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gamma-secretasemodulator 1 is a gamma-secretasemodulator, useful for Alzheimer's disease. Synonyms: gamma-secretasemodulator 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-secretasemodulator 2
gamma-secretasemodulator 2, a triazole derivative, a potent and selective γ-secretasemodulator 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-secretasemodulator 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-secretasemodulator 3
gamma-secretasemodulator 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-secretasemodulator 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-Secretasemodulators
gamma-SecretaseModulators 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-SecretaseModulators; 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-SecretaseModulators
gamma-SecretaseModulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Amyloid-β production inhibitor; γ-SecretaseModulators. 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 gammasecretasemodulators 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
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: Gammasecretase 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.
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: Gammasecretase 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 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-SecretaseModulator, 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.
E 2012
E 2012 is a potent gamma (γ) secretasemodulator 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 gammasecretasemodulator 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.
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: Gammasecretase 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-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: Gammasecretase 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 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: Gammasecretase 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: Gammasecretase inhibitors and modulators. Synonyms: MRK-003; MRK 003. CAS No. 623165-93-5. Molecular formula: C25H31F6N3O2S. Mole weight: 551.59.
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: Gammasecretase 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: Gammasecretase 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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