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| Product | Description | |
|---|---|---|
| BMS 299897, gamma-Secretase Inhibitor XXIV (4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic Acid, BMS-299897, BMS 299897) | An orally bioavailable sulfonamide compound that acts as a potent, reversible and allosteric y-secretase activity inhibitor with ~15-fold greater selectivity over Notch-1 proteolysis processing (IC50=7.1 and 105.9nM in HEK293-wtAPP) and preferentially inhibits PS1 (presenillin 1)-comprised y-secretase (EC50=8, 108, 286 and 29nM for PS1, Triple PS1-L172M,T281P, L282I, PS2 and Triple PS2-M178L, P287T, I288L), respectively). Shown to reduce the levels of Ab38, Ab40 and Ab42 in Tg2576 mice, Ab40 brain and plasma in APP-YAC mice (ED50=30 and 16mg/kg, p.o.) and Abtotal brain, CSF and plasma in guinea pigs (ED50=30mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. CAS No. 290315-45-6. Pack Sizes: 5mg. US Biological Life Sciences. |  Worldwide |
| gamma-Secretase Inhibitor XXV, FT-9 (2-[3- (3, 5-dichlorophenoxy) phenyl]propanoic Acid) | FT-9, a cell-permeable NSAID-like compound, is a partially selective gamma-Secretase Inhibitor in both microsomes and whole cells. Displays dose-dependent inhibition of the gamma-secretase cleavage of beta-Amyloid Precursor Protein (APP) and APLP2 with IC50 values against APP ICD (intracellular domain) and APLP2 ICD of 260uM, but there is a less potent effect on gamma-secretase processing of APLP1. The concentration of FT-9 required to cause a 2-fold increase in APP CTFs, 3.4 +/- 0.4uM, is significantly lower than that for APLP1 (25.7 +/- 8.9uM) (P = 0.001). For comparison, the concentration of another gamma-Secretase inhibitor compound E needed for a 2-fold increase in the magnitude of the CTF band signal is not significantly different, being 0.27nM for APP versus 0.24nM for APLP1. This is the first example that a GSI can preferentially target APP processing while sparing other gamma-substrates. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??Cl?O?. US Biological Life Sciences. | Worldwide |
| gamma-secretase modulator 1 | gamma-secretase modulator 1 is a gamma-secretase modulator, useful for Alzheimer's disease. Synonyms: gamma-secretase modulator 1; 1172637-87-4; 4,5,6,7-Tetrahydro-N-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-4-phenyl-2-benzothiazolamine; N-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]-4-phenyl-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine; VFSGAZRYSCNFDF-UHFFFAOYSA-N; SCHEMBL1616912; CHEMBL1915569; DTXSID90655321; XWB63787; AKOS030526283; CS-0329; NCGC00378743-01; HY-10043; MS-27256; F83676; A908573; [3-Methoxy-4-(4-methyl-imidazol-1-yl)-phenyl]-(4-phenyl-4,5,6,7-tetrahydro-benzothiazol-2-yl)-amine; N-[3-Methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-4-phenyl-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine. Grades: >98%. CAS No. 1172637-87-4. Molecular formula: C24H24N4OS. Mole weight: 416.54. |  |
| gamma-secretase modulator 2 | gamma-secretase modulator 2, a triazole derivative, a potent and selective γ-secretase modulator so as to selectively attenuate production of Aβ(1-42) and hence has the potential for treatment of Alzheimer's disease. Synonyms: 6-fluoro-3-[4-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]-1-(2,2,2-trifluoroethyl)-4,5-dihydro-3H-1-benzazepin-2-one; gamma-secretase modulator 2; 1093978-89-2; SCHEMBL3040102; DTXSID70732149; C25H22F4N6O2; 3374AH; ABP000472; BCP9000905; CS-0310; HE070827; HE211077; HY-50754; DB-014988; W-5511; 2H-1-BENZAZEPIN-2-ONE,6-FLUORO-1,3,4,5-TETRAHYDRO-3-[4-[3-METHOXY-4-(4-METHYL-1H-IMIDAZOL-1-YL)PHENYL]-1H-1,2,3-TRIAZOL-1-YL]-1-(2,2,2-TRIFLUOROETHYL)-; 6-fluoro-1,3,4,5-tetrahydro-3-[4-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-1H-1,2,3-triazol-1-yl]-1-(2,2,2-trifluoroethyl)-2H-1-Benzazepin-2-on; 6-Fluoro-1,3,4,5-tetrahydro-3-[4-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-1H-1,2,3-triazol-1-yl]-1-(2,2,2-trifluoroethyl)-2H-1-benzazepin-2-one; 6-fluoro-3-{4-[3-methoxy-4-(4-methyl-1h-imidazol-1-yl)phenyl]-1h-1,2,3-triazol-1-yl}-1-(2,2,2-trifluoroethyl)-1,3,4,5-tetrahydro-2h-1-benzazepin-2-one; 6-FLUORO-3-{4-[3-METHOXY-4-(4-METHYLIMIDAZOL-1-YL)PHENYL]-1,2,3-TRIAZOL-1-YL}-1-(2,2,2-TRIFLUOROETHYL)-4,5-DIHYDRO-3H-1-BENZAZEPIN-2-ONE. CAS No. 1093978-89-2. Molecular formula: C25H22F4N6O2. Mole weight: 514.47. | |
| gamma-secretase modulator 3 | gamma-secretase modulator 3 is a γ-secretase inhibitor. Synonyms: 4-(4-fluorophenyl)-N-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine; gamma-secretase modulator 3; CS-1149; HY-50889; W-6019; CS 1149; HY 50889; W 6019; CS1149; HY50889; W6019; 1431697-84-5. CAS No. 1431697-84-5. Molecular formula: C24H23FN4OS. Mole weight: 434.53. | |
| gamma-Secretase modulators | gamma-Secretase Modulators is a potent modulator of γ-secretase derived from oxadiazine. (IC50: Aβ42 = 11 nM, Aβ total/ Aβ42 = 1170). Synonyms: (4R,7E,9aS)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one; gamma-Secretase Modulators; 937812-80-1; (E)-(4R,9aS)-7-[3-Methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]-4-(3,4,5-trifluorophenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one; QCR-41; SCHEMBL2589995; DTXSID90647302; C26H24F3N3O3; hexahydro-7-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-4-(3,4,5-trifluorophenyl)-(4R,7E,9aS)-Pyrido[2,1-c][1,4]oxazin-6(1H)-one; 3690AH; ZINC95644683. CAS No. 937812-80-1. Molecular formula: C26H24F3N3O3. Mole weight: 483.48. | |
| gamma-Secretase Modulators | gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Amyloid-β production inhibitor; γ-Secretase Modulators. CAS No. 937812-80-1. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-50900. |  |
| 27-Deoxyactein | 27-Deoxyactein has shown stimulation of osteoblast function and inhibits bone resorbing mediators in the treatment of osteoporosis. It is a derivative of Actein (A191800), a gamma secretase modulators derived from botanicals. Group: Biochemicals. Grades: Highly Purified. CAS No. 264624-38-6. Pack Sizes: 1mg, 5mg. Molecular Formula: C37H56O10. US Biological Life Sciences. | Worldwide |
| 3-Amino-1-propanesulfonic acid | Tramiprosate, also nemed homotaurine, is an orally-administered, sulfated glycosaminoglycan mimic that targets amyloid &beta. γ-secretase: IC50 = 12 nM; Aβ40: IC50 = 7.4 nM; Aβ42: IC50 = 7.9 nM; gamma-secretase express: EC5050 = 7 nM (CHO cells); displacement of [3H]L685458 from human SPP express: IC50 = 28.7 μM (HEK293 cells). Uses: Anti-alzheimer agents; amyloid-β inhibitor. Synonyms: 3-aminopropane-1-sulfonic acid. Grades: 98%. CAS No. 3687-18-1. Molecular formula: C3H9NO3S. Mole weight: 139.17. | |
| Aftin-4 (N6-Methyl-(R)-roscovitine, Amyloid-beta Forty-Two Inducer 4) | Roscovitine-related purine with no activity on CDKs (used as control for roscovitine). Selectively and potently increases production of extracellular Abeta42 and decreases production of extracellular Abeta38 in cultured cells. Extracellular Abeta40 levels remain stable. Intracellular levels of these amyloids appear to remain stable. Alzheimer's Disease (AD) accelerator that interacts with VDAC1, prohibitin and mitofilin, possibly interfering with subcellular compartmentalization and lipid rafts properties, shifting gamma-secretase activity toward Abeta42 generation. Induces a reversible mitochondrial phenotype reminiscent of the one observed in AD brains. Tool to detect inhibitors of Aftin-induced actions (potential anti-AD compounds). Binds pyridoxal kinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 866893-90-5. Pack Sizes: 1mg, 5mg, 25mg. US Biological Life Sciences. | Worldwide |
| Aftin-5 ((2R)-2-[[9-Isopropyl-6-(N-methylanilino)purin-2-yl]amino]butan-1-ol, Amyloidbeta Forty-Two Inducer 5) | Roscovitine-related purine with no activity on CDKs (used as control for roscovitine). Selectively and potently increases production of extracellular Ab42 and decreases production of extracellular Ab38 in cultured cells. Extracellular Ab40 levels remain stable. Intracellular levels of these amyloids appear to remain stable. Alzheimer's Disease (AD) accelerator that interacts with VDAC1, prohibitin and mitofilin, possibly interfering with subcellular compartmentalization and lipid rafts properties, shifting gamma-secretase activity toward Ab42 generation. Induces a reversible mitochondrial phenotype reminiscent of the one observed in AD brains. Tool to detect inhibitors of Aftin-induced actions (potential anti-AD compounds). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 5mg, 25mg. US Biological Life Sciences. | Worldwide |
| Amyloid β-Protein (17-40) | Cleavage of APP by alpha- and gamma-secretase (i.e. the non-amyloidogenic pathway) yields p3 peptide, a mix of Aβ 17-40 and Aβ 17-42. P3 is a major component of diffuse plaques observed in AD brains and preamyloid plaques in patients with Down syndrome. Synonyms: β-Amyloid (17-40); H-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val-OH; L-leucyl-L-valyl-L-phenylalanyl-L-phenylalanyl-L-alanyl-L-alpha-glutamyl-L-alpha-aspartyl-L-valyl-glycyl-L-seryl-L-asparagyl-L-lysyl-glycyl-L-alanyl-L-isoleucyl-L-isoleucyl-glycyl-L-leucyl-L-methionyl-L-valyl-glycyl-glycyl-L-valyl-L-valine; Amyloid β-Protein Fragment 17-40. Grades: ≥90%. CAS No. 156790-69-1. Molecular formula: C110H178N26O31S. Mole weight: 2392.85. | |
| Avagacestat | BMS-708163 is a potent and orally bioavailable inhibitor of γ-secretase that more potently inhibits the cleavage of APP (IC50 = 0.30 nM) to Aβ40 than signaling through Notch (IC50s = 58 nM). Uses: Gamma secretase inhibitors and modulators. Synonyms: Avagacestat; BMS 708163; (2R)-2-[(4-chlorophenyl)sulfonyl-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide. Grades: >98%. CAS No. 1146699-66-2. Molecular formula: C20H17ClF4N4O4S. Mole weight: 520.89. | |
| Begacestat | Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC 50 Aβ 40 =15 nM) for the treatment of Alzheimer's disease [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSI-953. CAS No. 769169-27-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-14175. | |
| BMS 299897 | BMS 299897, under the IUPAC name 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid, synthesized by the radiosynthesis group at Bristol-Myers Squibb, is a β-secretase inhibitor that has the potential for treatment of Alzheimer's diseases (IC50 = 12 nM; gamma-secretase express: EC50 = 7 nM (CHO cells)). BMS 299897 blocks the formation of Aβ40 (IC50 = 7.9 nM) and Aβ42 (IC50 = 7.9 nM) in the brain, and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Synonyms: 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid; 4-(2-((1R)-1-(((4-chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid; BMS299897; BMS 299897; BMS-299897; 290315-45-6; 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoro-benzenebutanoic acid; C24H21ClF3NO4S; CHEMBL247471; SCHEMBL6394108; DTXSID50460039; 3496AH; ZINC28883606; AKOS024457319; CCG-222540; CS-1339; NCGC00346875-01; HY-50883; KB-75603; DB-017854; W-5550; BRD-K02950022-001-01-1; 2-[(1R)-1-[[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoroBenzenebutanoic acid; BMS 299897|2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid. CAS No. 290315-45-6. Molecular formula: C24H21ClF3NO4S. Mole weight: 511.94. | |
| BMS-433796 | BMS-433796 is a γ-secretase inhibitor. Chronic dosing of BMS-433796 in Tg2576 mice suggested a narrow therapeutic window and Notch-mediated toxicity at higher doses. Uses: Gamma secretase inhibitors and modulators. Synonyms: BMS433796; BMS-433796; BMS 433796. (2S)-2-[[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-N-[(5S)-3-methyl-4-oxo-5H-2,3-benzodiazepin-5-yl]propanamide; BMS-433796; UNII-R1E8M783K2; 935525-13-6; CHEMBL247361; R1E8M783K2; ZINC28899741; (alphaS)-N-[(1S)-2-[[(5S)-4,5-Dihydro-3-methyl-4-oxo-3H-2,3-benzodiazepin-5-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide; (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide; Benzeneacetamide, N-((1S)-2-(((5S)-4,5-dihydro-3-methyl-4-oxo-3H-2,3-benzodiazepin-5-yl)amino)-1-methyl-2-oxoethyl)-3,5-difluoro-alpha-hydroxy-, (alphaS)-. CAS No. 935525-13-6. Molecular formula: C21H20F2N4O4. Mole weight: 430.15. | |
| Compound 34 | Cell permeable, highly potent inhibitor of gamma-secretase (IC50 = 0.06nM). Group: Biochemicals. Alternative Names: (2S,3R)-3-(3,4-Difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy-N-((3S)-2-oxo-5-phenyl-2,3-1H-benzodiazepin-3-yl)butyramide. Grades: Highly Purified. CAS No. 564462-36-8. Pack Sizes: 200ug, 1mg. Molecular Formula: C31H24F3N3O3. US Biological Life Sciences. | Worldwide |
| Compound E | Cell permeable, potent, selective, non-transition state and non-competitive gamma-secretase inhibitor. Notch processing inhibitor. Only weakly affects presenilinase activity. Group: Biochemicals. Alternative Names: (2S)-2-(amino)-N-propanamide. Grades: Highly Purified. CAS No. 209986-17-4. Pack Sizes: 250ug, 1mg, 5mg. Molecular Formula: C27H24F2N4O3. US Biological Life Sciences. | Worldwide |
| Compound E | Compound E is a cell-permeable inhibitor of γ-secretase (GSI), which is a multifunctional transmembrane protein complex enzymatically catalyzing the cleavage of single-pass transmembrane proteins. Compound E can inhibit Notch processing (IC50 = 2.2 nM in SupT1 cells) and β-ammyloid production in cell culture (IC50 = 0.3 nM). Synonyms: γ-Secretase Inhibitor; Gamma-Secretase Inhibitor XXI; (S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide; (2S)-2-{[(3,5-Difluorophenyl)acetyl]amino}-N-[(3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]propanamide; N2-[(3,5-difluorophenyl)acetyl]-N-[(3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-L-alaninamide. Grades: 99%. CAS No. 209986-17-4. Molecular formula: C27H24F2N4O3. Mole weight: 490.5. | |
| Compound W | Compound W, also called 3,5-bis(4-Nitrophenoxy)benzoic acid, a 3,3'-diiodothyronine sulfate cross-reactive substance, is an inhibitor of γ-secretase which causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25). Synonyms: 3,5-bis(4-Nitrophenoxy)benzoic acid; 173550-33-9; gamma-Secretase Modulator, CW; ACMC-1CUIP; SCHEMBL264541; CHEMBL1553155; CTK8B1007; JOSXKPZXMVHRKU-UHFFFAOYSA-; DTXSID10587892; JOSXKPZXMVHRKU-UHFFFAOYSA-N; HMS3269J17; ZINC2576957; ANW-22664; MFCD02093450; AKOS015833412; 3,5-bis (4-nitrophenoxy) benzoic acid; NCGC00167814-01; AJ-42568; AK-63150; EN002659; OR182673; KB-234083; TR-007681; B2120; Compound W|CW|3,5-Bis(4-nitrophenoxy)benzoic acid; BRD-K98143539-001-01-4; I14-62910. Grades: >98.0%(T)(HPLC). CAS No. 173550-33-9. Molecular formula: C19H12N2O8. Mole weight: 396.31. | |
| DAPT | Cell permeable gamma-secretase inhibitor (IC50 = 115nM for total beta-amyloid, IC50 = 200nM for beta-amyloid 1-42). Reduces Abeta levels in vivo. Blocks the proteolytic processing of neurotrophin receptor alike death domain protein (NRADD). Does not inhibit persenilinase. Notch processing inhibitor. Enhances neuronal differentiation independent of sonic hedgehog (Shh) signaling. CDK5 activity inhibitor. Apoptosis enhancer. Group: Biochemicals. Alternative Names: (S)-Tert-butyl 2- ( (S) -2- (2- (3, 5-difluorophenyl) acetamido) propanamido) -2-phenylacetate; N-S-phenylglycine tert.butyl ester; GSI-IX; Secretase, gamma Inhibitor IX. Grades: Highly Purified. CAS No. 208255-80-5. Pack Sizes: 5mg, 25mg. Molecular Formula: C??H??F?N?O?. US Biological Life Sciences. | Worldwide |
| DAPT | DAPT, also called γ-Secretase Inhibitor IX, is a potent and selective inhibitor of γ-secretase which leads to a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (total Aβ: IC50 = 115 nM (human); Aβ42: IC50 = 200 nM (human)). Uses: Differentiation. Synonyms: tert-butyl (2S) -2-[[ (2S) -2-[[2- (3, 5-difluorophenyl) acetyl]amino]propanoyl]amino]-2-phenylacetate; dapt; 208255-80-5; DAPT (GSI-IX); gamma-Secretase Inhibitor IX; CHEBI:86193; MFCD04974585; DAPT, GSI-IX; InSolution gamma-Secretase Inhibitor IX; N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester; N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester(DAPT); C23H26F2N2O4; GSIIX; S2215_Selleck; AC1NSKCB; PubChem22436; GSI-IX; DAPT,GSI-IX; DAPT; DAPT - GSI-IX; MLS006010075; CHEMBL255682; QCR-29; SCHEMBL1360313; DTXSID00415519; AOB33372; DAPT-Supplied by Selleck Chemicals; EBD16444; ZINC1549363; ABP000317; ZINC01549363; AKOS024457209; CS-0264; NCGC00167803-03; (3,5-Difluorophenylacetyl)-Ala-Phg-OtBu; AC-23163; AK477268; BC649954; CJ-24363; HY-13027; KB-57235; SMR004701228; AB0033805; LS-191073; D4257; GSI-IX, 208255-80-5; X7572; W-5319; AB01566837_01; GSI-IX , GSI IX; 208255-80-5; N-[N-(3,5-difluorophenylacetyl)-L-alanyl]-(S)-phenylglycine t-butyl ester; DAPT|N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester; N-[(3,5-Difluorophenyl)acetyl]-[l-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester; N-[N-(3,5-difluorophenylacetyl)-L-alanyl]-(S)-phenylglycine t-butyl ester. Grades: 0.98. CAS No. 208255-80-5. Molecular formula: C23H26F2N2O4. Mole weight: 432.46. | |
| DBZ | DBZ, also called dibenzazepine, is a γ-secretase inhibitor to treat Alzheimer's Disease, and it also inhibits Notch signaling. Synonyms: YO-01027; YO 01027; YO01027; (2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide; dibenzazepine; GSI XX; Dibenzazepine; 209984-56-5; YO-01027; (S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanamide; Deshydroxy LY 411575; gamma-Secretase Inhibitor XX; DBZ; 209984-56-5 pound not YO 01027; (S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide; N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide; C26H23F2N3O3; GSI-XX; g-secretase inhibitor XX; Gamma-secretase inhibitor; Deshydroxy LY-411514; Deshydroxy LY-411575; MLS006011073; SCHEMBL3046688; DTXSID6040458; AOB1375; ANW-62574; ZINC22056928; AKOS016004347; RL02593; YO01027; NCGC00263188-01; AC-27417; AJ-80844; AK101890; BC638679; SMR004676467; AB0033830; KB-210919; TC-151319; FT-0666470; ST24035862; X7602; Z-3141; (2S)-2-[2-(3,5-. Grades: >98%. CAS No. 209984-56-5. Molecular formula: C26H23F2N3O3. Mole weight: 463.48. | |
| E 2012 | E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 870843-42-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 100 mg. Product ID: HY-10016. | |
| (-)-FRM-024 | (-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimers disease research [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2085780-85-2. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-115726A. | |
| JLK 6 | JLK 6, under the IUPAC name 7-amino-4-chloro-3-methoxyisochromen-1-one, an inhibitor of γ-secretase (IC50 = between 10 μM-1 mM) that belongs to the class of isocoumarin analogs, prevents recovery of Aβ40 and Aβ42 (IC50 < 100 μM) in HEK293 cells overexpressing wild-type and Swedish-mutant β-amyloid precursor protein (APP). Synonyms: JCP-251; JCP 251; JCP251 7-amino-4-chloro-3-methoxyisochromen-1-one; 7-Amino-4-chloro-3-methoxyisocoumarin; jlk6; 62252-26-0; JLK 6; 7-Amino-4-chloro-3-methoxy-isocoumarin; gamma-Secretase Inhibitor XI; 7-amino-4-chloro-3-methoxyisochromen-1-one; AC1L1GQZ; AC1Q3FXG; JLK-6; CHEMBL149518; SCHEMBL3056620; CTK2F1888; AMDGKLWVCUXONP-UHFFFAOYSA-N; HMS3269N03; ZINC2523036; AR-1H3136; ZINC02523036; 7-amino-3-methoxy-4-chloroisocoumarin; AKOS024457236; NCGC00167827-01; AK396360; HE005374; HE366264; TX-017351; 7-Amino-4-chloro-3-methoxy-isochromen-1-one; 7-Amino-4-chloro-3-methoxy-1H-isochromen-1-one; 1H-2-Benzopyran-1-one, 7-amino-4-chloro-3-methoxy-; BRD-K22010301-001-01-2; JLK 6|7-Amino-4-chloro-3-methoxy-1H-2-benzopyran; JLK 6; 7-AMINO-4-CHLORO-3-METHOXY-1H-2-BENZOPYRAN. CAS No. 62252-26-0. Molecular formula: C10H8ClNO3. Mole weight: 225.63. | |
| L-685,458 | L-685,458 is a potent and selective inhibitor of γ-secretase (IC50 = 17 nM) that shows 50-fold selectivity over a variety of aspartyl proteases. It also inhibits Aβ40 and Aβ42 peptides (in human neuroblastoma cells: IC50 = 48 and 67 nM respectively). Uses: Gamma secretase inhibitors and modulators. Synonyms: L-685458; tert-butyl N-[(2S,3R,5R)-6-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl]carbamate. Grades: >98%. CAS No. 292632-98-5. Molecular formula: C39H52N4O6. Mole weight: 672.85. | |
| LY 450139 | Semagacestat is a gamma-secretase inhibitor originally developed by Eli Lilly. In Aug 2010, Phase-III for Alzheimer's disease was discontinued. Uses: Alzheimer's disease. Synonyms: LY 450139; LY450139; LY-450139. (S)-2-hydroxy-3-methyl-N-((S)-1-(((S)-3-methyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1-yl)amino)-1-oxopropan-2-yl)butanamide. Grades: 98%. CAS No. 866488-53-1. Molecular formula: C19-H27-N3-O4. Mole weight: 361.44. | |
| LY-900009 | LY-900009 is a small-molecule inhibitor of Notch signalling with IC50 value of 0.27 nM via selective inhibition of the γ-secretase protein. LY-900009 was developed as a candidate therapeutic drug against AD (IDENTITY trial), which failed in phase III trials. Uses: Gamma secretase inhibitors and modulators. Synonyms: LY900009; LY-900009; LY 900009; (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]amino]-1-oxopropan-2-yl]butanamide. Grades: >98%. CAS No. 209984-68-9. Molecular formula: C23H27N3O4. Mole weight: 409.486. | |
| MK-0752 | MK-0752 is a gamma secretase inhibitor in clinical development. Group: Biochemicals. Alternative Names: cis-4-[ (4-Chlorophenyl) sulfonyl]-4- (2, 5-difluorophenyl) cyclohexanepropanoic Acid. Grades: Highly Purified. CAS No. 471905-41-6. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
| MK-0752 | MK 0752 is a potent and reversible inhibitor of γ-secretase (IC50 ~50 nM). It was shown to reduce the number of breast cancer stem cells in tumorgrafts. Uses: Gamma secretase inhibitors and modulators. Synonyms: Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-; cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid; MK 0752; MK0752. Grades: >98%. CAS No. 471905-41-6. Molecular formula: C21H21ClF2O4S. Mole weight: 442.91. | |
| MRK003 | MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway. Uses: Gamma secretase inhibitors and modulators. Synonyms: MRK-003; MRK 003. CAS No. 623165-93-5. Molecular formula: C25H31F6N3O2S. Mole weight: 551.59. | |
| MRK-560 | MRK-560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system. Group: Fluorinated apis. Alternative Names: N-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide. CAS No. 677772-84-8. Molecular formula: C19H17ClF5NO4S2. Mole weight: 517.92. Appearance: White to off-white solid powder. Purity: >98%. IUPACName: N-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide. Catalog: OFC677772848. |  |
| N-hydroxypipecolic acid | N-Hydroxypipecolic acid, a pivotal biochemical component of drug synthesis for treatment of Alzheimer's and other neurodegenerative diseases, remarkably inhibits gamma-secretase enzyme leading to decreased amyloid beta production, a hallmark of Alzheimer's. Synonyms: 1-hydroxy-2-piperidinecarboxylic acid; 2-Piperidinecarboxylic acid, 1-hydroxy-; hydroxypipecolic acid. Grades: 95%. CAS No. 115819-92-6. Molecular formula: C6H11NO3. Mole weight: 145.16. | |
| Semagacestat | Semagacestat is an inhibitor of the γ-secretase complex that blocks the production of Aβ38 (IC50= 12.0 nM), Aβ40 (IC50= 12.1 nM), and Aβ42 (IC50= 10.9 nM) from H4 human glioma cells stably overexpressing human wild-type APP into the culture medium. In vitro: blocks the production of Aβ38 (IC50= 12.0 nM), Aβ40 (IC50= 12.1 nM), and Aβ42 (IC50= 10.9 nM) without affecting cell viability. In vivo: decreases hippocampal levels of both Aβ42 and Aβ40 at 10 mg/kg (22-23% reduction) and 30 mg/kg (36-41% reduction) and increases β-CTF at 0.3-10 mg/kg in a dose dependent manner with no inhibition on the processing of other γ-secretase substrates, such as Notch, N-cadherin or EphA4, in the brain, but impairs normal cognition in wild-type mice and 3-month-old Tg2576 mice failing to restore cognitive deficits in the Y-maze test. Uses: Gamma secretase inhibitors and modulators. Synonyms: (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(5S)-3-methyl-4-oxo-2,5-dihydro-1H-3-benzazepin-5-yl]amino]-1-oxopropan-2-yl]butanamide; LY 411,575; LY 411575; LY 450139; LY-411,575; LY-411575; LY411,575; LY411575; LY450139; N2-((2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl)-N1-((7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo(b,d)azepin-7-yl)-L-alaninamide; N2-(2-(3,5-difluorophenyl)-2-hydroxyethanoyl)-N1-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo(b,d)azepin-7-yl)alaninamide; LY4501; LY-4501; LY 4501; LY450139; LY-450139; LY 450139; Semagacestat. 425386-60-3. Grades: >98%. CAS No. 425386-60-3. Molecular formula: C19H27N3O4. Mole weight: 361.44. | |
| Z-Ile-Leu-aldehyde | Z-Ile-Leu-aldehyde ia a cell-permeable and reversible inhibitor that inhibits γ-secretase and Notch signaling. It induces apoptosis of murine MOPC315.BM myeloma cells with high Notch activity in vitro. It has potent anti-MM activity and reduces osteolytic lesions in vivo. Uses: Gamma secretase inhibitors and modulators. Synonyms: Z-IL-CHO; GSI-XII; Z-Ile-Leu-al; Z Ile Leu al; Z IL CHO; Gamma-secretase inhibitor XII; [(1S,2S)-1-((S)-1-Formyl-3-methyl-butylcarbamoyl)-2-methyl-butyl]-carbamic acid benzyl ester; Benzyl ((2S,3S)-3-methyl-1-(((S)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)carbamate; N-benzyloxycarbonyl-L-isoleucyl-L-leucinal. Grades: ≥95%. CAS No. 161710-10-7. Molecular formula: C20H30N2O4. Mole weight: 362.46. | |
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