 Enalapril maleate salt powder, ≥98% (TLC) A long-acting angiotensin-converting enzyme inhibitor.
 
E9658 Enalaprilat dihydrate ≥98% (HPLC) Enalaprilat is an inhibitor of angiotensin converting enzyme (ACE), antihypertensive, and a Bradykinin B1 receptor activator. Enalaprilat has nM potency versus ACE and also activates B1 receptors to release NO.
 
E9156 Encainide hydrochloride ≥98% (HPLC), powder Encainide hydrochloride is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
 
SML0719   Enclomiphene hydrochloride ≥96% (HPLC) Enclomiphene is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes. Enclomiphene is the trans-isomer of clomiphene, which is about a 60-40 mix of trans (Enclomiphene) and cis (Zuclomiphene). While enclomiphene (trans-clomiphene) is an estrogen antagonist, zuclomiphene (cis-clomiphene) is a mixed agonist, responsible for the estrogenic activity and therefore the common side effects sometimes seen in males. The enclomiphene isomer is responsible for the anti-estrogen activity and the restoration of ones hypothalamic–pituitary–gonadal axis. In recent clinical trials, enclomiphene increased serum LH and FSH with concomitant increases in testosterone in men with secondary hypogonadism. Enclomiphene showed overall better results than testosterone gels, which raise serum testosterone but can lower LH and FSH at the same time.
 
SML1681 Endosidin2 ≥98% (HPLC) Endosidin2 is a cell-permeable benzylidene-benzohydrazide based compound that binds to the exocyst component of 70 kDa (EXO70) subunit of exocyst complex (Kd = 253 μM for interaction with EXO70A1) and reduces exocytosis and endosomal recycling in plant and mammalian cells. Displays good aqueous stability. Endosidin2 has shown to disrupt the trafficking of proteins between the plasma membrane and endosome, which leads to enhanced trafficking to the vacuole for degradation. It is reported to inhibit the recycling of endocytosed transferrin to plasma membrane in HeLa cells, and can target multiple isoforms of EXO70 in mammals, resulting in misregulation of exocytosis.  
 
E8284 (E/Z)-Endoxifen Hydrochloride Hydrate ≥98% (HPLC) (E/Z)-Endoxifen hydrochloride ((E/Z)-4-Hydroxy-N-desmethyltamoxifen hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). It is equipotent to 4-hydroxytamoxifen with respect to estrogen receptor binding and inhibition of 17-estradiol (E2)-induced cell proliferation. It is primarily catalyzed by cytochrome P450 2D6 (CYP2D6). Mutations in CYP2D6 may prevent response to tamoxifen by preventing formation of endoxifen. The gene expression patterns of five genes have been validated to be differentially regulated by endoxifen and 4-OH-Tamoxifen. Endoxifen and 4-OH-Tam have similar effects on global gene expression patterns in MCF-7 cells and the majority of the affected genes are estrogen-regulated genes.
 
SML0934   Enfuvirtide acetate salt ≥95% (HPLC) Enfuvirtide is an HIV fusion inhibitor used to patients with multi-drug resistant HIV. Enfuvirtide binds to gp41 preventing the creation of an entry pore for the HIV-1 virus.
 
SML1039   ENMD-1068 hydrochloride ≥97% (HPLC) ENMD-1068 is an antagonist of protease-activated receptor 2 (PAR2). The compound blocks TNFα production in synovial explants from patients with arthritis, and inhibits mast cell tryptase-induced recruitment of eosinophils into the pleural cavity of mice.
 
E9661   Enniatin A from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42).
 
E5411   Enniatin B from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42). Enniatins B and B1 inhibit the multi-drug resistance transporter Pdr5p from Saccharomyces cerevisiae, indicating their beneficial potential in cases of drug resistant patients.
 
E5161   Enniatin A1 from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42).
 
E5286   Enniatin B1 from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42). Enniatins B and B1 inhibit the multi-drug resistance transporter Pdr5p from Saccharomyces cerevisiae, indicating their beneficial potential in cases of drug resistant patients.
 
E1279 Enoximone solid Selective phosphodiesterase III (PDE3) inhibitor. Prevents the degradation of cAMP by PDE. Increased cAMP results in enhanced contractility of the heart.
human ... PDE3A(5139), PDE3B(5140)
SML0654   Entacapone ≥98% (HPLC) Entacapone is a catechol-O-methyl transferase (COMT) inhibitor. Used in treatment of Parkinson′s disease, entacapone is administered with L-DOPA to inihibit COMT from converting L-DOPA into a compound that cannot cross the blood brain barrier.
 
SML1103 Entecavir ≥98% (HPLC) Entecavir is an antiviral guanine analog that inhibits reverse transcription, DNA replication and transcription in the viral replication process. Entecavir is used to treat hepatitis B.
 
SML0762   Enzastaurin ≥98% (HPLC) Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent.
 
SML0527   Epalrestat ≥98% (HPLC) Epalrestat inhibits Aldose Reductase (AR) involved in the rate limiting step in the conversion of glucose to sorbitol under hyperglycemic conditions. Aldose reductase has been the target of multiple clinical investigatons to treat diabetic neuropathy and retinopathy. Epalrestat is an approved drug in Japan and India, used for the treatment of diabetic neuropathy.
 
SML1844 EPI-001 ≥98% (HPLC) EPI-001 is a specific inhibitor of the AR (androgen receptor) without inhibiting PR or GR transcriptional activities. EPI-001 selectively interacts with transactivation unit 5 (Tau-5) of the androgen receptor, which is essential for prostate cells to proliferate in the absence of androgens. EPI-001 is active against castration-resistant prostate cancer (CRPC) in xenografts.
 
E1145 (±)-Epibatidine dihydrochloride hydrate ≥98% (HPLC), powder The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.
 
SML1647 Epiblastin A ≥98% (HPLC) Epiblastin A is triamterene derivative that potently induces reprograming of epiblast stem cells (EpiSC) into embryonic stem cells (ESC). Epiblastin A is a potent reversible inhibitor of casein kinase 1 (CK1) α, δ, and ε that binds to ATP-binding site.
 
E1641 Epibrassinolide ≥85%    
E1753 (−)-Epicatechin ≥90% (HPLC) Antioxidant
human ... BACE1(23621), CYP1A2(1544)
E4018 (−)-Epicatechin ≥98% (HPLC), from green tea Antioxidant found in chocolate.
human ... BACE1(23621), CYP1A2(1544)
E3625 16-Epiestriol ≥93% (HPLC) 16-Epiestriol is an estradiol metabolite that exhibits significant anti-inflammatory activity without glycogenic activity.
 
E3750 17-Epiestriol 17-epiestriol is an estradiol metabolite and a selective estrogen receptor (ER) beta agonist.
 
E5156 Epinastine hydrochloride ≥98% (HPLC), solid Epinastine hydrochloride is a non-sedating H1 histamine receptor antagonist.
 
SML0013 Epinecidine-1 trifluoroacetate salt ≥98% (HPLC) Epinecidin-1 is an antimicrobial peptide (AMP) with antitumor and antiviral activity, which was cloned from orange-spotted grouper (Epinephelus coioides). Apparently epinecidin-1 binds to microbial surface and next destroys microbial membrane. Epinecidin-1 was effective in protecting grouper larvae from nervous necrosis viral (NNV) disease.
 
E4250 (−)-Epinephrine Adrenoceptor agonist.
rat ... Adra1a(29412), Adra2a(25083), Adrb1(24925), Adrb2(24176), Drd1a(24316), Drd2(24318)
E4375 (−)-Epinephrine (+)-bitartrate salt solid Adrenergic receptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
E4642 (±)-Epinephrine hydrochloride Adrenergic receptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
E6657 Eplerenone ≥98% (HPLC) Eplerenone is an aldosterone antagonist more specific for the mineralocorticoid receptor than spironolactone (S3378), having lower affinity for progesterone, androgen, and glucocorticoid receptors.
 
E3656 (−)-Epothilone A from Sorangium cellulosum, >95% (HPLC), solid (-)-Epothilone A is a microtubule (MT) stabilizing drug and natural macrolide antitumor from myxobacteria Sorangium cellulosum. EpoA exhibits kinetics similar to paclitaxel by inducing tubulin polymerization in vitro and producing enhanced microtubule stability and bundling in cultured cells. In contrast to paclitaxel, Epothilone A exhibits a greater cytotoxicity against P-glycoprotein-expressing multidrug resistant (MDR) cells (IC50 = 20 nM for MDR CCRF-CEM/VBL100 cells). Epothilone A is a competitve inhibitor of 3H-paclitaxel binding with comparable IC50 to paclitaxel in displacement competition assays. EpoA causes cell cycle arrest at the G2/M transition leading to cytotoxicity.
 
E2656 (−)-Epothilone B from Sorangium cellulosum, ≥98% (HPLC) (-)-Epothilone B is a microtubule (MT) stabilizing drug and natural macrolide antitumor from myxobacteria Sorangium cellulosum. EpoB has similar biological properties to EpoA. However, EpoB is 10-fold more potent than EpoA against P-glycoprotein-expressing multidrug resistant (MDR) cells (IC50 = 2 nM for MDR CCRF-CEM/VBL100 cells). (-)-Epothilone B is similar to paclitaxel in binding displacement, and a substitution for paclitaxel in dependent cell growth. EpoB causes cell cycle arrest (IC50 = 3.5 nM).
 
E4625 16,17-Epoxy-21-acetoxypregnenolone ≥98%    
E4875 16α,17α-Epoxypregnenolone    
E5000 16α,17α-Epoxypregnenolone acetate ~95%    
SML1350 EPPTB ≥95% (HPLC) EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1), a G protein-coupled receptor (GPCR) activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β)-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). TAAR1 is considered a promising target for the treatment of neuropsychiatric disorders, however study of TAAR1 has hampered by the fact that selective ligands have not been available. EPPTB is the first potent and selective TAAR1 antagonist with an IC50 of 28 nM at mouse TAAR1. EPPTB is less selective for rat and human with IC50 values of 4539 and 7487 nM, respectively.
 
E2535 Eprosartan mesylate ≥98% (HPLC) Angiotensin II type 1 (AT1) receptor antagonist; anti-hypertensive.
 
SML1042   Eptifibatide acetate ≥98% (HPLC) Eptifibatide is a specific inhibitor of fibrinogen binding to the platelet membrane integrin glycoprotein GPIIb/IIIa receptor, preventing platelet aggregation. Eptifibatide binds reversibly and competitively.
 
SML1421 EPZ015666 ≥98% (HPLC) EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC50 value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 μM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.
 
E8126 Equilin    
SML1929 Equisetin (Fusarium equiseti), ≥97% (HPLC) New Equisetin is a tetramic acid analog derived from Fusarium equisti. Equisetin is mainly known for its antibiotic and cytotoxic activity and for its inhibitory effect on HIV-1 integrase. Inhibition of HIV integrase by Equisetin was reported with IC50 values of 5-20 μM. Moreover, it was shown that Equisetin specifically inhibits the substrate anion carriers of the inner membrane of mitochondria and acts nonspecifically on protein membranes and protein hydrophobic domains. In addition, it was demonstrated that Equisetin causes phytotoxicity by causing root Necrosis and was also identified in a mycotoxin cocktail associated with cattle feeding problems.
 
E0656 ER-27319 ≥98% (HPLC), solid ER-27319 inhibits Syk activation with an IC50 = 10 μM. ER-27319 inhibits Syk by preventing the phosphorylated ITAM domain of FcεRI γ from activating Syk. ER-27319 does NOT inhibit previously activated Syk.
Selective Syk inhibitor. Induces tyrosine phosphorylation of Syk that has been demonstrated as critical for degranulation.
 
E7781 Erastin ≥98% (HPLC) Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces ferroptosis, a non-apoptotic tumor cell death, by altering mitochondrial voltage-dependent anion channel (VDAC) gating allowing cations to enter mitochondria and leading to release of oxidative species causing oxidative cell death.
human ... hRas(3265)
mouse ... hRas(15461)
rat ... hRas(293621)
PZ0183 ERB-041 ≥98% (HPLC) ERB-041 is a potent, selective estrogen ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα). ERβ plays a minor role in mediating estrogen action in the uterus, the hypothalamus/pituitary, the skeleton, and other classic estrogen target tissues. However, a clear role for ERβ has been established in the ovary, cardiovascular system, and brain as well as in animal models of inflammation including arthritis, endometriosis, inflammatory bowel disease, and sepsis. There is increasing interest in finding ERβ agonists for potential use in a variety of clinical applications without triggering classic estrogenic side effects.
 
E2634 Ergosta-5,7,9(11),22-tetraen-3β-ol ~96% (HPLC)    
E6510 Ergosterol ≥75%    
SML0467 ES936 ≥98% (HPLC) ES936 is a very potent and selective inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1). ES936 inhibits superoxide scavenging by NQO1 in tumor and cardiovascular cells. NQO1 is highly expressed in pancreatic cancers, and ES936 inhibits proliferation of pancreatic tumor lines Mia PaCa and BxPC-3 with nanomolar IC50 values.
 
E4786 Escitalopram oxalate ≥98% (HPLC), powder Escitalopram is a selective serotonin reuptake inhibitor (SSRI), the S-enantiomer and eutomer of citalopram.
 
E8375 Eserine Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
human ... ACHE(43), APP(351), BCHE(590)
mouse ... Ache(11423), Bche(12038), Chrm1(12669)
rat ... Ache(83817), Bche(65036), Chrm2(81645)
45710 Eserine ≥98.0% (N) Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
human ... ACHE(43), APP(351), BCHE(590)
mouse ... Ache(11423), Bche(12038), Chrm1(12669)
rat ... Ache(83817), Bche(65036), Chrm2(81645)
E8625 Eserine hemisulfate salt Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
 
SML1907 ESI-05 ≥98% (HPLC) ESI-05 is a selective inhibitor against cAMP-regulated guanine nucleotide exhange factor (GEF) EPAC2 (Exchange factor directly activated by cAMP 2) activation by targeting an EPAC2-specific allosteric site at the interface of the two cAMP-binding domains. ESI-05 inhibits EAPC2, but not EPAC1 or PKA, activation by cAMP in a highly potent (IC50 = 430 nM; 25 μM cAMP) and cAMP-competitive manner in cell-free assays, and suppresses cAMP analog 007-AM-induced cellular Rap1 activation in EPAC2-, but not EPAC1-, expressing HEK293 transfectants.
 
SML0814   ESI-09 ≥98% (HPLC) ESI-09 is a potent, specific inhibitor of EPAC (exchange protein directly activated by cAMP). ESI-09 inhibits EPAC1 and EPAC2 with IC50 values of 3.2 and 1.4 μM, respectively, with no activity against PKA at 25 μM. In pancreatic cell lines, the compound blocks phosphorylation of Akt and insulin secretion. ESI-09 inhibits migration of pancreatic cancer cell lines.
 
E8031 Esmolol hydrochloride ≥98% (HPLC), solid Esmolol hydrochloride is a ultrashort-acting β1 adrenoceptor antagonist (β1 receptor occupancy = 84.7%).
 
E7906 Esomeprazole magnesium hydrate ≥98% (HPLC), powder Esomeprazole magnesium dihydrate is a leading proton pump inhibitor.
 
E3638 Estazolam Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site.
 
SML1523 Estetrol ≥98% (HPLC) Estetrol (E4, 15α-Hydroxyestriol) is an estrogen steroid hormone produced exclusively during pregnancy by the fetal liver. Estetrol is a selective estrogen receptor modulator (SERM) with potent estrogenic effects on vaginal mucosa, bone and brain, neutral effect on liver, and anti-estrogen effects on breast tissue. Estetrol has higher affinity for ERα over ERβ. Estetrol is being studied for its potential as a contraceptive, a drug for meopausal symptoms, and an anticancer agent.
 
E8750 α-Estradiol powder, ≥98% (TLC) Estradiol (known as alpha Estradiol or 17 alpha Estradiol) is a biologically active estrogen in human breast cancer cells in tissue culture.17-estradiol and its selective receptor, ER-X, are not part of a classical hormone/receptor endocrine system but of a system with important autocrine/paracrine functions in the developing and adult brain. 17-Estradiol may have enormous implications for hormone replacement strategies at the menopause and in the treatment of such neurodegenerative disorders as Alzheimer’s disease and ischemic stroke.
human ... ESR1(2099), ESR2(2100)
rat ... Ar(24208)
E8875 β-Estradiol ≥98% The major estrogen secreted by the premenopausal ovary. Estrogens direct the development of the female phenotype in embryogenesis and during puberty by regulating gene transcription and, thus, protein synthesis. It also induces the production of gonadotropins which, in turn, induce ovulation. Exposure to estradiol increases breast cancer incidence and proliferation.
human ... ESR1(2099), ESR2(2100), ESRRA(2101), ESRRB(2103), GPER(2852), SERPINA6(866)
mouse ... Esr1(13982), Esr2(13983), Esrra(26379)
rat ... Afp(24177), Ar(24208), Esr1(24890), Esr2(25149), Shbg(24775)
E1132 β-Estradiol analytical standard The major estrogen secreted by the premenopausal ovary. Estrogens direct the development of the female phenotype in embryogenesis and during puberty by regulating gene transcription and, thus, protein synthesis. It also induces the production of gonadotropins which, in turn, induce ovulation. Exposure to estradiol increases breast cancer incidence and proliferation.
human ... ESR1(2099), ESR2(2100), ESRRA(2101), ESRRB(2103), GPER(2852), SERPINA6(866)
mouse ... Esr1(13982), Esr2(13983), Esrra(26379)
rat ... Afp(24177), Ar(24208), Esr1(24890), Esr2(25149), Shbg(24775)
E7879 β-Estradiol 17-acetate ≥99% β-Estradiol 17-acetate is a metabolite of estradiol.
 
E5630   β-Estradiol 6-(O-carboxy­methyl)oxime: BSA    
E6507   β-Estradiol 6-(O-carboxy­methyl)oxime: BSA fluorescein iso­thio­cyanate conjugate    
E8004 β-Estradiol 17-cypionate    
E2127 β-Estradiol 3-(β-D-glucuronide) sodium salt    
E1127 β-Estradiol 17-(β-D-glucuronide) sodium salt    
E2128 β-Estradiol 3-(β-D-glucuronide) 17-sulfate dipotassium salt    
E9252 β-Estradiol 17-hemisuccinate    
K1001 β-Estradiol-6-one    
K2126 β-Estradiol-6-one 6-(O-carboxymethyloxime)    
E9505 β-Estradiol 3-sulfate sodium salt ≥93%    
E1631 β-Estradiol 17-valerate ≥98%    
E1253 Estriol ≥97% Estriol is a metabolite of 17β-estradiol with much lower biological activity. It is the primary estrogen found in the urine. Large quantities of estriol and estrone are produced by the placenta during pregnancy. These are also the primary estrogens produced by adipose tissue in men and in post-menopausal women.
human ... SERPINA6(866)
mouse ... Esr1(13982)
rat ... Ar(24208)
E1877 Estriol 16α-(β-D-glucuronide) ≥97%    
E5255 Estriol 16α-(β-D-glucuronide) sodium salt ≥95% (HPLC)    
E9750 Estrone ≥99% Estrone is a luteolytic estrogen produced by the corpus luteum.
human ... ESR1(2099), ESR2(2100), ESRRA(2101), ESRRB(2103), HSD17B1(3292), SERPINA6(866)
mouse ... Esr1(13982)
rat ... Esr1(24890)
E1752 Estrone 3-(β-D-glucuronide) sodium salt    
E9875 Estrone 3-methyl ether ≥97% (HPLC)    
E0251 Estrone 3-sulfate sodium salt contains ~35% Tris as stabilizer    
E2661 Estropipate ≥98% (HPLC), powder Estropipate is the piperazine salt of the estrogen receptor agonist estrone-3-sulfate and a potent, specific inhibitor of the organic anion transporting polypeptide 1B1 (OATP1B1, IC50 = 60 nM).
 
SML1743 ETaKG ≥95% (HPLC) ETaKG is a cell-permeable, aqueous stable, bioavailable, non-toxic α-ketoglutarate/2-oxoglutarate (α-KG/2-OG) diester derivative that readily undergoes hydrolysis by cytosolic esterases to α-KG. The monoester analog, TaKG is also membrane permeant. ETaKG elevates intracellular [α-KG] by ~15-fold in a prologned fashion, destabilizes HIF-1α/2α and reactivates prolyl hydroxylases (PHDs) in hypoxic HCT116, A431 and RPE cells at 2 mM. Further, shown to selectively trigger PHD-dependent cell death in hypoxic cells and decreases cellular [ATP] and glucose uptake. ETaKG has shown to reduce glucose metabolism, elevate [α-KG] levels and suppress A375 xenograft tumor growth (750 mg/kg of mice, p.o., q.d., 14 days). Also, induces mTORC1 lysosomal translocation and stimulates mTORC1 activity in the absence of glutaminolysis in U2OS cells.
 
E1896 Etazolate hydrochloride solid Selective inhibitor of cAMP-specific phosphodiesterase.
human ... PRKAR1A(5573), PRKAR1AP(5574), PRKAR1B(5575), PRKAR2A(5576), PRKAR2B(5577)
SML1083 Ethacrynic acid ≥97% (HPLC) Ethacrynic acid is non sulfonamide loop diuretic that is used to treat high blood pressure and the swelling caused by diseases like congestive heart failure. Ethacrynic acid blocks sodium-potassium-chloride cotransport. Also, Ethacrynic acid potently inhibits glutathione S-transferase family members. Studies show that ethacrynic acid potently inhibits Tgase-2 (transglutaminase-2) dependent metastasis of cancer cells including lung and pancreatic cancers.
 
E1001 Ethisterone ≥99% (HPLC)    
E5406 Ethopropazine hydrochloride ≥98% (HPLC), powder Ethoproprazine hydrochloride is an inhibitor of butyrylcholinesterase; antiparkinsonian. It reduces extrapyramidal motor effects, characteristic of Parkinson′s disease; also alleviates thermal hyperalgesia in rats.
 
E7138 Ethosuximide Used for the treatment of absence-type seizures
human ... CACNA1G(8913)
E1379 7-Ethoxycoumarin Substrate for CYP2B6
 
SML0149 3-Ethoxy-5,6-dibromosalicylaldehyde ≥95% (HPLC) 3-Ethoxy-5,6-dibromosalicylaldehyde is a non-competitive inhibitor of Inositol-requiring enzyme 1 (IRE1). It inhibits XBP-1 splicing induced pharmacologically in human cells. 3-Ethoxy-5,6-dibromosalicylaldehyde potently inhibits the endoribonuclease of IRE1 but does not inhibit RNases A, T1, or L.
 
E2387 5′-(N-Ethylcarboxamido)adenosine powder Potent adenosine receptor agonist with nearly equal affinity at A1 and A2 receptors.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Adora3(25370)
E1904 Ethyl-3,4-dephostatin >99% (HPLC), solid Stable analog of dephostatin. Selective inhibitor of protein tyrosine phosphatase 1B and SHPTP-1. Does not inhibit CD45-associated phosphatases.
 
E3145 3-Ethyl-3-(ethylaminoethyl)-1-hydroxy-2-oxo-1-triazene ≥90%    
E2895 (±)-(E)-4-Ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide ≥98% Activates intracellular guanylyl cyclase.
 
A3085 5-(N-Ethyl-N-isopropyl)amiloride Selective blocker of Na+/H+ antiport
human ... SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340), SLC9A1(6548), SLC9A5(6553)
mouse ... Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278)
rat ... Scnn1a(25122), Scnn1b(24767), Scnn1g(24768), Slc9a1(24782), Slc9a2(24783), Slc9a3(24784), Slc9a4(24785)
E3020 (±)-(E)-4-Ethyl-2-[(Z)-hydroxyimino]-5-nitro-3-hexen-1-yl-nicotinamide ≥97%    
E7263 Ethynodiol diacetate    
E4876 17α-Ethynylestradiol ≥98% 17α-Ethynylestradiol is an orally bio-active synthetic estrogen used as an oral contraceptive.
rat ... Afp(24177), Esr1(24890), Shbg(24775)
E7887 17α-Ethynylestradiol 3-cyclopentyl ether    
E101 S-(−)-Eticlopride hydrochloride ≥98% (HPLC), powder Potent and selective D2 dopamine receptor antagonist.
human ... DRD2(1813)
P5248 Etidronate disodium hydrate ≥97% (NMR), solid Bisphosphonate antiresorptive agent. Less potent inhibitor of farnesyl diphosphate synthase (IC50 = 80 μM) as compared to the nitrogen containing bisphosphonates
 
SML0272 Etifoxine hydrochloride ≥98% (HPLC) Etifoxine is an anxiolytic anticonvulsant, which promotes axonal regeneration. It binds to β2 and β3 subunits of the GABAA receptor complex, a different target site to benzodiazepines, and binds to the translocator protein (18 kDa) TSPO, formerly known as the peripheral or mitochondrial benzodiazepine receptor. TSPO carries cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step of steroidogenesis. Whereas, its anxiolytic effects involve GABAA receptors and TSPO, etifoxine′s neuroregenerative effects mainly involve TSPO.
 
E5126 Etiocholan-3α-ol-17-one   human ... SERPINA6(866)
rat ... Gabra1(29705), Gabra2(29706), Gabrg2(29709)
E0516 Etodolac Non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX-1 and COX-2.
human ... PTGS1(5742), PTGS2(5743)
E6530 Etomidate >98% (HPLC), powder Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
human ... GABRA1(2554)
E1905 (+)-Etomoxir sodium salt hydrate ≥98% (HPLC), powder Irreversible O-carnitine palmitoyltransferase-1 (CPT-1) inhibitor; PPARα activator
 
SML0356 Etonogestrel ≥98% (HPLC) Etonogestrel is a third-generation progestin contraceptive. Etonogestrel is used as a contraceptive itself and is also the active metabolite of the drug desogestrel used in some combination contraceptives.
 
E1383 Etoposide synthetic, ≥98%, powder Etoposide is an antitumor agent that complexes with topoisomerase II and DNA to enhance double-strand and single-strand cleavage of DNA and reversibly inhibit religation. Blocks the cell cycle in in S-phase and G2-phase of the cell cycle; induces apoptosis in normal and tumor cell lines; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2.
human ... ABCB1(5243), CYP3A4(1576), TOP2A(7153)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Top2a(360243)
SML1321 ETP-46464 ≥98% (HPLC) ETP-46464 is a potent and selective inhibitor of the DNA damage response kinase Ataxia telangiectasia-mutated (ATM) - and Rad3-related (ATR) with an IC50 of 25 nM. ETP-46464 shows moderate activity against PI3K and is a potent inhibitor of mTor, but is selective for ATR versus ATM and DNA -dependent protein kinase (DNA -PKcs) even at high doses. ETP-46464 inhibited phosphorylation of Chk1, the downstream kinase of ATR, but did not affect ionizing radiation–induced γH2AX formation, which is jointly controlled by ATM and DNA-PKc.
 
SML0742   EUK-8 ≥95% (HPLC) EUK-8 is a salen manganese complex that exhibit potent antioxidant activities. EUK-8 is a superoxide dismutase (SOD) that inhibits amyloid fibril formation, including islet amyloid polypeptide (IAPP), β-amyloid and lysozyme amyloid aggregation. It appears that EUK-8 disrupts the pre-formed amyloid fibrils. EUK-8 increases the viability of the SK-N-MC cells exposed to preformed IAPP fibrils.
 
SML0743   EUK-134 ≥95% (HPLC) EUK-134 is a manganese-salen derivative that exhibit potent antioxidant activities. EUK-134 is a superoxide dismutase (SOD) that inhibits amyloid fibril formation, including islet amyloid polypeptide (IAPP), β-amyloid and lysozyme amyloid aggregation. It appears that EUK-134 disrupts the pre-formed amyloid fibrils. EUK-134 increases the viability of the SK-N-MC cells exposed to preformed IAPP fibrils.
 
SML1689 Eupatilin ≥98% (HPLC) Eupatilin is a flavone with anti-oxidative, anti-inflammatory, and anti-cancer properties.
 
E4660 Eupatorin ≥97% (HPLC) Eupatorin acts as an antiproliferative in cells expressing the CYP1A- family. It induces G2/M block follow by apoptosis in cells expressing the CYP1A- family. It also functions as an anti-inflammatory.
 
SML0579 EVP4593 ≥98% (HPLC) EVP4593 is a high affinity partial antagonist of NF-KB pathway activation acting by inhibiting store-operated calcium (Ca2+) entry (SOC). It appears that EVP4593 targets heteromeric channels containing TRPC1 as one of the subunits in HD neurons. EVP4593 exhibits neuroprotective effects from glutamate toxicity in nanomolar concentrations.
 
SML1680 Ex26 ≥98% (HPLC) Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist (IC50 = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). Ex26 significantly elevates CpG-A-stimulated interferon (IFN) production in plasmacytoid dendritic cell culture (10 μM) and prevents S1P1 agonist-induced S1P1 receptor internalization and polyubiquitinylation in HEK cells (0.1-1,000 nM). Ex26 induces lymphocyte sequestration (ED50 = 0.06 mg/kg, i.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in mice, leading to the inhibition of lymphocyte and thymocyte egress (0.1 mg/kg/hr continuously for 3 days after a loading dose of 3 mg/kg). Ex26 has been shown to ameliorate experimental autoimmune encephalomyelitis (EAE) in a mouse MS model and elevate CpG-A-stimulated serum IFN upregulation in mice in vivo (30 mg/kg/d, i.p.).
 
E7034 EX-527 ≥98% (HPLC) EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.
 
PZ0006 Exemestane ≥98% (HPLC) Exemestane is a steroidal antiestrogen and irreversible aromatase inhibitor. Exemestane acts as a false substrate for the aromatase enzyme. Exemestane also prevents the conversion of androgens to estrogens and is used to treat estrogen-dependent breast cancer.
 
E8280 Exo 1 ≥98% (HPLC), solid Reversible inhibitor of exocytosis; Golgi ARF 1 (ADP-Ribosylation Factor) GTPase activator.
 
E7159 Exo2 ≥98% (HPLC) Exo2 acts as a chemical probe of intracellular transport. Edxo2 has activities similar to Brefeldin A with membrane trafficking to the Golgi appartus, but appears more selective.
 
SML1330 Extracellular Death Factor trifluoroacetate salt ≥95% (HPLC) Extracellular Death Factor (EDF) is a bacterial quorum sensing pentapeptide that activates a cell death pathway. EDF is required for mazEF-mediated toxin-antitoxin system of cell death in Escherichia coli.
 
SML1081   Ezatiostat ≥98% (HPLC) Ezatiostat is an inhibitor of glutathione S-transferase P1-1 (GSTP1-1). After intracellular de-esterification, the active form of ezatiostat binds to and inhibits GST P1-1, leading to activation of Jun kinase (JNK), a key regulator of cellular growth and differentiation of blood precursor cells, thereby restoring JNK and MAPK pathway activities and promoting MAPK-mediated cellular proliferation and differentiation. Ezatiostat promotes the proliferation and maturation of hematopoietic precursor cells, granulocytes, monocytes, erythrocytes and platelets. Ezatiostat has recently been given orphan drug designation for it for the treatment of myelodysplastic syndrome.