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Gamma-secretase

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Gamma-secretase Signaling Pathway Map

Isoform-selective Inhibitors

Gamma-secretase Products

All (15)
Gamma-secretase Inhibitors (12)
Gamma-secretase Antibodies (1)
Gamma-secretase Modulators (2)
New Gamma-secretase Products

Catalog No.	Product Name	Information	Product Use Citations
S1262	Avagacestat (BMS-708163)	Avagacestat (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.	Cell, 2021, 184(2):521-533.e14 Biochem Biophys Res Commun, 2021, 570:137-142 Carcinogenesis, 2020, 41(7):993-1004
S1575	RO4929097	RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.	Proc Natl Acad Sci U S A, 2021, 118(22)e2026184118 Cell Rep, 2021, 37(1):109774 Cell Death Differ, 2021, 10.1038/s41418-021-00861-5
S1594	Semagacestat (LY450139)	Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.	Life Sci Alliance, 2021, 4(4)e202000844 Cancer Cell, 2020, 13;37(1):104-122e12 Carcinogenesis, 2020, 41(7):993-1004
S2215	DAPT (GSI-IX)	DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.	Immunity, 2021, S1074-7613(21)00344-7 Neuron, 2021, 109(12):1949-1962.e6 Sci Adv, 2021, 7(5)eabc9781
S2660	MK-0752	MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.	Carcinogenesis, 2020, 41(7):993-1004 Mol Cancer Ther, 2020, molcanther.0654.2020 Sci Rep, 2019, 9(1):1897
S2711	Dibenzazepine (YO-01027)	Dibenzazepine (YO-01027, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.	Nature, 2021, 598(7881):510-514 Signal Transduct Target Ther, 2021, 6(1):148 ACS Nano, 2020, 22
S2714	LY411575	LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.	Nat Commun, 2021, 12(1):6839 J Endocrinol, 2021, JOE-21-0016.R1 Nature, 2020, 10.1038/s41586-020-2946-9
S7169	Crenigacestat (LY3039478)	Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.	Nucleic Acids Res, 2021, gkab800 Cancer Res, 2021, canres.0524.2021 Oncoimmunology, 2021, 10(1):1881268
S7394	MDL-28170	MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
S7673	L-685,458	L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with K_i of 17 nM.	Biochem Biophys Res Commun, 2021, 570:137-142 Aging (Albany NY), 2020, 12(1):481-501 J Cell Biol, 2019, 218(2):644-663
S8018	Nirogacestat (PF-03084014)	Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.	Stem Cell Res Ther, 2020, 11(1):258 Pharm Res, 2020, 37(10):185 Mol Ther Oncolytics, 2019, 13:58-66
S8185	FPS-ZM1	FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE.	Cell Death Discov, 2021, 7(1):337 J Cancer, 2021, 12(2):518-529 Ann Transl Med, 2021, 9(6):494
A5298	ADAM10 Rabbit Recombinant mAb	ADAM10 Rabbit Recombinant mAb detects endogenous level of total ADAM10.
S7323	Itanapraced (CHF 5074)	Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
S8603	NGP 555	NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.
S1262	Avagacestat (BMS-708163)	Avagacestat (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.	Cell, 2021, 184(2):521-533.e14 Biochem Biophys Res Commun, 2021, 570:137-142 Carcinogenesis, 2020, 41(7):993-1004
S1575	RO4929097	RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.	Proc Natl Acad Sci U S A, 2021, 118(22)e2026184118 Cell Rep, 2021, 37(1):109774 Cell Death Differ, 2021, 10.1038/s41418-021-00861-5
S1594	Semagacestat (LY450139)	Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.	Life Sci Alliance, 2021, 4(4)e202000844 Cancer Cell, 2020, 13;37(1):104-122e12 Carcinogenesis, 2020, 41(7):993-1004
S2215	DAPT (GSI-IX)	DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.	Immunity, 2021, S1074-7613(21)00344-7 Neuron, 2021, 109(12):1949-1962.e6 Sci Adv, 2021, 7(5)eabc9781
S2660	MK-0752	MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.	Carcinogenesis, 2020, 41(7):993-1004 Mol Cancer Ther, 2020, molcanther.0654.2020 Sci Rep, 2019, 9(1):1897
S2711	Dibenzazepine (YO-01027)	Dibenzazepine (YO-01027, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.	Nature, 2021, 598(7881):510-514 Signal Transduct Target Ther, 2021, 6(1):148 ACS Nano, 2020, 22
S2714	LY411575	LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.	Nat Commun, 2021, 12(1):6839 J Endocrinol, 2021, JOE-21-0016.R1 Nature, 2020, 10.1038/s41586-020-2946-9
S7169	Crenigacestat (LY3039478)	Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.	Nucleic Acids Res, 2021, gkab800 Cancer Res, 2021, canres.0524.2021 Oncoimmunology, 2021, 10(1):1881268
S7394	MDL-28170	MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
S7673	L-685,458	L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with K_i of 17 nM.	Biochem Biophys Res Commun, 2021, 570:137-142 Aging (Albany NY), 2020, 12(1):481-501 J Cell Biol, 2019, 218(2):644-663
S8018	Nirogacestat (PF-03084014)	Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.	Stem Cell Res Ther, 2020, 11(1):258 Pharm Res, 2020, 37(10):185 Mol Ther Oncolytics, 2019, 13:58-66
S8185	FPS-ZM1	FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE.	Cell Death Discov, 2021, 7(1):337 J Cancer, 2021, 12(2):518-529 Ann Transl Med, 2021, 9(6):494
A5298	ADAM10 Rabbit Recombinant mAb	ADAM10 Rabbit Recombinant mAb detects endogenous level of total ADAM10.
S7323	Itanapraced (CHF 5074)	Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
S8603	NGP 555	NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.