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GNE-495
GNE-495 is a Selective MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) Inhibitor. IC50 value is 3.7 nM. GNE-495 shows excellent potency and good PK In vivo. GNE-495 was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that are observed in the inducible Map4k4 knockout mice. Synonyms: GNE-495; GNE 495; GNE495. 8-amino-N-(1-(cyclopropanecarbonyl)azetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide. Grades: 98%. CAS No. 1449277-10-4. Molecular formula: C22H20FN5O2. Mole weight: 405.43.
GNE-6776
GNE-6776 is a potent and non-covalent USP7 inhibitor with IC50 of 1.34 uM. GNE-6776 targets cellular USP7, MDM2, and p53 signalling pathways, and induces tumor cell death. Synonyms: GNE 6776; GNE-6776; GNE6776; 5-[6-amino-4-ethyl-5-(4-hydroxyphenyl)-3-pyridyl]-N-methyl-pyridine-2-carboxamide. Grades: 98%. CAS No. 2009273-71-4. Molecular formula: C20H20N4O2. Mole weight: 348.406.
GNE-7915
GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM. Synonyms: GNE7915; GNE 7915; GNE-7915. CAS No. 1351761-44-8. Molecular formula: C19H21F4N5O3. Mole weight: 443.403.
GNE-8525
This active molecular is a selective pan-TRK inhibitor. GNE-8525 shows potent antiproliferation activity (IC50 = 0.003 μM) and it shows in vivo antitumor efficacy in tumor xenograft model derived from the KM12 cell line. TRKA are believed to be the key oncogenic driver in many tumors including glioblastoma, melanoma and so on. Uses: Antitumor. Synonyms: GNF-8625; GNF 8625; GNF8625. (R)-1-(6-(6-(2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)-[2,4'-bipyridin]-2'-yl)piperidin-4-ol. Grades: 98%. CAS No. 1196546-33-4. Molecular formula: C31H30FN7O. Mole weight: 535.63.
GNF 5837
GNF 5837 is a potent and selective pan-Trk inhibitor that blocks tumor gowth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. GNF 5837 displays antiproliferative effects in cellular Ba/F3 assays with IC50 values of 7, 9 and 11 nM for cells expressing Tel-TrkC, Tel-TrkB and Tel-TrkA respectively. Synonyms: GNF5837; GNF-5837; GNF 5837. 1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-[4-methyl-3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]urea. CAS No. 1033769-28-6. Molecular formula: C28H21F4N5O2. Mole weight: 535.503.
GNF-6231
GNF-6231 is a potent porcupine inhibitor that blocks Wnt signaling. GNF-6231 exhibits potential antitumor properties via inhibition of aberrant Wnt signaling. Synonyms: [2,4'-Bipyridine]-5-acetamide, N-[5-(4-acetyl-1-piperazinyl)-2-pyridinyl]-2'-fluoro-3-methyl-; N-[5-(4-Acetyl-1-piperazinyl)-2-pyridinyl]-2'-fluoro-3-methyl[2,4'-bipyridine]-5-acetamide; GNF 6231; GNF6231; N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2'-fluoro-3-methyl-[2,4'-bipyridin]-5-yl)acetamide. Grades: >98%. CAS No. 1243245-18-2. Molecular formula: C24H25FN6O2. Mole weight: 448.49.
Golotimod
Golotimod is an orally bioactive synthetic peptide containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Golotimod has been shown to inhibit the expression of STAT-3, reversing immunosuppression and stimulating an anti-tumor immune response. It may stimulate the production of T-lymphocytes (in particular the helper T [Th1] cells), activate macrophages, and increase levels of interleukin 2 and interferon gamma. Synonyms: SCV-07; Gamma-D-Glu-L-trp; SCV07; SCV 07; Gamma-D-Glutamyl-L-tryptophan; (2R)-2-amino-5-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoic acid. Grades: >98%. CAS No. 229305-39-9. Molecular formula: C16H19N3O5. Mole weight: 333.34.
Gonadorelin a synthetic decapeptide prepared for gonadotropin-releasing hormone (GnRH), affects follicle stimulating hormones. Uses: Use in reproduction medicine diagnosis of the hypothalamic-pituitary-gonadal axis function cryptorchism. Synonyms: Luteinizing hormone-releasing factor (swine), acetate (1:x); Luteinizing hormone-releasing factor (pig), acetate (salt); Luteinizing hormone-releasing factor (swine), acetate (salt); 16: PN: WO2006018418 SEQID: 12 claimed protein; Cystorelin; Fertiline; Luprolite acetate; Lutrelef; Lutrepulse; Synthetic luteinizing hormone-releasing factor acetate. Grades: >98%. CAS No. 34973-08-5. Molecular formula: C55H75N17O13.xC2H4O2. Mole weight: 1182.29 (free base).
Goserelin Acetate
Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. Goserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Uses: Antineoplastic agents, hormonal. Synonyms: (D-Ser(tBu)6,Azagly10)-LHRH Acetate; Zoladex; 6-[O-(1,1-Dimethylethyl)-D-serine]-1-9-luteinizing Hormone-releasing Factor (swine) 2-(Aminocarbonyl)hydrazide Acetate; Fertilan; Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH2.CH3CO2H; L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N'-carbamoyl-L-prolinehydrazide acetic acid. Grades: 98%. CAS No. 145781-92-6. Molecular formula: C61H88N18O16. Mole weight: 1329.49.
Gossypol Acetic Acid
Gossypol Acetic Acid is a phenol compound from plants of the Gossypium genus, Malvaceae. It binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively. It exhibits antiviral activity at low concentration. Uses: Spermatocidal agents. Synonyms: Gossypol acetate; Acetate gossypol. Grades: 98 % by HPLC. CAS No. 12542-36-8. Molecular formula: C32H34O10. Mole weight: 578.61.
GPBAR-A
GPBAR-A is a GPBA receptor agonist. GPBAR-A increases GLP-1 secretion from intestinal cultures. Synonyms: GPBAR-A; GPBAR A; GPBARA; 4-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-6-(2-fluorophenyl)-4,5-dihydro-pyrido[3,2-f]-1,4-oxazepin-3(2H)-one. Grades: ≥98% by HPLC. CAS No. 877052-79-4. Molecular formula: C23H15F7N2O2. Mole weight: 484.37.
GPi 688
GPi 688 is an allosteric glycogen phosphorylase inhibitor that inhibits glucagon-mediated hyperglycemia in the rat. Synonyms: GPi 688; GPi688; GPi-688; 2-Chloro-N-[1-[(2R)-2,3-dihydroxypropyl]-1,2,3,4-tetrahydro-2-oxo-3-quinolinyl]-6H-thieno[2,3-b]pyrrole-5-carboxamide. Grades: ≥99% by HPLC. CAS No. 918902-32-6. Molecular formula: C19H18ClN3O4S. Mole weight: 419.88.
GR 144053 trihydrochloride
GR 144053 trihydrochloride is a potent and selective orally bioactive platelet fibrinogen receptor glycoprotein IIb/IIIa (GpIIb/IIIa) antagonist (IC50 = 37 nM). GR 144053 potently inhibits thrombus formation in vivo. Synonyms: GR 144053; GR-144053; GR144053; GR 144053 trihydrochloride. 4-[4-[4-(Aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid trihydrochloride. Grades: ≥99% by HPLC. CAS No. 1215333-48-4. Molecular formula: C18H27N5O2.3HCl. Mole weight: 454.83.
GR 203040
GR 203040 is a selective NK1 receptor antagonist with high affinity. GR 203040 potently inhibits substance P binding to NK1 receptors (pKi = 10.1 to 10.5). Synonyms: (2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine dihydrochloride. Grades: ≥98% by HPLC. CAS No. 168398-02-5. Molecular formula: C20H24N6O·2HCl. Mole weight: 437.37.
GR 64349
GR 64349 is a potent and selective agonist of tachykinin NK2 receptor (EC50 = 3.7 nM in rat colon). Synonyms: GR 64349; GR64349; GR-64349; LYS-ASP-SER-PHE-VAL-GLY-R-GAMMA-LACTAM-LEU-MET-NH2; [LYS3, GLY8-R-GAMMA-LACTAM-LEU9]NEUROKININ A (3-10); L-Lys-L-Asp-L-Ser-L-Phe-L-Val-N-[(3R)-1-[(R)-1-[[[(S)-1-(Aminocarbonyl)-3-(methylthio)propyl]amino]carbonyl]-3-methylbutyl]-2-oxo-3α-pyrrolidi. Grades: >98%. CAS No. 137593-52-3. Molecular formula: C42H68N10O11S. Mole weight: 921.12.
Gramicidin S
Gramicidin S is an antibiotic produced by the strain of Bacillus brevis. It is effective against some gram-positive and gram-negative bacteria as well as some fungi. Uses: For research use only. Synonyms: Gramicin S-A; Gramicin S 1; Cyclo(L-valyl-L-ornithyl-L-leucyl-D-phenylalanyl-L-prolyl-L-valyl-L-ornithyl-L-leucyl-D-phenylalanyl-L-prolyl); Gramacidine S; Gramicidina S; Gramicidinum S. Grades: >95%. CAS No. 113-73-5. Molecular formula: C60H92N12O10. Mole weight: 1141.46.
Graveoline
Graveoline isolated from ethanolic extract of Ruta graveolens triggers apoptosis and autophagy in skin melanoma cells: a novel apoptosis-independent autophagic signaling pathway. Synonyms: 2-(benzo[d][1,3]dioxol-5-yl)-1-methylquinolin-4(1H)-one; Foliosine; Graveolin. Grades: 96 % (HPLC). CAS No. 485-61-0. Molecular formula: C17H13NO3. Mole weight: 279.29.
GRGDS
GRGDS is a synthetic integrin antagonist. Synonyms: GRGDS; GRGDS 1/2ACOH 2H2O; GRGDS, FIBRONECTIN ATTACHMENT PEPTIDE; GLY-ARG-GLY-ASP-SER; GLY-ARG-GLY-ASP-SER 1/2ACOH 2H2O; H-GLY-ARG-GLY-ASP-SER-OH; glycyl-arginyl-glycyl-aspartyl-serine; GLY-ARG-GLY-ASP-SER ACETATE. Grades: ≥97% by HPLC. CAS No. 96426-21-0. Molecular formula: C17H30N8O9. Mole weight: 490.5.
GRGDSP
GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor which can be used to modify the surface of cardiovascular implants such as vascular grafts to promote endothelialization. Synonyms: H-Gly-Arg-Gly-Asp-D-Ser-Pro-OH; glycyl-L-arginyl-glycyl-L-alpha-aspartyl-D-seryl-L-proline. Grades: ≥95%. CAS No. 91037-75-1. Molecular formula: C22H37N9O10. Mole weight: 587.58.
GRI 977143
GRI 977143 is a selective and non-lipid agonist of lysophosphatidic acid 2 (LPA2) receptor (EC50 = 3.3 μM) exhibiting no activity for other LPA GPCRs at concentrations up to 10 μM. GRI 977143 inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. It also activates ERK1/2 survival pathway. Synonyms: GRI977143; GRI-977143; GRI 977143; 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]benzoic acid. Grades: ≥98% by HPLC. CAS No. 325850-81-5. Molecular formula: C22H17NO4S. Mole weight: 391.44.
Groenlandicine
Groenlandicine, a botanical-derived constituent, exhibits profound implications for biomedical applications of studying an array of afflictions, encompassing neoplastic disorders and cardiovascular impairments. Synonyms: 11,12-Dihydro-8-methoxy-9-hydroxybenzo[a]-1,3-benzodioxolo[4,5-g]quinolizinium; 11,12-Dihydro-9-hydroxy-8-methoxybenzo[a]-1,3-benzodioxolo[4,5-g]quinolizinium; Groenlandicine; Tetrahydricheilanthifolinium; Tetrahydrocheilanthifoline; Tetradehydrocheilanthifoline. Grades: >98%. CAS No. 38691-95-1. Molecular formula: C19H16NO4+. Mole weight: 322.33464.
GS 143
GS 143 is a β-TrCP1 ligase inhibitor. GS 143 exhibits inhibitory effects on IκBα ubiquitination (IC50 = 5.2 μM), LPS-induced expression of inflammatory cytokines in human myelomonocytic cells, antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice. Synonyms: GS-143; GS 143; GS143; 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid. Grades: ≥98% by HPLC. CAS No. 916232-21-8. Molecular formula: C28H19FN2O4. Mole weight: 466.46.
GS 389
GS 389 is a novel tetrahydroisoquinoline analog which significantly increased cGMP levels in the rat aorta and inhibited cGMP phosphodiesterase from the rabbit brain. Uses: A novel tetrahydroisoquinoline analog. Synonyms: GS 389; GS-389; GS389. 6,7-dimethoxy-1-[(4-methoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline. Grades: ≥98%. CAS No. 41498-37-7. Molecular formula: C19H23NO3. Mole weight: 313.39.
GSK-1071306
GSK-1071306 is one of the metabolites of pazopanib which is a inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity as a approved drug. Synonyms: GSK-1071306; GSK1071306; GSK 1071306; Pazopanib metabolite M27;5-((4-((2,3-dimethyl-2H-indazol-6-yl)amino)-2-pyrimidinyl)amino)-2-methyl-Benzenesulfonamide. Grades: 98%. CAS No. 1252927-47-1. Molecular formula: C20H21N7O2S. Mole weight: 423.49.
GSK-114
GSK-114 is a selective TNNI3 Interacting Kinase (TNNI3K) inhibitor with IC50 of 25nM. GSK-114 shows significant bias for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellular and in vivo studies. Ralated studies has shown that TNNI3 Interacting Kinase has been linked to the progression of dilated cardiomyopathy, cardiac hypertrophy, and ischemia/reperfusion injury using models that employ TNNI3K overexpressing or TNNI3K knockout animals. Synonyms: GSK-114; GSK 114; GSK114; 3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide; 1301760-19-9 (2HCl). Grades: 98%. CAS No. 1301761-96-5. Molecular formula: C19H23N5O4S. Mole weight: 417.48.
GSK-114 2Hcl
GSK-114 is a potent and selective TNNI3K inhibitor (TNNI3 IC50 = 25nM; B-RafV600E IC50 = 1000 nM). GSK-114 displays significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to enable its use in cellular and in vivo studies. Synonyms: GSK-114 2Hcl; GSK114 2Hcl; GSK 114 2Hcl. CAS No. 1301760-19-9. Molecular formula: C19H23N5O4S.2HCl. Mole weight: 495.484.
GSK121 trifluoroacetate salt
GSK121 is an inhibitor for protein arginine deiminase 4 (PAD4), which has been shown to inhibit the citrullination of PAD4 target proteins in a functional assay with an IC50 value of 3.2 μM. Synonyms: (3-amino-1-piperidinyl)[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzimidazol-5-yl]-methanone, 2,2,2-trifluoroacetate. Grades: ≥98%. CAS No. 1652591-80-4. Molecular formula: C23H25N5O·CF3COOH. Mole weight: 501.5.
GSK-1268992
GSK-1268992 is one of a metabolite of Pazopanib which is a selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. Synonyms: GSK-1268992; GSK1268992; GSK 1268992; Pazopanib metabolite M24;5-((4-((3-(Hydroxymethyl)-2-methyl-indazol-6-yl)-methyl-amino)pyrimidin-2-yl)amino)-2-methyl-benzenesulfonamide. Grades: 98%. CAS No. 1414375-49-7. Molecular formula: C21H23N7O3S. Mole weight: 453.52.
GSK-1268997
GSK-1268997 is one of a metabolite of Pazopanib which is a selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. Synonyms: GSK-1268997; GSK1268997; GSK 1268997; Pazopanib metabolite M26; 5-((4-((2,3-Dimethylindazol-6-yl)-methyl-amino)pyrimidin-2-yl)amino)-2-(hydroxymethyl)benzenesulfonamide. Grades: 98%. CAS No. 1414375-50-0. Molecular formula: C21H23N7O3S. Mole weight: 453.52.
GSK-1440115
GSK-1440115 is an orally active urotensin II receptor antagonist. It is used for the treatment of asthma. Uses: Gsk-1440115 is used for the treatment of asthma. Synonyms: GSK 1440115; GSK-1440115; GSK1440115. 4'-(1-(((6,7-Dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl)(methyl)amino)-2-(4-morpholinyl)ethyl)-4-diphenylcarboxylic acid;4-[4-[(1R)-1-[[2-(6,7-dichloro-3-oxo-1,4-benzoxazin-4-yl)acetyl]-methylamino]-2-morpholin-4-ylethyl]phenyl]benzoic acid. Grades: >98 %. CAS No. 1003878-16-7. Molecular formula: C30H29Cl2N3O6. Mole weight: 598.47.
GSK172981
This molecular is a novel non-peptide tachykinin NK3 receptor antagonist and it has a very high affinity for native guinea pig (pK(I) value 7.8) tachykinin NK(3) receptors and recombinant human (pK(I) value 7.7). Meanwhile, GSK172981 also exhibited a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK(B)=8.1). In the near future, this active molecular may be promising drug candidate in the treatment of schizophrenia. Uses: Treatment of schizophrenia. Synonyms: GSK172981; GSK-172981; GSK 172981. (S)-3-amino-N-(cyclopropyl(phenyl)methyl)-2-(3-fluorophenyl)quinoline-4-carboxamide. Grades: 98%. CAS No. 1133705-99-3. Molecular formula: C26H22FN3O. Mole weight: 411.48.
GSK1842799
GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. It showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3 upon phosphorylation. It has good oral bioavailability. It was selected as a candidate for further clinical on the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations. Uses: Gsk1842799 was selected as a candidate for further clinical. Synonyms: (S)-2-amino-2-(5-(4-(octyloxy)-3-(trifluoromethyl)phenyl)-1,3,4-thiadiazol-2-yl)propan-1-ol;GSK1842799; GSK 1842799; GSK 1842799. Grades: >98 %. CAS No. 1005407-76-0. Molecular formula: C20H28F3N3O2S. Mole weight: 431.52.
GSK199 hydrochloride
GSK199 is a potent and reversible inhibitor of PAD4 with an IC50 value of 200 nM) which is less potent than the related PAD4 inhibitor GSK484 (IC50 = 50 nM). Synonyms: [(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride. Grades: ≥98%. CAS No. 1549811-53-1. Molecular formula: C24H28N6O2·HCl. Mole weight: 469.
GSK2194069
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. Synonyms: GSK 2194069; GSK-2194069. Grades: >98%. CAS No. 1332331-08-4. Molecular formula: C25H24N4O3. Mole weight: 428.48.
GSK-2262167 hydrate
GSK-2262167 is a potent S1P3-sparing and S1P1 agonist and has a potent activity is in a collagen-induced arthritis model as efficacious as fingolimod and shows excellent pharmacokinetic properties preclinically. Uses: Arthritis. Synonyms: GSK-2262167 sodium; GSK 2262167 sodium; GSK2262167 sodium; sodium 3-(6-(5-(3-cyano-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)-5-methyl-3,4-dihydroisoquinolin-2(1H)-yl)propanoate. Grades: ≥98%. CAS No. 1458576-13-0. Molecular formula: C25H28N4O5. Mole weight: 464.51.
GSK-2262167 sodium
This molecular is a potent S1P3-sparing and S1P1 agonist. Meanwhile GSK-2262167 has a potent activity is in a collagen-induced arthritis model as efficacious as fingolimod and shows excellent pharmacokinetic properties preclinically. Uses: Arthritis. Synonyms: GSK-2262167 sodium; GSK 2262167 sodium; GSK2262167 sodium; sodium 3-(6-(5-(3-cyano-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)-5-methyl-3,4-dihydroisoquinolin-2(1H)-yl)propanoate,1165924-28-6 (free acid); 458576-13-0 (hydrate). Grades: 98%. CAS No. 1165923-54-5. Molecular formula: C25H25N4NaO4. Mole weight: 468.49.
GSK2330672
GSK-2330672, an ASBT inhibitor, has been developed for the treatment of type 2 diabetes and is currently under Phase II trail against primary biliary cirrhosis and type 2 diabetes. IC50: 42 ± 3 nM. Uses: Gsk-2330672 is an asbt inhibitor that has been developed for the treatment of type 2 diabetes and is currently under phase ii trail against primary biliary cirrhosis and type 2 diabetes. Synonyms: CHEMBL2387408; UNII-386012Z45S; GSK2330672; GSK-2330672; SCHEMBL2586025; CZGVOBIGEBDYTP-VSGBNLITSA-N. Grades: 98%. CAS No. 1345982-69-5. Molecular formula: C28H38N2O7S. Mole weight: 546.68.
GSK2334470
GSK2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM), which does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes. Synonyms: GSK2334470; GSK2334470; GSK2334470. Grades: 0.98. CAS No. 1227911-45-6. Molecular formula: C25H34N8O. Mole weight: 462.602.
GSK256066
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. Synonyms: GSK256066; GSK 256066; GSK-256066. Grades: >98%. CAS No. 801312-28-7. Molecular formula: C27H26N4O5S. Mole weight: 518.58.
GSK256066 2,2,2-trifluoroacetic acid
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. Synonyms: GSK-256066; GSK 256066. Grades: >98%. CAS No. 1415560-64-3. Molecular formula: C29H27F3N4O7S. Mole weight: 632.61.
GSK256471
This active molecular is a selective and potent NK(3) antagonist. It has a high affinity for recombinant human (pK(I) value 8.9) and native guinea pig (pK(I) value 8.4) tachykinin NK(3) receptors. In the near future, GSK256471 may be potentially very useful in the treatment of schizophrenia. Uses: Treatment of schizophrenia. Synonyms: GSK256471; GSK-256471; GSK 256471. N-[ (S)-cyclopropyl (phenyl)methyl]-3-[[methyl (methylsulfonyl)amino]methyl]-2-phenylquinoline-4-carboxamide. Grades: 98%. CAS No. 1133706-08-7. Molecular formula: C29H29N3O3S. Mole weight: 499.63.
GSK 2606414
GSK 2606414 is a potent and selective PERK inhibitor that suppresses PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small-molecule inhibitors. Synonyms: GSK2606414; GSK-2606414; GSK 2606414; GSK PERK Inhibitor. 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone. Grades: 98%. CAS No. 1337531-36-8. Molecular formula: C24H20F3N5O. Mole weight: 451.453.
GSK 264220A
GSK 264220A is an endothelial lipase and lipoprotein lipase inhibitor (IC50 = 0.13 and 0.10 μM, respectively). Inhibition of endothelial lipase may lead to an increase in HDL levels and GSK 264220A is expected to be a therapy for cardiovascular disease. Uses: Potential treatment of cardiovascular disease. Synonyms: GSK-264220A; GSK 264220A; GSK264220A. N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N'-phenylurea; 3-[2-methyl-5-(piperidine-1-sulfonyl)furan-3-yl]-1-phenylurea; 1-(2-methyl-5-piperidin-1-ylsulfonylfuran-3-yl)-3-phenylurea. Grades: ≥98% by HPLC. CAS No. 685506-42-7. Molecular formula: C17H21N3O4S. Mole weight: 363.43.
GSK2837808A
GSK2837808A is a potent and specific lactate dehydrogenase A (LDHA) with IC50 values of 1.9 and 14 nM for LDHA and LDHB, respectively and inhibits lactate production in selected cancer cell lines. Synonyms: GSK2837808A; GSK-2837808A; GSK 2837808A; GSK2837808; GSK-2837808; GSK 2837808. 3-[[3-(cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl]amino]-5-(3,5-difluorophenoxy)benzoic acid. CAS No. 1445879-21-9. Molecular formula: C31H25F2N5O7S. Mole weight: 649.62.
GSK2879552 dihydrochloride
GSK2879552 dihydrochloride, a selective, irreversible and orally active lysine specific demethylase 1 (LSD1/KDM1A) inhibitor, has potential antineoplastic activity. Synonyms: Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-, hydrochloride (1:2); 4-{[4-({[(1R,2S)-2-Phenylcyclopropyl]amino}methyl)-1-piperidinyl]methyl}benzoic acid dihydrochloride. Grades: ≥95%. CAS No. 1902123-72-1. Molecular formula: C23H30Cl2N2O2. Mole weight: 437.40.
GSK299115A
GSK299115A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor. Synonyms: GSK299115A; GSK 299115A; GSK-299115A. 4-(3,4-dichlorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyridine-5-carboxamide. Grades: 98%. CAS No. 864082-35-9. Molecular formula: C20H16Cl2N4O2. Mole weight: 415.27.
GSK317354A
GSK317354A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) inhibitor,but no detailed information has been published yet. Synonyms: GSK317354A; GSK-317354A; GSK 317354A. 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-(6-(trifluoromethyl)pyridin-3-yl)-1,4-dihydropyrimidine-5-carboxamide. Grades: 98%. CAS No. 874119-13-8. Molecular formula: C25H18F4N6O. Mole weight: 494.45.
GSK-356278
GSK-356278 is a selective Type 4 cyclic nucleotide phosphodiesterase inhibitor. It shows anxiolytic and cognition-enhancing effects and it has the ability to elevate cAMP in various cell types of the central nervous system. No development was reported for phase-I development in Major depressive disorder and Huntington's-disease. Uses: Huntington's disease; major depressive disorder. Synonyms: GSK-356278; GSK356278; GSK 356278; 5-(5-((2,4-dimethyl-5-thiazolyl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-n-(tetrahydro-2H-pyran-4-yl)-1H-Pyrazolo(3,4-b)pyridin-4-amine. Grades: 98%. CAS No. 720704-34-7. Molecular formula: C21H25N7O2S. Mole weight: 439.54.
GSK376501A
GSK376501A is a bio-active chemical compound used for the treatment of type 2 diabetes and hypercholesterolemia. It was developed by GlaxoSmithKline and was once in clinic phase 1, but now it has been terminated. Uses: Gsk376501a is used for the treatment of type 2 diabetes and hypercholesterolemia. Synonyms: GSK-376501A;GSK376501;GSK-376501;1-[[3,5-bis(2-methoxyethoxy)phenyl]methyl]-3-(4-tert-butylphenyl)indole-2-carboxylic acid;1H-Indole-2-carboxylic acid, 1-((3,5-bis(2-methoxyethoxy)phenyl)methyl)-3-(4-(1,1-dimethylethyl)phenyl)-. Grades: >98 %. CAS No. 1010412-80-2. Molecular formula: C32H37NO6. Mole weight: 531.64.
GSK4027
GSK4027 is a potent and selective inhibitor of p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay). Synonyms: 4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone. Grades: ≥95%. CAS No. 2079896-25-4. Molecular formula: C17H21BrN4O. Mole weight: 377.3.
GSK4112
GSK 4112, a kind of synthetic agonist of REV-ERBα, could suppress the expression of sorts of genes involved in gluconeogenesis. IC50: 0.4 μM (EC50). Uses: Gsk 4112 is a kind of synthetic agonist of rev-erbα and could suppress the expression of sorts of genes involved in gluconeogenesis. Synonyms: GSK4112; GSK 4112; GSK-4112. SR6452;CHEMBL1961795;1216744-19-2;MLS006010708;GTPL2903. Grades: 95%. CAS No. 1216744-19-2. Molecular formula: C18H21ClN2O4S. Mole weight: 396.89.
GSK466317A
GSK466317A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor. Synonyms: GSK466317A; GSK-466317A; GSK 466317A. N-(7-chloro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide. Grades: 98%. CAS No. 864082-48-4. Molecular formula: C21H16ClF3N4O2. Mole weight: 448.83.
GSK481
GSK481 is a potent inhibitor of Receptor-interacting serine/threonine-protein kinase 1 (RIPK1 or RIP1; IC50 value 2.8 nM for inhibition of Ser166 autophosphorylation of hWT RIP1) with preference for RIP1 over 450 other kinases. Synonyms: GSK481; GSK-481; GSK 481. 5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1,2-oxazole-3-carboxamide. Grades: 98%. CAS No. 1622849-58-4. Molecular formula: C21H19N3O4. Mole weight: 377.39.
GSK-484
GSK-484 is a potent protein-arginine deiminase type-4 (PAD-4) inhibitor. Synonyms: GSK484; GSK 484. Grades: ≥98% by HPLC. CAS No. 1652629-23-6. Molecular formula: C27H31N5O3. Mole weight: 473.6.
GSK583
GSK583 is a selective receptor-interacting serine/threonine-protein kinase 2 (RIP2 Kinase) inhibitor and the RIP2K binding IC50 is 5 nM. GSK583 can inhibit both TNF-α and IL-6 production with an IC50 value of 200 nM in an ex vivo human translational model. Synonyms: GSK583; GSK 583; GSK-583. 6 - (tert-Butylsulfonyl) - N - (5-fluoro - 1H - indazol-3-yl)quinolin-4-amine. Grades: 98%. CAS No. 1346547-00-9. Molecular formula: C20H19FN4O2S. Mole weight: 398.46.
GSK'872
GSK'872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with high affinity (IC50=1.8 nM), and is approximately >1,000-fold selective over 300 kinases in a fluorescence polarization assay at a concentration of 1 μM. Besides, GSK'872 inhibits kinase activity (IC50=1.3 nM). Synonyms: GSK872; GSK-872; GSK 872; N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine. CAS No. 1346546-69-7. Molecular formula: C19H17N3O2S2. Mole weight: 383.49.
GSK894490A
GSK894490A is a non-peptide ghrelin receptor agonist. It crosses the blood/brain barrier and elicit pro-cognitive effects in recognition and spatial learning and memory tests. It may be used as a potential drug target for therapeutic approaches to treat diseases affecting cognition. Uses: Gsk894490a may be used as a potential drug target for therapeutic approaches to treat diseases affecting cognition. Synonyms: Benzenesulfonamide, N-(5-((3R,5S)-3,5-dimethyl-1-piperazinyl)-2-methoxyphenyl)-4-(5-methyl-2-furanyl)-, hydrochloride (1:1), rel-;N-[5-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-2-methoxyphenyl]-4-(5-methylfuran-2-yl)benzenesulfonamide hydrochloride;GSK-894490A. Grades: >98 %. CAS No. 1012035-06-1. Molecular formula: C24H30ClN3O4S. Mole weight: 492.03.
GSK963
GSK963 is a potent and selective inhibitor of RIP1 kinase (RIPK1; IC50=29 nM in FP binding assays). GSK963 displays >10?000-fold selective for RIP1 over 339 other kinases. Synonyms: 2,2-dimethyl-1-[(3S)-3-phenyl-3,4-dihydropyrazol-2-yl]propan-1-one. Grades: ≥98%. CAS No. 2049868-46-2. Molecular formula: C14H18N2O. Mole weight: 230.31.
GSK-F1
PI4KA inhibitor-F1 is a potent PI4KA inhibitor. Synonyms: PI4KA inhibitor-F1. Grades: 98%. CAS No. 1384097-27-1. Molecular formula: C27H18F5N5O4S. Mole weight: 603.5.
GsMTx4
GsMTx4 is a mechanosensitive and stretch-activated ion channel inhibitor. It is used as a tool for identifying the role of these excitatory MSCs in normal physiology and pathology. Grades: >98%. CAS No. 1209500-46-8. Molecular formula: C185H273N49O45S6. Mole weight: 4095.86.
Guaiacin
Guaiacin is a lignan isolated from the leaves of Guaiacum officinale. Guaiacin inhibits COX-1 and COX-2 leading to the reduction of inflammations. Synonyms: (6R,7S,8S)-8-(4-hydroxy-3-methoxyphenyl)-3-methoxy-6,7-dimethyl-5,6,7,8-tetrahydronaphthalen-2-ol. Grades: >98%. CAS No. 36531-08-5. Molecular formula: C20H24O4. Mole weight: 328.408.
Guanethidine sulfate
Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. It is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine.It may also inhibit the release of granules by decreasing norepinephrine. Uses: Sympatholytics. Synonyms: Guanethidine monosulfate. Grades: >98%. CAS No. 645-43-2. Molecular formula: C10H24N4O4S. Mole weight: 296.39.
Guanosine 5'-diphosphate disodium salt
Guanosine 5'-diphosphate disodium salt is an imperative biomolecule esteemed in the biomedical sector, exhibiting noteworthy involvement in cellular signaling and serves as a substrate for diverse nucleic acid metabolism-encompassing enzymes. Its significance is exemplified through extensive employment in research and manufacturing, enabling comprehensive exploration of G-protein coupled receptors, protein synthesis and drug discovery-related signaling pathways, as well as disease research. Synonyms: GDP-Na2; Disodium 5'-O-{[ (hydroxyphosphinato) oxy]phosphinato}guanosine; GDP.Na2; 5'-GDP-Na2; Guanosine 5'-(trihydrogen diphosphate), disodium salt; Guanosinepyrophosphate, disodium salt; Disodium guanosine 5'-diphosphate; Guanosine-5'-diphosphoric acid disodium salt. Grades: 98%. CAS No. 7415-69-2. Molecular formula: C10H13N5Na2O11P2. Mole weight: 487.16.
Guanosine 5-monophosphomorpholidate
Guanosine 5-monophosphomorpholidate - an invaluable biomedical product - finds its application in the treatment of various diseases. As a precursor for synthesizing targeted drugs against viral infections and cancerous cells, it showcases its remarkable potential. Notably, this compound plays a pivotal role in signaling pathways, guiding and governing vital cellular processes concerning DNA synthesis and repair. Its multifaceted involvement in these intricate mechanisms underscores its significance in the realm of biomedical sciences. Synonyms: N,N'-Dicyclohexylmorpholine-4-carboximidamide ((2R,3S,4R,5R)-5-(2-amino-6-oxo-1H-purin-9(6H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl morpholinophosphonate;guanosine 5'-monophospho morpholidate 4-morpholine-N,N'-dicyclohexylcarboxamidine salt; Guanosine 5'-monophosphomorpholidate 4-morpholine-N,N'-dicyclohexylcarboxamidine salt, ~95%; Guanosine 5'-monophosphomorpholidate-4-morpholine-N,N'-dicyclohexylcarboxamidine salt; (Z)-N,N'-dicyclohexylmorpholine-4-carboximidamide; {[(2R,3S,4R,5R)-5-(2-amino-6-oxo-6,9-dihydro-1H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(morpholin-4-yl)phosphinic acid; N,N'-Dicyclohexylmorpholine-4-carboximidamide--5'-O-[hydroxy(morpholin-4-yl)phosphoryl]guanosine (1/1). Grades: 95%. CAS No. 7361-7-1. Molecular formula: C31H52N9O9P. Mole weight: 725.8.
Guanosine-5'-triphosphate sodium salt
Guanosine-5'-triphosphate sodium salt could be used as a phosphoryl donor in signal transduction and protein synthesis. Synonyms: Guanosine 5'-(tetrahydrogen Triphosphate), Trisodium Salt; 5'-GTP Trisodium Salt; Trisodium 5'-GTP; GTP Trisodium Salt. Grades: ≥97% by HPLC. CAS No. 36051-31-7. Molecular formula: C10H13N5Na3O14P3. Mole weight: 589.13.
Guanoxyfen sulfate
Guanoxyfen sulfate is an inhibitor of vasoconstrictor responses to sympathetic nerve stimulation. It could potentiate the actions of adrenaline and noradrenaline. It also could increase the blood glucose concentration and decrease the appetite. Uses: Guanoxyfen could potentiate the actions of adrenaline and noradrenaline. it also could increase the blood glucose concentration and decrease the appetite. Synonyms: PD-34799 hemisulfate;PPG hemisulfate;(3-Phenoxypropyl)guanidine sulfate;(3-Phenoxypropyl)guanidine hemisulfate. Grades: >98 %. CAS No. 1021-11-0. Molecular formula: C20H32N6O6S. Mole weight: 484.57.
Gue 1654
Gue 1654 is an oxoeicosanoid receptor 1 (OXE-R) modulator selectively inhibiting Gβγ but not Gαi signaling upon activation of the Gαi-βγ heterotrimer by OXE-R. Gue 1654 was shown to inhibit Gβγ-mediated opening of GIRK1/2 channels in HEK293 cells. Synonyms: Gue1654; Gue 1654; Gue-1654. N-[7-(Methylthio)benzo[1,2-d:4,3-d']bisthiazol-2-yl]-α-phenylbenzeneacetamide. Grades: ≥97% by HPLC. CAS No. 397290-30-1. Molecular formula: C23H17N3OS3. Mole weight: 447.6.
Gunagratinib
Gunagratinib is a tyrosine kinase inhibitor, with antineoplastic activity. Synonyms: 3-[(3,5-dimethoxyphenyl)ethynyl]-5-(methylamino)-1-[(3S)-1-(prop-2-enoyl)pyrrolidin-3-yl]-1H-pyrazole-4-carboxamide; (S)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl)ethynyl)-5-(methylamino)-1H-pyrazole-4-carboxamide. CAS No. 2211082-53-8. Molecular formula: C22H25N5O4. Mole weight: 423.47.
guselkumab
guselkumab is a selectively blocking agent for interleukin-23 (IL-23), a cytokine involved in plaque psoriasis. guselkumab was approved by FDA as an anti-inflammatory drug for the treatment of moderate to severe plaque psoriasis. Uses: Anti-inflammatory drug. Synonyms: Tremfya. CAS No. 1350289-85-8. Molecular formula: C6402H9864N1676O1994S42. Mole weight: 143.6.