γ-secretase

Gamma secretase

γ-secretase

Related Products

γ-Secretase is a multimeric aspartyl protease that cleaves the membrane-spanning region of the β-carboxyl terminal fragment (βCTF) generated from β-amyloid precursor protein. γ-Secretase defines the generated molecular species of amyloid β-protein (Aβ), a critical molecule in the pathogenesis of Alzheimer's disease (AD).

γ-Secretase is composed of four subunits: Aph-1, nicastrin (Nct), Pen-2 and presenilin (PS), which is the catalytic subunit of the enzyme. Endoproteolysis of PS, which results in the formation of PS1-NTF (N-terminal fragment) and CTF (C-terminal fragment) heterodimer, is required for γ-secretase activation. γ-Secretase cleaves amyloid precursor protein (APP), Notch and many other substrates. Aberrant cleavage of APP contributes to the pathogenesis of AD and abnormal Notch signaling promotes tumor growth. γ-Secretase is a highly valued drug target in Alzheimer's disease and cancer. Multiple classes of small molecules that target γ-secretase have been developed, including both inhibitors (GSIs) and modulators (GSMs).

γ-secretase Related Products (90)
Antibodies (5)

By Effects:	Controls (2) Inhibitors (54) Modulators (28)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-145428

BT-GSI	Inhibitor
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.

HY-156012

PSEN1-IN-2	Inhibitor
PSEN1-IN-2 (Compound 13K) is a PSEN1 inhibitor. PSEN1-IN-2 inhibits PSEN1-APH1A and PSEN1-APH1B complex with IC₅₀s of 6.9 and 2.4 nM. PSEN1-IN-2 can be used for Alzheimer's disease research.

HY-147720

γ-Secretase modulator 11
γ-Secretase modulator 11 (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.

HY-117482A

BPN-15606 besylate	Modulator
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

HY-15211

MRK 003	Inhibitor
MRK 003 is a potent, selective and orally active γ-secretase inhibitor. MRK 003 reduce brain Aβ production in vivo. MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation in vivo and in vitro.

HY-156011

PSEN1-IN-1	Inhibitor
PSEN1-IN-1 (Compound (+)-13b) is a PSEN1 inhibitor. PSEN1-IN-1 inhibits PSEN1-APH1A and PSEN1-APH1B complex with IC₅₀s of 19 and 5.5 nM. PSEN1-IN-1 can be used for Alzheimer's disease research.

HY-117957

BMS-932481	Modulator
BMS-932481 is an orally active modulator for γ-secretase, selectively reduce Aβ1-42 and Aβ1-40 production, with IC₅₀s of 6.6 and 25.3 nM, respectively.

HY-B1786S

Sulindac sulfide-d₃	Inhibitor
Sulindac sulfide-d₃ is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.

HY-164451

GSI-18	Inhibitor
GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 inhibits the attachment-free growth of pancreatic cancer cells by inhibiting Notch signaling.

HY-16633

ELND 007	Inhibitor
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease.

HY-14176G

Compound E (GMP)	Inhibitor
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a γ-secretase inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀ values of 0.24, 0.37, and 0.32 nM, respectively.

HY-50884

BMS 433796	Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.

HY-117381

γ-secretase-IN-2	Inhibitor
γ-secretase-IN-2 (Compound 34) is an inhibitor for γ-secretase, with an IC₅₀ of 0.06 nM. γ-secretase-IN-2 can be used for the study of Alzheimer's disease.

HY-158012

LY3056480	Inhibitor
LY3056480 is a gamma-secretase inhibitor (GSI) that inhibits Notch signaling. LY3056480 improves mild to moderate sensorineural hearing loss and is safe and tolerable. Intratympanic administration of LY3056480 induces hair cell regeneration and partial hearing recovery in mammals.

HY-163885

SSZ	Inhibitor
SSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice.

HY-146151

γ-Secretase modulator 12	Modulator
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC₅₀ of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice.

HY-147720A

γ-Secretase modulator 11 hydrochloride	Modulator
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC₅₀ of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease.

HY-139052

III-31-C	Inhibitor
III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor. III-31-C inhibits Aऔ production with an IC₅₀ of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research.

HY-19550

PF-06442609	Modulator
PF-06442609 is an orally active γ secretase modulator, with an IC₅₀ of 6 nM for Aβ42. PF-06442609 possesses brain good penetration.

HY-B1786R

Sulindac sulfide (Standard)	Inhibitor
Sulindac sulfide (Standard) is the analytical standard of Sulindac sulfide. This product is intended for research and analytical applications. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.

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γ-secretase

γ-secretase

γ-secretase Related Products (90)

Antibodies (5)

γ-secretase Related Products (90):