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PZ0187 Begacestat ≥98% (HPLC) Begacestat (GSI-953) is a selective β-secretase inhibitor that selectively inhibits cleavage of APP over Notch.
 
SML1232 cGAMP sodium salt ≥98% (HPLC) Cyclic AMP-GMP (cGAMP) is one of several naturally occurring cyclic dinucleotides that act as a bacterial second messengers to regulate important signaling mechanisms in prokaryotes that control bacterial survival, adhesion, colonization, biofilm formation, and virulence factors production. In cholera c-AMP-GMP promotes intestinal colonization by down-regulating chemotaxis. During infections bacterial cGAMP is bound by host STING (stimulator of interferon genes) activating innate immune responses leading to expression of interferon genes.
 
SML1229 2′,3′-cGAMP sodium salt ≥98% (HPLC) 2′,3′-cGAMP (cyclic [G(2’,5’)pA(3’,5’)p]) is the natural agonist for the STING (STimulator of INterferon Genes) pathway, recently discovered to be a pathway for antiviral innate immunity. 2’3’-cGAMP is a second messenger produced in mammalian cells by the cytosolic DNA sensor cGAS (cGAMP synthase) to activate innate immune responses by binding to STING and initiating an interferon response. The affinity of 2′3′-cGAMP for human STING is much higher than that of the bacterial 3′3′-cyclic dinucleotides (CDNs), with a Kd of 4.59 nM compared to >1 μM for bacterial 3′3′-CDNs.
 
SML1449 G3335 ≥98% (HPLC) G3335 ( L-tryptophyl-L-glutamic acid) is a cell-permeable dipeptide that acts as a selective and reversible PPARγ antagonist with a Kd value of 8.34 μM for PPARγ and much lower activity at other PPAR subtypes. G3335 reversibly and competitively blocks activation of PPARγ by the PPARγ agonist rosiglitazone, and conversely, in rat astrocyte culture higher levels of rosiglitazone reduced harmful effects induced by G3335. At higher concentration G3335 may act as a PPARα agonist, interacting with the PPARα ligand binding domain with a KD of 120 μM. G3335 is reported to reduce hepatic lipid accumulation in lipid-loaded hepatocytes by activation of PPARα.
 
G3798 10074-G5 ≥98% (HPLC) 10074-G5 is a c-Myc/Max interaction inhibitor. The c-Myc oncoprotein and its partner Max are intrinsically disordered (ID) monomers that undergo coupled folding and binding upon heterodimerization. 10074-G5, similarly to 10058-F4 (#F3680), specifically inhibits this interaction by binding to c-Myc, thus preventing C-Myc specific DNA binding and target genes regulation. 10074-G5 (2.8 microM) is slightly more potent that 10058-F4 (5.2 microM). It was discovered that 10074-G5 binds to a different specific binding site (region) of C-Myc than 10054-F4. Thus, the compound may become desirable for probing different interactions.
 
G154 Gabapentin solid Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.
human ... ADORA1(134), CACNA2D1(781)
rat ... Cacna1a(25398)
C4905 Galactocerebrosides from bovine brain ≥97% (TLC) Galactose linked to ceramide by a β-glycosidic linkage; the major lipid in adult brain, representing approximately 16% of total lipid; they are mainly localized to myelin and are markedly reduced in demyelinating diseases.
 
G8134 Gallamine triethiodide ≥98% (TLC), powder, muscarinic receptor antagonist Muscle relaxant; allosteric muscarinic receptor antagonist with an order of potency of M2 > M1 = M4 > M3 = M5. Ligand for the peripheral anionic binding site of acetylcholinesterase.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
G6657 (−)-Gallocatechin ≥98% (HPLC) Possesses free radical scavenging ability. Inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.
 
G6782 (−)-Gallocatechin gallate from green tea, ≥98% (HPLC) Antioxidant
 
SML0776 Galloflavin ≥95% (HPLC) Galloflavin is an inhibitor of lactate dehydrogenase (LDH). The compound blocks both isoforms of (LDH-A and –B) with Ki values of 5.5 and 15 μM, respectively. Inhibition of the glycolytic pathway by galloflavin induces oxidative stress and apoptosis in breast tumor cell lines.
 
G8171 Gambogic acid ≥95% (HPLC), powder Gambogic acid acts as a caspase activator and apoptosis inducer, which causes an irreversible arrest in the G2/M phase of the cell cycle.
 
G0548   14-3-3 Gamma, histidine-tagged human recombinant, expressed in E. coli, buffered aqueous glycerol solution, ≥90% (SDS-PAGE) The 14-3-3 proteins are a multifunctional protein family comprising seven mammalian isoforms that interact with over two hundred different intracellular molecules including kinases, phosphatases, transcription factors, scaffold proteins, and DNA. 14-3-3 proteins are linked to many human diseases. The 14-3-3 γ isoform is abundantly expressed in the brain with increased levels in Alzheimer′s disease and Down′s syndrome. 14-3-3 γ is involved in cancerous processes including the stimulation of abnormal cell proliferation.
 
G7795 Ganaxolone solid Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnane-20-one) is a positive allosteric modulator of the GABAA receptor subtype; synthetic analog of the endogenous neurosteroid allopregnanolone; effective against chemically induced seizures in rats and mice. Ganaxolone is an orally active analog of allopregnanolone that is not converted to the hormonally active 3-keto form. The enhanced anticonvulsant potency of ganaxolone after neurosteroid withdrawal supports the use of ganaxolone as a specific treatment for perimenstrual catamenial epilepsy.
human ... GABRA1(2554)
mouse ... Gabrg2(14406)
G2536 Ganciclovir ≥99% (HPLC), powder Ganciclovir is a pro-drug nucleoside analog that is activated by phosphorylation. It is useful in the study of gene therapy in cancer research.
Upon expression of a viral suicide gene encoding thymidine kinase, the non-toxic pro-drug is converted to a phosphorylated active analog and is incorporated into the DNA of replicating eukaryotic cells, causing death of the malignant dividing cell. The cell cycle is irreversibly arrested at the G2-M checkpoint. Gap junction involvement in the ganciclovir bystander effect has been studied. Ganciclovir has been used to study loss of telomeres and to evaluate sensitivity of viruses to antiviral treatments.
 
SML0241   Ganirelix acetate salt ≥95% (HPLC) Ganirelix is a decapeptide GnRH antagonist. Ganirelix acts by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of LH and FSH.
 
G8923 GANT58 ≥98% (HPLC) GANT58 is a Hedgehog signaling pathway inhibitor. GANT58 inhibits the hedgehog signaling pathway downstream of Smo. GANT58 inhibits Gli transcriptional activity, and reduces cellular levels of the Hh pathway components Gli1, Shh, and patched.
 
G9048   GANT61 ≥98% (HPLC) GANT61 blocks hedgehog pathway signaling by inhibiting the transcripional activity of Gli1 (IC50 = 5 μM). GANT 61 led to a regression of 22Rv1 human prostate tumor cell xenografts in nude mice.
 
SML1426   Gap19 trifluoroacetate salt ≥95% (HPLC) Gap19, nonapeptide from the cytoplasmic loop of Connexin-43, is a selective blocker of connexin 43 (Cx43) hemichannel that does not block GJ or Cx40/Panx-1 channels in cardiomyocytes and astrocytes. Gap19 prevents Cx43 hemichannel opening and protect against myocardial ischemia/reperfusion injury.
 
SML0877   Gardiquimod ≥98% (HPLC) Gardiquimod is a potent and specific agonist for human or mouse Toll-like receptor 7 (TLR7). Also, at high concentration gardiquimod activates TLR8. Similarly to imiquimod, gardiquimod could mimic the effects of viral nucleic acids on the immune system.
 
SML1618 Garenoxacin mesylate monohydrate ≥98% (HPLC) Garenoxacin is a broad spectrum fluoroquinolone antibiotic suitable for treatment of gram-positive and gram-negative bacterial infections. Garenoxacin has a low mutant prevention concentration and a narrow mutant selection window. Data shows that garenoxacin has anti-inflammatory properties. It significantly alleviates LPS-induced IL-8 production through the negative regulation of the ERK1/2 pathway both in the human airway epithelial cell line A549 and the monocyte cell line THP-1.
 
SML1926 GAT211 ≥98% (HPLC) New GAT211 is a positive allosteric modulator (PAM) of cannabinoid CB1 receptor signaling. GAT211 was found to amplify the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. GAT211 caused a CB1-dependent suppression of paclitaxel-induced mechanical and cold allodynia with no sign of tolerance over 19 days of administration.
 
D052 GBR 12909 dihydrochloride solid, ≥98% (HPLC) Highly selective dopamine reuptake inhibitor with behavioral effects similar to cocaine.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
G9659 GBR 12935 dihydrochloride ≥98% (TLC), powder Inhibits the dopamine and norepinephrine transporters with Kis of 21.5 nM and 225 nM, respectively. Does not inhibit the serotonin transporter (Ki = 6.5 μM). Binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.
 
SML1657 Gefitinib ≥98% (HPLC) Gefitinib is a selective epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Gefitinib has antineoplastic activity, and has been approved for the treatment on non-small cell lung cancer (NSCLC).
 
G3381 Geldanamycin from Streptomyces hygroscopicus ≥98% (HPLC), powder Geldanamycin is a potent antitumor antibiotic active at nanomolar concentration against 60 cell lines.
Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, Geldanamycin is a potent inhibitor of the nuclear hormone receptor family.
 
SML0985 Geldanamycin-Biotin ≥98% (HPLC) Geldanamycin-Biotin is a benzoquinone ansamycin antitumor antibiotic. Geldanamycin binds specifically to Hsp90 (HeatShock Protein 90). and to its endoplasmic reticulum homologue GP96. The Hsp90 chaperone is required for the activation of several families of eukaryotic protein kinases and nuclear hormone receptors, many of which are proto-oncogenic and play a prominent role in cancer. The geldanamycin antibiotic has antiproliferative and antitumor effects, as it binds to Hsp90, inhibits the HSP90-mediated conformational maturation/refolding reaction, and results in the degradation of Hsp90 substrates. Hsp90 also plays a key role in regulating the physiology of cells exposed to environmental stress and thus, geldanamycin interferes with cellular stess response.
 
SML1277   Geldanamycin-FITC ≥98% (HPLC), from Streptomyces hygroscopicus Geldanamycin is a potent antitumor antibiotic active at nanomolar concentration against 60 cell lines. Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, Geldanamycin is a potent inhibitor of the nuclear hormone receptor family.
 
SML1278   Geldanamycin Ready Made Solution 1 mg/mL, from Streptomyces hygroscopicus Geldanamycin is a potent antitumor antibiotic active at nanomolar concentration against 60 cell lines. Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, Geldanamycin is a potent inhibitor of the nuclear hormone receptor family.
 
G6423 Gemcitabine hydrochloride ≥98% (HPLC) Gemcitabine is a widely used antitumor agents in both clinics and research labs. It is an antineoplastic agent and antimetabolite.
 
G9518 Gemfibrozil Gemfibrozil selectively increases Apolipoprotein A-I levels. In yeast cells, application of gemfibrozil delays the start of DNA replication. It is used as a therapeutic agent for dyslipidemia.
 
SML1625 Gemifloxacin mesylate ≥98% (HPLC) Gemifloxacin is a broad-spectrum quinolone antibacterial. Fluoroquinolones stabilize DNA strand breaks created by DNA gyrase and topoisomerase IV by binding to the enzyme-DNA complex generating persistent, covalent enzyme–DNA adducts, inhibiting DNA synthesis. Gemifloxacin is used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin has also been found to inhibit migration and invasion of human colon cancer cells.
 
G4796 Genipin ≥98% (HPLC), powder Genipin stimulates insulin secretion in UCP2-dependent manner (Uncoupling protein 2). Genipin is a protein, collagen, gelatin, and chitosan cross-linker.
 
SML0153 Geniposide ≥98% (HPLC) Geniposide is an iridoid glycoside with a variety of biological activities including neuroprotective, anti-diabetic, antiproliferative, and antioxidative activity. Geniposide has been shown to regulate Nrf2 translocation and upregulate downstream antioxidant protein HO-1 expression through the PI3K/Akt signaling pathway, which may account for its neuroprotective and antioxidative activity. Glucagon-like peptide 1 (GLP-1) receptor may also play a critical role in geniposide induced HO-1 expression.
 
G6649 Genistein synthetic, ≥98% (HPLC), powder Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
human ... AKT1(207), CYP19A1(1588), EGFR(1956), ESR1(2099), ESR2(2100)
mouse ... Esr1(13982), Hexa(15211)
rat ... Adora1(29290), Adora2a(25369), Ar(24208)
G6776 Genistein from Glycine max (soybean), ~98% (HPLC) Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
human ... AKT1(207), CYP19A1(1588), EGFR(1956), ESR1(2099), ESR2(2100)
mouse ... Esr1(13982), Hexa(15211)
rat ... Adora1(29290), Adora2a(25369), Ar(24208)
G0897 Genistin from Glycine max (soybean), ≥95% (HPLC) Inactive analog of genistein; useful as a negative control for genistein and other tyrosine kinase inhibitors.
Selective inhibitor of mammalian terminal deoxynucleotidyl transferase (TdT), with no measurable effect on mammalian or microbial DNA polymerases.
 
UC18 (±)-Geosmin ≥97% (GC) Geosmin is a naturally occurring biomolecule that contributes to the earthy or musty flavor and odor in water supplies. This water contaminant can be detected by humans at ng/l (parts per trillion) concentrations.
 
G5048 Geranylgeranylacetone Geranylgeranylacetone can induce expression of HSP70, HSPB8, and HSPB1. Induction of HSP70 expression is protective against the development of various diseases, such as inflammatory bowel disease, hypoxic/ischemic brain injury and spinal and bulbar muscular atrophy (cytoprotective and anti-inflammatory effects). Reports indicate that GGA protects against NSAID-induced gastric and intestinal lesions by induction of HSP70 expression. Other studies have shown that GGA induces expression of HSPB8 and HSPB1 and reduces the formation of amyloid oligomers as well as insoluble aggregates in HSPB5 R120G TG mice.
 
G6025 Geranylgeranyl pyrophosphate ammonium salt solution, ≥95% (TLC), ~1 mg/mL in methanol: NH4OH (7:3) Isoprenoid from the intracellular mevalonate pathway used for prenylation of several low molecular weight G proteins, including Ras. Intermediate in terpene biosynthesis.
 
SML0292 Gestodene ≥98% (HPLC) Gestodene is a synthetic progestin used as a contraceptive. Gestodene displays a high binding affinity to the progesterone receptor, and also binds strongly to adrogen and glucocorticoid receptors.
 
B6292 GF 109203X hydrochloride ≥95% Inhibitor of protein kinase C; potent inhibitor of GSK-3.
 
G5294 GGTI-2133 ≥98% (HPLC), solid GGTI-2133 is a cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I; IC50 = 38 nM) with a 140-fold selectivity over farnesyltransferase (FTase; IC50 = 5.4 μM).
human ... FNTA(2339), PGGT1B(5229)
SML1186   GGTI-286 dihydrochloride ≥90% (HPLC) GGTI-286 is a cell permeable, potent and selective inhibitor of geranylgeranyltransferase I (GGTase I) that selectively disrupts oncogenic K-Ras4B. New study shows that GGTI-286 reduces nuclear localization of β-catenin.
 
G5169 GGTI 298 trifluoroacetate salt hydrate ≥90% (HPLC), film GGTI 298 is a cell-permeable, prodrug form of the geranylgeranyltransferase I (GGTase I) inhibitor GGTI-297. It inhibits the processing of Rap 1A without effecting the processing of H-Ras.
human ... PGGT1B(5229)
SML0789 GI254023X ≥98% (HPLC) GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). In a study using recombinant TACE and ADAM10 ectodomain, the IC50 for GI254023X was 5.3 nM for ADAM10 vs 541 nM for TACE.
GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor.
 
SML0184 Ginsenoside Rg3 ≥98% (HPLC) Ginsenoside Rg3 is a natural product isolated from Panax ginseng. Similar to other ginsenosides it exhibits cardio protective effects. Ginsenoside Rg3 enhances cardiac, hERG (IKr) and KCNQ (Iks), channel currents by interaction with the channel pore entryway. It also inhibits the palmitate-induced apoptosis of MIN6N8 mouse insulinoma beta-cells through modulating p44/42 MAPK activation. Ginsenoside Rg3 increases the level of the transcription factor Nrf2 and induces the mRNA levels of multidrug resistance-associated protein (Mrp) 1 and Mrp3. Rg3 modulate neuroinflammation by attenuating the activation of microglia in response to systemic LPS treatment. It activates AMPK in HepG2 cells and reduces the lipid accumulation thereby decreasing the risk of cardiovascular disease due to dyslipidemia.
 
PZ0172 Gisadenafil besylate salt ≥98% (HPLC) Gisadenafil (UK 369003) is a PDE5 inhibitor. It is 80 fold selective over PDE6, and greater than 3000 fold selective over PDEs 1-4 and 7.
 
SML1772 Givinostat hydrochloride hydrate ≥95% (HPLC) Givinostat (ITF2357) is a hydroxamate HDAC inhibitor that inhibits class I and class II enzymes. Givinostat posseses a very promising activity profile in multiple myeloma and acute myelogenous leukemia in vitro and in vivo. Givinostat also has anti-inflammatory activity and inhibits the secretion of the tumor necrosis factor-alpha (TNF-α), IL-1, and IL-6. Givinostat has been in multiple Phase 2 studies for both inflammatory diseases (Duchenne Muscular Dystrophy , Juvenile arthritis, Polycythemia Vera) and blood cancers (myelomas and lymphomas).
 
SML0849   GKA50 ≥98% (HPLC) GKA50 is a specific activator of glucokinase (EC50 = 0.03 μM). In mouse MIN6 insulin-secreting cells and rat pancreatic islet cells, GKA50 elicits a leftward shift in response to sub-maximal glucose concentrations as measured by insulin secretion and elevation of intracellular calcium levels.
 
G9548 Glabridin ≥98% (HPLC), powder Glabridin is a bio-available isoflavan isolated from licorice (Glycyrrhiza glabra L.) root extract. Glabridin has been reported to posses varies biological activities including strong antioxidant activity, antioxidant against LDL oxidation, anti-Helicobacter pylori properties, estrogen-like activity and antinephritic and radical scavenging activities. Also it appears to inhibit serotonin re-uptake, melanogenesis, inflammation and cytochrome P450 3A4, 2B6, and 2C9.
 
G2167 Gliclazide powder, ≥98% Oxidative modification of low-density lipoprotein (LDL) plays an important role in vascular dysfunction associated with diabetes mellitus. Gliclazide is a second-generation sulfonylurea with free-radical-scavenging activity. Incubation of human aortic smooth muscle cell (HASMC) with native human LDL (100 μg/mL) in the presence of increasing concentrations of gliclazide (1 to 10 μg/mL) resulted in a dose-dependent decrease in HASMC-mediated LDL oxidation. Exposure of HASMCs to gliclazide (1 to 10 μg/mL) and native LDL (100 μg/mL) also led to a dose-dependent decrease in oxidized LDL-induced human monocyte adhesion to HASMCs. In addition, incubation of HASMCs with gliclazide dramatically reduced the ability of oxidized LDL to stimulate the proliferation of these cells. Finally, treatment of HASMCs with gliclazide resulted in a marked decrease in oxidatively modified LDL-induced monocyte chemoattractant protein (MCP)-1 and human heat shock protein 70 (HSP 70) expression, both at the gene and protein levels. These results show that gliclazide, at concentrations in the therapeutic range (5 to 10 μg/mL), is effective in vitro in reducing vascular smooth muscle cell (VSMC) dysfunction induced by oxidatively modified LDL. Administration of gliclazide to type 2 diabetic patients could form part of the strategy for the prevention and management of diabetic cardiovascular diseases
human ... KCNJ1(3758)
G2295 Glimepiride ≥98% (HPLC), solid Glimepiride is a potent blocker of cardiac KATP channels activated by pinacidil with an IC50 of 6.8 nM.
human ... KCNJ1(3758)
G9893 Gliotoxin from Gliocladium fimbriatum An antiphagocytic and immunomodulating agent that acts by blocking membrane thiol groups.
 
G117 Glipizide solid ATP-dependent K+ channel blocker.
human ... KCNJ1(3758)
G8048   GLP-1R agonist ≥98% (HPLC) GLP-1R is a small molecule GLP-1 receptor agonist. GLP-1 receptor signaling is a predominant mechanism for regulating glucose homeostasis. This compound represents a unique non-peptide tool for studying the role of GLP-1 in both in vivo and in vitro diabetes and obesity models.
 
G3291 Glutamate, Caged hydrate powder Glutamate derivative that is resistant to hydrolysis and biologically inert prior to photolysis.
 
SML1327   Glutaminase Inhibitor 968 ≥98% (HPLC) Glutaminase Inhibitor 968 is an allosteric inihibitor of the mitochondrial enzyme glutaminase C (GAC), which is overexpressed in a number of cancer cell lines. Glutaminase Inhibitor 968 shows 21% inhibition at 10 μM, 94% at 25 μM. Glutaminase Inhibitor 968 blocked human cancer cell proliferation in culture, and in inhibited tumor formation in mouse xenograft models.
 
G8291 Glu-Val-Asn-[(2R,4S,5S)-5-amino-4-hydroxy-2,7-dimethyloctanoyl]-Ala-Glu-Phe >93% (HPLC), solid Inhibitor of brain β-secretase
 
G0639 Glybenclamide ≥99% (HPLC) Selectively blocks ATP-sensitive K+ channels; high affinity binding sites found in brain, pancreatic β cells, and cardiovascular system.
human ... KCNH2(3757), KCNJ1(3758), KCNJ11(3767)
rat ... Kcnj1(24521)
SML0029 Glycopyrrolate ≥98% (HPLC) Glycopyrrolate is long-acting muscarinic antagonist (LAMA). It is kinetically selective muscarinic M3 receptor antagonist.
 
SML0109 GLYX-13 trifluoroacetate ≥98% (HPLC) GLYX-13 is a glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor (NMDAR). It is a brain penetrable tetrapeptide which acts as a positive allosteric modulator of the NMDA receptor, acting via the glycine site. GLYX-13 has been found to be a cognitive enhancer in learning models and is currently in clinical trials as an antidepressant.
 
SML0874 GMQ hydrochloride ≥95% (HPLC) GMQ/2-Guanidine-4-methylquinazoline is a potent and selective modulator of acid-sensing ion channel (ASIC) that activates ASIC3 channels under neutral pH. GQM blocks acid-induced maximal peak current and alters ASICs pH dependence for activation and inactivation.
 
SML0646   GMX1778 ≥98% (HPLC) GMX1778 (CHS-828) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) that exhibits a potent anticancer activity both in vitro and in vivo. GMX1778 exerts a cytotoxic effect by decreasing the cellular level of NAD+. GMX1778 increases intracellular ROS in cancer cells but does not induce ROS in normal cells.
 
G9420 GNF-2 ≥98% (HPLC), solid GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.
 
SML0511 GNF-5 ≥98% (HPLC) GNF-5 is a BRC-Abl inhibitor.
 
SML1501   GNF-7 ≥98% (HPLC) GNF-7 is a multi-targeted kinase inhibitor that inhibits RAS signaling in addition to inhibiting the T315I “Gatekeeper” mutant of Bcr-Abl. GNF-7 inhibits NRAS-dependent cells in pre-clinical models of AML and ALL and inhibited T315I-Bcr-Abl dependent tumor growth in a murine model of CML.
 
SML1878 GNF-1331 ≥98% (HPLC) GNF-1331 is an orally available, potent and selective Porcupine (PORCN) inhibitor.
 
SML0844   GNF 5837 ≥98% (HPLC) GNF-5837 is an orally bioavailable Trk inhibitor (IC50 = 8 and 12 nM for TrkA and TrkB, respectively). GNF-5837 inhibits growth of Ba/F3 cells expressing Tel-Trl fusions. IC50 values for growth inhibition are Tel-TrkA = 11 nM, Tel-TrkB = 9 nM and Tel-TrkC = 7 nM.
 
G1918 Gö 6983 ≥97% Protein kinase C (PKC) inhibitor that selectively inhibits several PKC isozymes (IC50 = 7 nM for PKCα and PKCβ; 6 nM for PKCγ; 10 nM for PKCδ; and 60 nM for PKCζ), but does not inhibit PKCμ (IC50 = 20 mM).
 
G0923 Golgicide A ≥98% (HPLC) Golgicide A is a potent, highly specific, reversible inhibitor of the cis-Golgi ArfGEF GBF1. Arf proteins are members of the Ras superfamily of small guanosine triphosphatases (GTPases) that mediate vesicular transport. Golgicide A binds within an interfacial cleft formed between Arf1 and the GBF1 Sec7 domain. Golgicide A is a unique and powerful tool for further elucidating the mechanisms underlying assembly and transport within the Golgi, comparable to the use of dynasore for studying the dynamics of dynamin-mediated clathrin coat formation.
 
SML1251 Gomisin A ≥98% (HPLC) Gomisin A is a major dibenzocyclooctadiene lignan from medicinal plant Schizandra Chinese that exhibit a wide variety of interesting biological activities, including hepatoprotective, antiviral, anticancer, neuroprotective and anti-inflammatory. Gomisin A suppressed the expressions of iNOS and COX-2 in LPS-stimulated N9 microglia through suppression of NF-κB/MAPKs pathway.
 
SML0761 Gossypin ≥90% (HPLC) Gossypin is an anti-inflammatory pentahydroxyflavone glucoside isolated from Hibiscus vitifolius that is used as an herbal remedy for diabetes, jaundice, and inflammation. Gossypin potently inhibits human cancer cell proliferation, including melanoma and glioma cells. Gossypin directly binds and inhibits BRAFV600E and CDK4 kinases, and also regulates Chk1 and Cdc25C in U251 glioma cells.
 
G8761 (±)-Gossypol from cotton seeds ≥95% (HPLC) Gossypol is a male antifertility agent and PAF antagonist/inhibitor. Gossypol is a poisonous pigment found in cottonseed and its name is derived from the botanical name of the cotton plant, Gossypium.. Gossypium is extracted from selected hybrid species between two Gossypium species, Gossypium hirsutum and Gossypium barbadens. As a PAF antagonist/inhibitor, Gossypium markedly inhibited the contractile responses of guinea pig lung parenchyma strips stimulated with leukotriene B4, seukotriene D4, and PAF-acether.
human ... AKR1B1(231), BAD(572), BCL2(596), LDHA(3939), LDHB(3945), MCL1(4170)
SML1207 GPBAR-A ≥98% (HPLC) GPBAR-A is a very potent agonist of the bile acid receptor GPBA (also known as TGR5). In murine primary intestinal cultures, GPBAR-A induces an elevation in intracellular cAMP and calcium levels, and stimulates secretion of GLP-1.
 
SML0174 GPR35 Agonist, Compound 10 ≥98% (HPLC) GPR35 agonist Compound 10 is a GPR35 agonist the binds with higher affinity than other known agonists, such as kynurenic acid and zaprinast. Compound 10 was more potent than zaniprast (pEC50 = 5.3 vs 4.18) for recombinantly expressed human GPR35, and unlike zaprinast, is equipotent for human and rat GPR35
 
SML0135 GPV574 ≥98% (HPLC) GPV574 is a derivative of the Class 1C antiarrhythmic drug propafenone. GPV574 inhibits the delayed rectifier K+ channel HERG with similar affinity and time constant as propafenone (IC50 = 5 mM), but unlike the parent compound, does not remain permanently trapped in the channel pore. After wash-out of GPV574, channel activity is recovered within 60 seconds.
 
G0544 GR 103691 ≥98% (HPLC), solid D3 dopamine receptor antagonist.
rat ... Htr1a(24473)
G5918 GR 113808 ≥98% (HPLC), solid GR 113808 is a 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
rat ... Htr3a(79246), Htr4(25324)
G5793 GR 127935 hydrochloride hydrate >98% (HPLC), powder Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
human ... HTR1B(3351), HTR1D(3352)
SML0780   GR203040 ≥98% (HPLC) GR203040 is a high affinity, non-peptide tachykinin NK1 receptor antagonist. GR203040 inhibits substance P binding to human NK1 receptors in CHO cells with a pKi or 10.3. The compound prevents emisis, and reduces bladder damage induced by radiation, cisplatin and cyclophosphamide. 11C-labeled GR203040 is used as a radioligand to image NK1 receptors in the CNS by PET scanning.
 
G5044 GR 32191B ≥98% (HPLC), solid Selective TP prostanoid receptor antagonist. Inhibits U-46619-induced contraction of guinea pig trachea with IC50=1.8 nM.
 
G133 GR 89696 fumarate salt solid Selective κ2 opioid receptor agonist.
human ... OPRK1(4986)
G5002   Gramicidin from Bacillus aneurinolyticus (Bacillus brevis) Linear polypeptide antibiotic complex. A mixture of gramicidins A, B, C, and D. Linear polypeptide antibiotic, a mixture of gramicidin A, B, C, and D. Gramicidin D, a channel-forming ionophore that flip-flops slowly across the membrane is a known Pgp substrate and surprisingly was found to inhibit Pgp ATPase activity. This inhibition was reversed by other Pgp substrates suggesting a common drug binding site among MDR substrate-type drugs and chemosensitizers.
 
G3796 Granisetron hydrochloride ≥98% (HPLC), solid Granisetron hydrochloride is a serotonin 5-HT3 receptor antagonist and antiemetic.
 
P8895   Grass pollens from Poa pratensis (Kentucky blue)    
SML0544   GRI977143 ≥98% (HPLC) GRI977143 is a potent, specific LPA2 receptor agonist with no affinity for other LPA receptors. GRI977143 inhibits the initiation of apoptosis induced by adriamycin or serum withdrawal in MEFs derived from LPA2 knock-out mice transfected with an LPA2 expression vector, but has no affect in non-transfected cells.
 
G4753 Griseofulvin from Penicillium griseofulvum, 97.0-102.0% Antifungal. Mode of action: Disrupts the mitotic spindle structure and inhibits nuclear division. Induces apoptosis in human tumor cell lines.
 
PZ0293 GRN-529 ≥97% (HPLC) GRN-529 is a brain penetrant, potent and selective negative allosteric modulator of the mGluR5 receptor (metabotropic glutamate receptor subtype 5) with an IC50 of 3.1 nM and >1000-fold selectivity vs mGluR1. GRN-529 was shown to alleviate multiple diagnostic behavioral symptoms of autism in BTBR and C58 mice models.
 
SML1520 GS39783 ≥98% (HPLC) GS39783 is a positive allosteric modulator (PAM) of GABA-B receptors. GABAB receptor positive allosteric modulators have potential for treatment of many neuro-psychiatric disorders as well as drug dependence and seizures. The receptor is a GPCR expressed throughout the CNS; it acts as both an auto-receptor and heteroreceptor to modulate GABA release and regulate K+ channels and Ca++ channels. GS39783 has been shown to inhibit alcohol self-administration and to have an antipsychotic-like effect in animal models of addiction and schizophrenia, respectively.
 
SML1746 GS87 ≥95% (HPLC) GS87 is a highly specific GSK3 (glycogen synthase kinase 3) inhibitor that induces extensive differentiation of AML cells. GS87 potently inhibits growth of AML cells in mice with little effect on normal bone marrow cells. GS87 causes terminal differentiation of AML cells.
 
SML1171 GSA-10 ≥98% (HPLC) GSA-10 is a novel, potent activator of the smoothened receptor (Smo). GSA-10 binds to Smo at a unique site compared to agonists such as SAG and purmorphamine, and is not affected by the Smo antagonist cyclopamine. GSA-10 promotes the differentiation of mesenchymal pluripotent C3H10T1/2 cells into osteoblasts.
 
G5797 GSK0660 ≥98% (HPLC) GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (160 nM). GSK0660 is nearly inactive on PPARα and PPARγ with IC50s greater than 10 μM.
 
G0798 GSK1016790A ≥98% (HPLC) GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).
 
SML0083 GSK 1059615 sodium salt hydrate GSK 1059615 is a phosphatidylinositol-3-kinases (PI3K) inhibitor. GSK 1059615 inhibits proliferation of breast cancer BT474 cells via four different mechanisms that include retinoblastoma 1 (RB1)-mediated cell cycle arrest, elevated forkhead box protein O1 (FOXO) signaling, deduced MYC and transferrin receptor (TFRC) signaling and decreased cellular metabolism. Additionally, GSK 1059615 can suppress cell proliferation by decreasing mitogen-activated protein kinase (MAPK) signaling and imparts sensitivity to phosphoinositide 3-kinase (PI3K) inhibitor in cells resistant to the protein kinase B or AKT inhibitor. GSK 1059615 functions as a druggable target to reduce radiation-induced apoptosis in NCCIT cells. GSK 1059615 has entered clinical trial in patients with solid tumors or lymphoma and refractory malignancies.
GSK 1059615 is a potent inhibitor of PI3 Kinase. (IC50 = 2 nM)
 
SML0666   GSK1210151A ≥98% (HPLC) GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. GSK1210151A displaces BRD3 and BRD4, PAFc and SEC components from chromatin resulting in inhibition of transcription at key genes (BCL2, C-MYC and CDK6) involved in the initiation of mixed lineage leukemia (MLL). GSK1210151A (I-BET151) showed good efficacy in 2 MLL animal models.
 
SML1152 GSK137647A ≥98% (HPLC) GSK137647A is a selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which is involved in long-chain fatty acid stimulated GLP-1 secretion and has been implicated in glucose homeostasis, adiposity, and regulation of the anti-inflammatory response. GSK137647A has pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3.
 
SML0995   GSK1838705A ≥98% (HPLC) GSK1838705A is a cell penetrant anti-tumor agent that potently inhibits the insulin-like growth factor-I receptors (IGF-IR), insulin receptors (IR) and anaplastic lymphoma kinase (ALK). GSK1838705A potently inhibits cell proliferation of multiple solid and hematologic cancers and retards the growth of human tumor xenografts. GSK1838705A does not significantly affect other kinases. GSK1838705A has minimal effects on glucose homeostasis in mice.
 
SML1617 GSK2033 ≥98% (HPLC) GSK2033 is an antagonist of the nuclear receptor liver-X-receptor (LXR) with pIC50 values of 7.0 for LXRα and 7.4 for LXRβ. Treatment of murine CD41 T cells with GSK2033 enhanced cellular proliferation and Th1/Th2/Th17 differentiation. In another study, the conjugated linoleic acid (CLA)-induced expression of efflux protein ATP-binding-cassette transporter A1 (ABCA1) was completely abolished by preincubation with GSK2033, showing that CLA mediated regulation of ABCA-1 expression is LXR dependent.
 
SML0942   GSK2193874 ≥98% (HPLC) GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.
 
SML1259 GSK2194069 ≥97% (HPLC) GSK2194069 is a fatty acid synthase (FAS) inhibitor. GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM for the overall hFAS reaction. FAS is upregulated in some cancers, including prostate cancer. GSK2194069 was found to inhibit tumour growth in prostate cancer C42b cell xenografts generated in Nod-SCID-gamma mice. Cellular FAS inhibition reduced cell growth were also demonstrated in non-small-cell lung (A549) cancer cell lines with an average EC50 of 15 ± 0.5 nM.
 
SML0217 GSK2334470 ≥98% (HPLC) GSK2334470 is a highly specific and potent inhibitor of PDK1 (3-Phosphoinositide dependent protein kinase-1). GSK2334470 can be used in cells to ablate T-loop phosphorylation and activate SGK, S6K1 and RSK as well as suppress the activation of Akt.
 
SML0660   GSK2578215A ≥98% (HPLC) GSK2578215A is a potent inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson’s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped that LRRK2 inhibitors may be useful in treating the disease. GSK2578215A inhibited both wild-type and G2019S mutant LRRK2 kinase activity with IC50s of 10.9 and 8.9 nM respectively. It has good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.
 
SML0768 GSK2801 ≥98% (HPLC) GSK2801 is a potent inhibitor of the BAZ2 family of bromodomain containing proteins. BAZ2A is an essential component of the nucleolar remodeling complex (NoRC), which mediates recruitment of histone modifying enzymes and DNA methylase involved in the silencing of ribosomal RNA transcription. BAZ2B is believed to be involved in regulating nucleosome mobilization along linear DNA. For full characterization details, please visit the GSK2801 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1048   GSK2830371 ≥98% (HPLC) GSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1, also known as PPM1D/ PP2Cδ), an oncogenic type 2C serine/threonine phosphatase that negatively regulates key proteins in the DNA damage–response pathway. GSK2830371 is selective for Wip1 with an IC50 of 6 nM against Wip1 compared to >10 μM IC50 for PPM1A & PPM1K, and >30 μM IC50 for 22 other phosphatases tested. GSK2830371 is believed to interact with the flap subdomain located near the Wip1 catalytic site, a feature that distinguishes Wip1 from other members of the protein phosphatase 2C (PP2C) family. GSK2830371 increased phosphorylation of Wip1 substrates and caused growth inhibition in both hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53.
 
SML1684 GSK2850163 ≥98% (HPLC) GSK2850163 is a highly selective inhibitor of inositol requiring enzyme-1 alpha (IRE1α) with dual activity: it inhibits IRE1α kinase activity with an IC50 value of 20 nM and RNase activity with an IC50 value of 200 nM. IRE1α is a dual serine/threonine-protein kinase/endoribonuclease with two enzymatic domains: a trans-autophosphorylation domain and and endoribonuclease (RNase) domain. When activated, usually in response to endoplasmic reticulum (ER) stress such as the unfolded protein response (UPR), IRE1α oligomerizes and activates mRNA splicing of adaptive XBP1 transcription factor, which upregulates ER chaperones and ER associated degradation (ERAD) genes that promote degradation of ER unfolded proteins and facilitate recovery from ER stress. However, if ER stress is too high or chronic, IRE1α is hyperactivated, increasing many ER mRNAs, resulting in apoptosis. GSK2850163 interacts with IRE1α catalytic residues Lys599 and Glu612, displacing the kinase activation loop to the inactive DFG-out conformation. The rearrangement of the kinase domain-dimer interface also results in the RNAse domains rotating away from each other, inhibiting the RNase activity.
 
SML0500 GSK334429 hydrochloride ≥98% (HPLC) GSK334429 is a selective histamine H3 receptor antagonist. H3 antagonists increase the release of brain histamine, ACh, NE and DA neurotransmitters that modulate cognitive processes. Studies look at their analgesic efffects including efficacy for neuropathic pain.
 
SML0766 GSK343 ≥98% (HPLC) GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC50 for inhibition of H3K27 methylation is < 200 nM in HCC1806 cells. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
G7423 GSK3787 ≥98% (HPLC), white to off-white, powder GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5). It acts by covalently modifying Cys249 within the ligand binding pocket, and has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells.
 
G0673 GSK4112 ≥98% (HPLC) GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.
 
SML0231   GSK-429286 ≥98% (HPLC) GSK-429286 is a potent, selective, orally available Rho kinase (ROCK1) inhibitor and reduced arterial pressure in spontaneously hypertensive rats
 
G6173 GSK 4716 ≥98% (HPLC) GSK 4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
 
SML1658 GSK484 ≥98% (HPLC) GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC50 values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1–11 even at 100 μM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a β-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0262 GSK575594A ≥98% (HPLC) GSK575594A is a selective agonist of human GPR55. It is specific for human over rodent GPR55. GSK575594A had no activity across a set of more than 200 validated molecular target assays from diverse classes including kinases, proteases and other enzymes, GPCRs, ion channels, nuclear receptors, and membrane transporters.
 
SML1751 GSK591 ≥97% (HPLC) GSK591 is a SGC probe for PRMT5. GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex. For full characterization details, please visit the GSK591 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0773   GSK-650394 ≥98% (HPLC) GSK-650394 is a potent and selective Serum- and glucocorticoid-regulated kinase 1 (SGK1) antagonist.
 
SML0428 GSK690693 ≥98% (HPLC) GSK690693 is an ATP competitive, potent pan-AKT kinase inhibitor with IC50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively.
 
G5547   GSK837149A ≥98% (HPLC), solid GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors.
 
SML1757 GSK864 ≥98% (HPLC) GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. It appears that GSK864 binds to an allosteric binding site and locks WT and mutant IDH1s in a catalytically inactive conformation. GSK864 is a highly bioavailable analog of GSK321. For full characterization details, please visit the GSK864 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
 
SML1824 GSK983 ≥98% (HPLC) GSK983 blocks RNA virus replication with EC50 values of 10–40 nM, and also blocks cell proliferation. GSK983 acts by inhibition of dihydroorotate dehydrogenase (DHODH), necesssary for pyrimidine biosynthesis. Exogenous deoxycytidine was able to reduce GSK983 cytotoxicity, allowing cells to synthesize DNA, but still preventing RNA virus replication. GSK983 was active against dengue fever and Venezuelan equine encephalitis viruses.
 
SML1825 GSK984 ≥98% (HPLC) GSK984 is an inactive control probe for GSK983, which is an inhibitor of dihydroorotate dehydrogenase (DHODH) with antiviral activity. GSK983 blocks RNA virus replication with EC50 values of 10–40 nM, and also blocks cell proliferation. GSK984 acts by inhibition of dihydroorotate dehydrogenase (DHODH), necesssary for pyrimidine biosynthesis. Exogenous deoxycytidine was able to reduce GSK983 cytotoxicity, allowing cells to synthesize DNA, but still preventing RNA virus replication. GSK983 was active against dengue fever and Venezuelan equine encephalitis viruses. GSK984, the (S)-isomer, is almost 200-fold less active, so would make a good control.
 
SML0709 GSK-J1 ≥98% (HPLC) GSK-J1 is a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. For full characterization details, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0701 GSK-J4 ≥98% (HPLC) GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. For characterization details for GSK-J4 and full characterization details for GSK-J1, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1072 GSK-LSD1 ≥98% (HPLC) GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. For full characterization details, please visit the GSK-LSD1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0326 GTS-21 ≥97% (HPLC) GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.
 
G110 Guanabenz acetate salt powder Centrally acting α2 adrenoceptor agonist; I2 imidazoline binding site ligand; antihypertensive.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
G1043 Guanfacine hydrochloride ≥98% (HPLC) α-2 noradrenergic receptor agonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
G3416 5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate solid, ≥98% (HPLC) Selective κ opioid receptor antagonist; GNTI is five-fold more potent and 500-fold more selective than norbinaltorphimine (nor-BNI) for the κ opioid receptor in smooth muscle preparations.
human ... OPRK1(4986)
G7504 Guanosine 3′,5′-cyclic monophosphate ≥98% (HPLC), powder An important second messenger, cGMP is a major intracellular mediator of extracellular signals such as nitric oxide and natriuretic peptides. Cyclic GMP interacts with three types of intracellular receptor proteins: cGMP-dependent protein kinases, cGMP-regulated channels, and cGMP-regulated cyclic nucleotide phosphodiesterases. A primary action of elevated cGMP levels in vivo is the stimulation of cGMP-dependent protein kinase (PKG).
 
G6129 Guanosine 3′,5′-cyclic monophosphate sodium salt ≥99% (HPLC), powder An important second messenger, cGMP is a major intracellular mediator of extracellular signals such as nitric oxide and natriuretic peptides. Cyclic GMP interacts with three types of intracellular receptor proteins: cGMP-dependent protein kinases, cGMP-regulated channels, and cGMP-regulated cyclic nucleotide phosphodiesterases. A primary action of elevated cGMP levels in vivo is the stimulation of cGMP-dependent protein kinase (PKG).
 
G136 Sp-Guanosine 3′,5′-cyclic monophosphorothioate triethylammonium salt solid Sp-cGMPS is a metabolically resistant activator of cGMP-dependent protein kinases.
 
G135 Guanosine 3′,5′-cyclic monophosphorothioate, Rp Isomer triethylammonium salt solid cGMPS-dependent protein kinase Iα inhibitor.
 
G7637 Guanosine 5′-[β-thio]diphosphate trilithium salt ≥85% (HPLC), powder    
G8634 Guanosine 5′-[γ-thio]triphosphate tetralithium salt ≥75% (HPLC), powder GTP-γ-S is a non-hydrolyzable GTP analog, known for its role as a G-protein activator. It has recently been shown to protect proteins from proteolytic degradation, stimulate GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization in vitro.
 
G5884 Guanosine 5′-triphosphate lithium salt ~95% (HPLC), powder GTP functions as a carrier of phosphates and pyrophosphates involved in channeling chemical energy into specific biosynthetic pathways. GTP activates the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades. Proliferation and apoptosis are regulated in part by the hydrolysis of GTP by small GTPases Ras and Rho. Another type of small GTPase, Rab, plays a role in the docking and fusion of vesicles and may also be involved in vesicle formation. In addition to its role in signal transduction, GTP also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
 
G8877 Guanosine 5′-triphosphate sodium salt hydrate ≥95% (HPLC), powder GTP functions as a carrier of phosphates and pyrophosphates involved in channeling chemical energy into specific biosynthetic pathways. GTP activates the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades. Proliferation and apoptosis are regulated in part by the hydrolysis of GTP by small GTPases Ras and Rho. Another type of small GTPase, Rab, plays a role in the docking and fusion of vesicles and may also be involved in vesicle formation. In addition to its role in signal transduction, GTP also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
human ... HRAS(3265)
SML0434 Gue1654 ≥98% (HPLC) Gue1654 inhibits signaling of the chemoattractant GPCR 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-oxo-ETE) receptor (OXE-R), but only signaling involving Gβγ, not Gα signaling triggered upon activation of the Gαi-βγ heterotrimer by OXE-R. Gue1654 is the first small-molecule inhibitor for the oxoeicosanoid receptor and the first to uncouple Gα and Gβγ signaling within a heterotrimer for any GPCR.
 
G5168 (Z)-Guggulsterone ≥89% (HPLC), powder (Z)-Guggulsterone is a natural product that lowers cholesterol due to its function as an antagonist ligand for the bile acid receptor. (Z)-Guggulsterone is a nuclear hormone receptor that regulates the transcription of several genes involved in cholesterol metabolism and plays a role in cholesterol level regulation. (Z)-Guggulsterone is also a selective farnesoid X receptor (FXR) modulator.
 
G007 Guvacine hydrochloride ≥97% (NMR), solid GABA uptake inhibitor.
human ... FGF9(2254), GABBR1(2550), GABBR2(9568), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
SML1551 GV-58 ≥97% (HPLC) GV-58 is a roscovitine analog that retains the ability to prolong the open state of calcium channels, but unlike roscovitine, is inactive against Cdk activity. GV-58 is a selective agonist of N-type and P/Q type calcium channels, which are critical to the triggering of neurotransmitter release at the neuromuscular junction. GV-58 has been studied as a possible therapeutic agent in a mouse model of Lambert-Eaton myasthenic syndrome (LEMS). The EC50 values for activation of N-, P/Q- and L- type calcium channels are 6.8, 9.9 and >100 μM, respectively.
 
G3295 GW0742 ≥98% (HPLC) GW0742 is a highly selective PPARδ agonist. EC50 = 1 nM vs 1 μM and 2 μM for PPARα and PPARγ, respectively.
human ... PPARA(5465), PPARD(5467), PPARG(5468)
G5668 GW1929 hydrate >98% (HPLC), solid GW1929 is a high affinity agonist of PPAR-γ.
human ... PPARG(5468)
SML1047   GW2580 ≥98% (HPLC) GW2580 is a cell-permeable, potent and selective ATP-competitive inhibitor of cFMS kinase, receptor for macrophage-colony stimulating factor, M-CSF or CSF-1, and a key regulator of macrophage and osteoclast activation and differentiation. FMS is a type III receptor tyrosine kinase that binds to the macrophage or monocyte colony-stimulating factor (M-CSF or CSF-1). Overexpression of CSF-1 and/or FMS has been implicated in a number of disease states including the growth of metastasis of some types of cancer, in promoting osteoclast proliferation in bone osteolysis, and in several inflammatory disorders. GW2580 selectively inhibits cFMS-mediated cellular functions in vitro at 0.06 μM as well as CSF-1-dependent tumor growth in vivo. GW2580 was inactive against 26 other kinases.
 
G0668 GW2974 ≥98% (HPLC), solid Potent and selective dual inhibitor of EGFR (IC50 = 0.016 mM) and ErbB-2 receptor tyrosine kinase.
human ... EGFR(1956), ERBB2(2064)
G6295 GW3965 hydrochloride ≥98% (HPLC), powder GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ. GW3965 has an EC50 = 125 nM in a cell-free ligand-sensing assay of LXRα and profiles as a full agonist on hLXRα and hLXRβ in cell-based assays with EC50 = 190 nM and 30 nM, respectively. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). The literature agonist, T0901317 (Tularik), had an EC50 = 60 nM and 85 nM in the cell-free and cell-based assays, respectively.
 
G1421 GW405833 hydrochloride ≥98% (HPLC), solid GW405833 is a selective cannabanoid CB2 receptor agonist; analgesic. GW405833 binds with high affinity at both human and rat CB2 receptors (Ki′s 3.9 and 3.6 nM); acts as a partial agonist (50% inhibition of forskolin-stimulated cAMP formation compared to full agonist CP55,940). GW405833 has potent analgesic activity in rat models of inflammatory, neuropathic and incisional pain; devoid of CNS effects common with CB1 agonists.
 
SML0855   GW438014A ≥98% (HPLC) GW438014A is a potent and selective neuropeptide Y Y5 receptor antagonist. GW438014A induces a potent reduction of food intake in rodents.
 
G3420 GW441756 hydrochloride ≥97% (HPLC), powder, red Highly selective and potent TrkA kinase inhibitor. Orally active. IC50 = 2 nM
 
D1692 GW4869 ≥90% (NMR) A cell-permeable, potent, specific, non-competitive inhibitor of N-SMase (neutral sphingomyelinase)
 
SML1491 GW501516 ≥98% (HPLC) GW501516 is a selective Peroxisome Proliferator-Activated Receptor delta (PPARδ) agonist with high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ and > 1000 fold selectivity over PPARα and PPARγ. GW501516 was shown to activate some of the same pathways activated through exercise, and was investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. However, GW501516 also showed an increase in cancer in rats.
 
G6416 GW5074 powder cRaf1 kinase inhibitor, immediately downstream of Ras in the MAPK signaling pathway.
human ... RAF1(5894)
SML0403 GW542573X ≥98% (HPLC) GW542573X is a very selective activator of the small conductance calcium-activated potassium channel SK1 (KCa2.1).
 
G3545 GW583340 dihydrochloride ≥97% (HPLC), solid Potent dual ErbB-2/EGFR tyrosine kinase inhibitor. IC50= 0.01 and 0.014 μM for EGFR and ErbB-2. Orally active.
 
G5045 GW6471 ≥98% (HPLC) GW6471 is a PPARα antagonist, which completely inhibits GW409544-induced activation of PPARα with an IC50 = 0.24 μM. GW6471 induces a PPARα conformation that interacts efficiently with co-repressors.
 
G6793 GW7647 ≥98% (HPLC) Potent human PPARα agonist. Use to study the biology of PPARα receptor in human cells.
human ... PPARA(5465)
SML0116 GW788388 Hydrate ≥98% (HPLC) GW788388 is a potent selective inhibitor of TGF-beta type I receptor [activin receptor-like kinase 5 (ALK5)]. GW788388 is orally available with a half-life of approximately 4 hours.
 
SML0230   GW-803430 ≥98% (HPLC) GW-803430 antagonizes central MCHR1 and produces anxiolytic, anti-depressant and anti-obesity effects in rats and mice. It also controls the alcohol-seeking behavior in rats and is a promising treatment for alcohol use-related disorders.
GW-803430 is a centraly active and selective melanin-concentrating hormone receptor (MCHR) 1 antagonist
 
G8173 GW833972A ≥98% (HPLC), powder GW833972A is a CB2 cannabinoid receptor agonist with 1000-fold selectivity relative to CB1. It is, however, 15-fold less potent than HU210 for CB2 (Ki 7.8 vs. 0.52 nM). The antitumor compound oxaliplatin induces marked hypersensitivity to cold, heat, and chemical pain stimuli (to the point where oxaliplatin therapy has to be discontinued). The hyperalgesia effect is almost completely blocked by pretreatment with GW833972A.
GW833972A is a CB2 receptor agonist with 1000-fold selectivity relative to CB1. GW833972A is 15 fold less potent than HU210 for CB2 (Ki 7.8 vs. 0.52 nM). The compound was used to determine the role of CB2 in airway sensory nerve function.
 
G2171 GW843682X ≥98% (HPLC), solid GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.
 
G7791 GW8510 solid GW8510 is an inhibitor of cyclin kinase 2 (CDK2). It prevents and/or reduces the side effects of chemotherapy (alopecia, plantar-palmar syndrome and mucositis).
human ... CDC2(983), CDK2(1017)
G9797 GW9508 ≥98% (HPLC) GW9508 is a selective FFA1/GPR40 agonist. GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have now been identified as free fatty acids (FFAs). The receptor, named FFA receptor 1, has been implicated in the pathophysiology of type 2 diabetes and is a drug target because of its role in FFA-mediated enhancement of glucose-stimulated insulin release. GW9508 showed greater than 500-fold selectivity for GPR40 over GPR41 and GPR43 and possessed a good in vitro and in vivo profile with excellent bioavailability. GW9508 stimulated intracellular Ca2+ mobilization in human embryonic kidney HEK-293 cells expressing GPR40 or GPR120, but not in the parent HEK-293 cell line. GW9508 dose dependently potentiated glucose-stimulated insulin secretion in MIN6 cells, but not in primary rat or mouse islets. GW9508 potentiates the KCl-mediated increase in insulin secretion in MIN6 cells.
 
M6191 GW9662 >98% (HPLC) GW9662 is an irreversible PPARγ antagonist. GW9662 inhibits connective tissue growth factor and activation of CD36 by IL-4.
human ... PPARG(5468)
G119 GYKI 52466 hydrochloride solid Selective allosteric AMPA receptor antagonist; anti­convulsant; skeletal muscle relaxant.
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
G7798   GYKI-53655 hydrate >99.0% (HPLC) GYKI-53655 is an AMPA antagonist and noncompetitive negative allosteric modulator.
 
G9423 GYPGQV trifluoroacetate salt ≥98% (HPLC), powder Protease-activated receptor-4 (PAR4) agonist
 
SML1256 Gyramide A hydrochloride ≥98% (HPLC) Gyramide A is a selective bacterial DNA gyrase inhibitor and bacteriostatic agent with an IC50 of 3.3 ± 1.0 μM. Gyramide A competitively inhibits the ATPase activity of Escherichia coli gyrase resulting in supercoiled DNA and stopping DNA replication. Unlike other DNA gyrase inhibitors ciprofloxacin and novobiocin, Gyramide A targets only DNA gyrase without inhibiting the closely related topoisomerase IV. Gyramide A is not as potent an antibiotic, but should be a more useful tool for studying bacterial gyrase.
 
SML0100 GYY4137 Dichloromethane complex ≥98% (HPLC) GYY4137 is a small molecule releaser of H2S with vasodilator and antihypertensive activity. H2S has been found to be an important biological mediator with multiple effects on neuromodulation, hypertension, inflammation, and vascular tone. GYY4137 should prove useful in the study of the many and varied biological effects of H2S.
 
SML0851   GZ-793A ≥98% (HPLC) GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles. GZ-793A is 50-fold selective for VMAT over the serotonin or dopamine transporters. VMAT2 has recently been considered a target for the treatment of methamphetamine abuse. In rat studies, GZ-793A decreased self-administration of methamphetamine with no development of tolerance.