|Description||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).|
|Brife Description||An inhibitor of γ-secretase (IC50= between 10 μM-1 mM)|
|Synonyms||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|
|Solubility||Soluble to 100 mM in DMSO and to 25 mM in ethanol|
|Storage||Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -26℃ for long term (months to years).|
|Boiling Point||456.1℃ at 760 mmHg|
gamma-secretase modulator 3
gamma-secretase modulator 3 is a γ-secretase inhibitor.
Semagacestat is a gamma-secretase inhibitor originally developed by Eli Lilly. In Aug 2010, Phase-III for Alzheimer's disease was discontinued.
LY-411575 isomer 3, is an isomer of LY411575, which is a potent, cell-permeable γ-secretase inhibitor (IC50= 0.078 nM/0.082 nM (in membrane-assay/in cell-based...
MK 0752, a potent, reversible inhibitor of γ-secretase (IC50 ~50 nM), reduces the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells (IC50= 5 nM).
gamma-secretase modulator 1
gamma-secretase modulator 1 is a gamma-secretase modulator, useful for Alzheimer's disease.
RO4929097, a small-molecule inhibitor of γ secretase (IC50= 4 nM, EC50= 5 nM), inhibits cellular processing of Aβ40 (EC50= 14 nM) and Notch(EC50= 5 nM). In vitr...
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 prima...
LY-411575, also known as LSN-411575, is a potent, cell-permeable γ-secretase inhibitor (IC50= 0.078 nM/0.082 nM (in membrane-assay/in cell-basedγ-secretase ass...
E 2012, is a potent selective, orally bioavailable γ-secretase modulator without affecting Notch processing that can used to treat Alzheimer's Disease.
CHF5074, also known as CSP-1103, is a novel γ-secretase modulator. It could reduce Aβ42 and Aβ40 secretion, which IC50 value is 3.6 and 18.4 μM respectively. It...
TC-E 5006, also called BIIB042, a potent γ-secretase modulator, which lowered Aβ42, increased Aβ38, but had little to no effect on Aβ40 levels both in vitro and...
PF 3084014 hydrobromide, developed by Pfizer, is a potent γ-secretase inhibitor (in whole cell: IC50= 1.2 nM; in cell-free assaysand IC50= 6.2 nM).
K 01-162 binds and destabilizes AβO (β-amyloid( EC50= 0.080 mM; IC50= 80 nM), can reduce the brain amyloid burden that exists in both fibrillar and RIPA-soluble...
ELND006 is one of the newest molecules to be reported on regarding the testing of the β-amyloid hypothesis. At the 2010 Alzheimer’s Association International Co...
LY-411575 isomer 2, is an isomer of LY411575, which is a potent, cell-permeable γ-secretase inhibitor (IC50= 0.078 nM/0.082 nM (in membrane-assay/in cell-based...
Begacestat is a selective thiophene sulfonamide inhibitor of amyloid precursor protein γ-secretase. Begacestat inhibits Abeta production with low nanomolar pote...
LY-411575 isomer 1
LY-411575 isomer 1, is an isomer of LY411575, which is a potent, cell-permeable γ-secretase inhibitor (IC50= 0.078 nM/0.082 nM (in membrane-assay/in cell-based...
gamma-Secretase Modulators, as a potent modulator of γ-secretase, it is derived from oxadiazine. IC50: Aβ42=11 nM, Aβtotal/ Aβ42=1170.
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) fro...
L-685,458, a transition state analogue inhibitor, as a selective and potent inhibitor of γ-secretase (IC50 = 17 nM) it shows > 50-fold selectivity over a variet...