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Gamma-secretase

Gamma secretase is a multi-subunit protease complex, itself an integral membrane protein, that cleaves single-pass transmembrane proteins at residues within the transmembrane domain. Proteases of this type are known as intramembrane proteases. The most well-known substrate of gamma secretase is amyloid precursor protein, a large integral membrane protein that, when cleaved by both gamma and beta secretase, produces a short 37-43[verification needed] amino acid peptide called amyloid beta whose abnormally folded fibrillar form is the primary component of amyloid plaques found in the brains of Alzheimer's disease patients. Gamma secretase is also critical in the related processing of several other type I integral membrane proteins, such as Notch, ErbB4, E-cadherin, N-cadherin, ephrin-B2, or CD44.

DAPT
T6202208255-80-5
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.
  • $53
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γ-Secretase-IN-1
T3521209986-17-4
γ-Secretase-IN-1 is a potent γ-secretase inhibitor that displays partial antiproliferative activity on T-47D cells and inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage.
  • $129
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MK-0752
T2625471905-41-6
MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
  • $52
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Nirogacestat
T69351290543-63-3
Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
  • $34
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RO7185876
T397022226038-71-5In house
RO7185876 is a selective gamma secretase modulator, which can be used in the study of Alzheimer's disease.
  • $293 TargetMol
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Valproic Acid
T706499-66-1
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.
  • $50
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Gossypolone
T319874547-72-2In house
Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch Wnt signaling and induces apoptosis.
  • $195
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γ-Secretase modulator 13
T622631353570-40-7In house
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.
  • $293 TargetMol
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Rovalpituzumab
T766981613313-01-1
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).
  • $178
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BMS-906024
T146801401066-79-2In house
BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.
  • $545
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Bruceine D
TWS204521499-66-1
1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the growth of three pancreatic cancer cell lines, i.e., PANC-1, SW199 and CAPAN-1; induces cytotoxicity in Capan-2 cells via the induction of cellular apoptosis involving the mitochondrial pathway.
  • $41
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RO4929097
T6274847925-91-1
RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14 5 nM).
  • $44
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L-685458
T6870292632-98-5
L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
  • $122
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YO-01027
T6135209984-56-5In house
YO-01027 (DBZ) is a potent γ-secretase inhibitor.
  • $44
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Jagged-1 (188-204) TFA(219127-21-6 free base)
TP1293
Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.
  • $235
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5β-Cholanic acid
T88859546-18-9
5β-Cholanic acid (5beta-Cholanic acid) is a potent γ-secretase modulator used in Alzheimer's disease research.
  • $37
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ELN318463 racemate
T11178L851599-82-1In house
ELN318463 racemate (ELN 318463 racemate) is the racemate of ELN318463 which is an amyloid precursor protein (APP) selective γ-secretase inhibitor.
  • $165
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MRK-560
T16133677772-84-8
MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.
  • $35
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LY-411575
T6063209984-57-6
LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.
  • $38
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Valproic acid sodium salt
T16021069-66-5
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.
  • $42
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Crenigacestat
T36331421438-81-4
Crenigacestat (LY3039478) is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most tumor cell lines tested. It effectively inhibits mutant Notch receptor activity and, in a xenograft tumor model, inhibits the expression of Notch-regulated genes and N1ICD cleavage in the tumor microenvironment.
  • $56
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RBPJ Inhibitor-1
T355662682114-39-0
RBPJ Inhibitor-1 (RIN1), a compound that impedes the functional interaction between RBPJ and SHARP, effectively inhibits NOTCH-dependent tumor cell proliferation[1].
  • $34
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Aβ42-IN-2
T96411914989-80-2In house
Aβ42-IN-2, a γ-secretase modulator with an IC50 of 6.5 nM for Αβ42, can be used for Alzheimer's disease research [1].
  • $35
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Brontictuzumab
T767851447814-75-6
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.
  • $297
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