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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.
Cat. No. 製品名 CAS No. Purity Chemical Structure
T3075 FLI-06 313967-18-9 98%
FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
T71534L CIA-1 (Free base) 452087-38-6 98%
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) inhib...
T6861 IMR-1 310456-65-6 98%
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T6870 L-685458 292632-98-5 98%
L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
T16133 MRK-560 677772-84-8 98%
MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.
T76788 Demcizumab 1243262-17-0 98%
Demcizumab
Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody. Demcizumab is a potent Notch pathway inhibitor. Demcizumab is effective in multiple cancer models, bo...
T76698 Rovalpituzumab 1613313-01-1 98%
Rovalpituzumab
Rovalpituzumab is a humanized monoclonal antibody targeting delta-like protein 3 (DLL3). Rovalpituzumab can be used to synthesize antibody-active molecule conjug...
T3540 IMR-1A 331862-41-0
IMR-1A is the metabolite of IMR-1 which is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T3399 Psoralidin 18642-23-4
Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive p...
TQ0026 MDR-1339 1018946-38-7
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
T9641 Aβ42-IN-2 1914989-80-2 100%
Aβ42-IN-2 is a γ-secretase modulator. Aβ42-IN-2 has an IC 50 of 6.5 nM for Αβ 42. Aβ42-IN-2 can be used for the Alzheimer's disease research[1].
T14673 BMS 299897 290315-45-6 100%
BMS 299897 is a sulfonamide γ-secretase inhibitor. It has an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor pr...
T21890 JLK6 62252-26-0 96.50%
JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling
T31987 Gossypolone 4547-72-2 96.66%
Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch/Wnt signaling and induces apoptosis.
T6063 LY-411575 209984-57-6 97.03%
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 0.3...
T4S1990 Carvacrol 499-75-2 97.52%
1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effect...
T6274 RO4929097 847925-91-1 97.68%
RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
T10532 BI-1408 2231075-94-6 97.91%
BI-1408 is a modulator potent of γ secretase (IC50: 0.04 μM for Aβ42).
T2262 Itanapraced 749269-83-8 98%
Itanapraced (CHF5074), a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
T13410 ZLDI-8 667880-38-8 98.09%
ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.
FLI-06
T3075
FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
CIA-1 (Free base)
T71534L
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) inhib...
IMR-1
T6861
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
L-685458
T6870
L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
MRK-560
T16133
MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.
Demcizumab
T76788
Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody. Demcizumab is a potent Notch pathway inhibitor. Demcizumab is effective in multiple cancer models, bo...
Rovalpituzumab
T76698
Rovalpituzumab is a humanized monoclonal antibody targeting delta-like protein 3 (DLL3). Rovalpituzumab can be used to synthesize antibody-active molecule conjug...
IMR-1A
T3540
IMR-1A is the metabolite of IMR-1 which is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
Psoralidin
T3399
Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive p...
MDR-1339
TQ0026
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
Aβ42-IN-2
T9641
Aβ42-IN-2 is a γ-secretase modulator. Aβ42-IN-2 has an IC 50 of 6.5 nM for Αβ 42. Aβ42-IN-2 can be used for the Alzheimer's disease research[1].
BMS 299897
T14673
BMS 299897 is a sulfonamide γ-secretase inhibitor. It has an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor pr...
JLK6
T21890
JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling
Gossypolone
T31987
Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch/Wnt signaling and induces apoptosis.
LY-411575
T6063
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 0.3...
Carvacrol
T4S1990
1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effect...
RO4929097
T6274
RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
BI-1408
T10532
BI-1408 is a modulator potent of γ secretase (IC50: 0.04 μM for Aβ42).
Itanapraced
T2262
Itanapraced (CHF5074), a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
ZLDI-8
T13410
ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.
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