gamma-secretase

Gamma-secretase modulator 3 (γ-secretase modulator 3) is a γ-secretase modulator that reduces Aβ production.

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

CIA-1 (Free base) is a nuclear receptor COUP-TFII inhibitor with IC50 values ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines. CIA-1 (Free base) inhibits tumor growth in a mouse model of prostate cancer xenografts.

Gamma-secretase inhibitor-1 is a gamma-secretase modulator valuable for Alzheimer's disease [1].

Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.

gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value.

Gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSM) that crosses the blood-brain barrier and inhibits the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). This compound is valuable for studying Alzheimer's disease.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115 200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

RO7185876 is a selective gamma secretase modulator, which can be used in the study of Alzheimer's disease.

γ-Secretase modulator 13 is a γ-secretase modulator (GSMs) that inhibits the production of amyloid β-peptide Aβ42 and can be used to study Alzheimer's disease and tumors.

CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).

Begacestat (GSI-953) is a potent and selective gamma-secretase inhibitor (γ-secretase) that inhibits Amyloid-beta production with nanomolar potency, selectively inhibits cleavage of APP in cellular level Notch cleavage assays, reverses situational memory deficits, and can be used to study Alzheimer's disease.

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

Avagacestat (BMS-708163) (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

Legumain inhibitor 1 is a highly potent and specific Legumain inhibitor with potential anticancer activity for cancer research.

HDAC6-IN-9 is an orally active and highly effective γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.

CIA-1 inhibits the nuclear receptor COUP-TFII, with IC50s ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines.CIA-1 inhibits the growth of a variety of prostate cancer cell lines in vitro and inhibits COUP-TFII activity to regulate its target genes.CIA-1 in vivo exhibits tumor growth inhibitory effects in a mouse model of prostate cancer xenografts. inhibitory effect on tumor growth in a xenograft mouse model of prostate cancer in vivo.

Rovalpituzumab is a humanized monoclonal antibody targeting delta-like protein 3 (DLL3) and is utilized to synthesize antibody-active molecule conjugates (ADCs). It exhibits anticancer activity and is used in the treatment of small cell lung cancer (SCLC).

Brontictuzumab (OMP 52M5) is a monoclonal antibody that targets Notch1 and inhibits activation of the pathway. It has antitumor activity, inhibits tumor cell proliferation, and can be used in the study of leukemias and lymphomas.

Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody and a potent Notch pathway inhibitor, demonstrating efficacy in various cancer models both as a monotherapy and in conjunction with chemotherapy agents.