| Cat. No. |
Product Name |
CAS No. |
Information |
| H8353 |
γ-secretase modulator 14a
|
1485066-18-9 |
A potent, selective, orally active γ-secretase modulator with Aβ42 IC50 of 39 nM; shows good to excellent selectivity for the reduction of Aβ42 in the cellular assays; significantly reduces Aβ42 in the CNS compartment in vivo in nontransgenic rat models. |
| H8352 |
Z-Ile-Leu-aldehyde
|
161710-10-7 |
Z-Ile-Leu-aldehyde (Z-IL-CHO, GSI-XII, γ-Secretase inhibitor XII) is a potent gamma-secretase and Notch signaling inhibitor; induces morphologic erythroid differentiation and promotes hemoglobin production, suppresses short-term growth and colony formation in erythroid leukemia cell lines; impairs murine osteoclast differentiation of RANKL-stimulated RAW264.7 cells in vitro, exhibits potent anti-MM activity and reduces osteolytic lesions in he murine myeloma model. |
| H8351 |
Semagacestat
|
425386-60-3 |
A potent γ-secretase inhibitor that inhibits β-amyloid Aβ42, Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; reduces the secretion of Aβ42, Aβ40, and Aβ38 in cells and increases β-CTF in cell lysates, also inhibits Notch signaling with IC50 of 14.1 nM; increases intracellular byproduct peptides, produced along with Aβ through serial γ-cleavage of βAPP, as well as intracellular long Aβ species, in cell-based and in vivo studies of AD model mice; a pseudo-inhibitor of γ-secretase. |
| H8350 |
SCH 900229
|
1100361-36-1 |
SCH 900229 is a potent and presenilin 1 selective, and orally active inhibitor of γ-secretase (Aβ40 IC50=1.3 nM); demonstrates excellent lowering of Aβ in preclinical animal models. |
| H8349 |
RO4929097
|
847925-91-1 |
RO4929097 (RG 4733) is a potent, selective, orally active γ-secretase inhibitor with IC50 of 4 nM, inhibits Notch processing in the Notch cell-based reporter assay with IC50 of 5 nM; displays >100-fold selectivity against a panel of 75 other proteins of various types including receptors, ion channels and enzymes; inhibits Notch processing in human tumor-derived cells, inhibits the production of ICN, reducing the expression of the downstream Notch target Hes1 in A549 cells; demonstrates in vivo efficacy in A549 xenograft model. |
| H8348 |
PF-06648671
|
1587727-31-8 |
PF-06648671 (PF6648671) is a novel oral γ-secretase modulator being developed for the treatment of Alzheimer's disease. |
| H8347 |
MRK-560
|
677772-84-8 |
MRK-560 is a potent, brain-penetrant and orally bioavailable γ-secretase inhibitor that inhibits proteolytic cleavage of APP over the Notch pathway; inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with IC50 of 0.65 nM, reduces levels of Aβ in the brain and cerebrospinal fluid (CSF) in rats with ED50 of 6 and 10 mg/kg. |
| H8346 |
MRK-003
|
623165-93-5 |
A potent γ-secretase inhibitor with IC50 of 0.4 nM, inhibition of Aβ secretion from SH-SY5Y SPA4CT cells; inhibits the γ-secretase-mediated cleavage of the Notch receptor, reduces tumor cell proliferation, inhibits serum independence, and induces apoptosis in vitro and in vivo using mouse xenograft models. |
| H8345 |
MK-0752
|
471905-41-6 |
A potent γ-secretase inhibitor that shows dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells; Notch signaling inhibitor. |
| H8344 |
LY900009
|
209984-68-9 |
LY900009 (LY-900009) is an orally active small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein, inhibits Notch signalling in tumour cell lines and endothelial cells with IC50 of 0.005-20 nM; dose dependently inhibits Notch cleavage and induced apoptosis 24 h after a single 3 mg/kg oral dose in xenograft tumour models, also demonstrates inhibition of angiogenesis through formation of leaky vasculature. |
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