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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12188 |
NB-360
|
BACE | Neuroscience |
NB-360 是一种有效的脑穿透性 BACE1 和 BACE2 抑制剂,对小鼠和人源 BACE1 和 BACE2 的 IC50 分别为 5、5 和 6 nM。 NB-360 对相关的天冬氨酰蛋白酶、胃蛋白酶、组织蛋白酶 E 和组织蛋白酶 D 具有出色的特异性。 | |||
T2639 |
LY2811376
|
Beta Amyloid; Beta-Secretase; BACE | Neuroscience |
LY2811376 是可口服的非肽段β-secretase (BACE1)抑制剂,IC50=239 nM-249 nM,能够降低 Aβ 蛋白的分泌,EC50=300 nM。 | |||
T13253 |
Umibecestat
CNP520 |
BACE | Neuroscience |
Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。 | |||
T11175 |
Elenbecestat
E2609 |
Beta-Secretase; BACE | Neuroscience |
Elenbecestat (E2609) 是一种高效、有口服活性的,能透过 CNS 的 BACE-1抑制剂,它有用于阿尔茨海默病 (AD) 的研究潜力。 | |||
T6058 |
LY2886721
|
Beta-Secretase; BACE | Neuroscience |
LY2886721 是选择性的,口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂,对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性,但缺乏对 BACE2的选择性。它可透过血脑屏障,并可用于研究阿尔茨海默氏病。 | |||
T4398 |
LX2343
|
Beta Amyloid; Beta-Secretase; BACE; PI3K; Autophagy | Autophagy; Neuroscience; PI3K/Akt/mTOR signaling |
LX2343 是一种非 ATP 竞争性 PI3K 抑制剂,IC50 为 15.99±3.23 μM。它是一种 BACE1 酶抑制剂,IC50 值为 11.43±0.36 μM。它在促进 Aβ 清除中刺激自噬。 | |||
T6772 |
AZD3839 free base
AZD3839 |
Beta-Secretase; BACE | Neuroscience |
AZD3839 free base 是一种具有口服活性的、选择性的、可透过大脑屏障的BACE1抑制剂 (Ki=26 nM),对 BACE2 和组织蛋白酶 D 的选择性分别为 14 倍和 >1000 倍。在小鼠、豚鼠和非人灵长类动物中,它剂量和时间依赖性的降低血浆、脑和脑脊液 Aβ 水平,可用于研究阿尔茨海默病。 | |||
T7011 |
Verubecestat
MK-8931,维罗司他 |
Beta-Secretase; BACE | Neuroscience |
Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂,Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40,并具有潜力用于阿尔茨海默氏病。 | |||
T3285 |
Eslicarbazepine Acetate
Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa |
Beta-Secretase; Sodium Channel | Membrane transporter/Ion channel; Neuroscience |
Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。 | |||
T13434 |
β-Secretase Inhibitor IV
|
Others | Others |
β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively). | |||
T40260 |
β-Secretase Inhibitor II
|
Others | Others |
β-Secretase Inhibitor II is a tripeptide aldehyde compound that acts as an inhibitor of β-Secretase. It exhibits a simple structure and has an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM specifically against Aβ 1-42. This compound is particularly useful in research related to Alzheimer's disease. | |||
T39251 |
β-Secretase Inhibitor I
|
Others | Others |
β-Secretase Inhibitor I is a highly potent inhibitor of the β-secretase enzyme. This compound exhibits exceptional inhibitory activity while also demonstrating a significant reduction in cardiovascular and liver toxicity. | |||
T3161 |
β-Secretase inhibitor-STA
|
Beta-Secretase | Neuroscience |
BACE-IN-1 是淀粉样前体蛋白 β-分泌酶抑制剂。 | |||
T11362 |
gamma-Secretase Modulators
γ-Secretase Modulators,Amyloid-β production inhibitor |
Others | Others |
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. | |||
T83616 |
SEW06622
|
BACE; AChE | Neuroscience |
SEW06622 是一种有效的 乙酰胆碱酯酶(AChE)和β-分泌酶-1(BACE-1)抑制剂,是治疗阿尔茨海默病的潜在候选化合物。 | |||
T6870 |
L-685458
L-685,458 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
L-685458 (L-685,458) 是一种过渡状态模拟 γ-分泌酶抑制剂,抑制淀粉样 β-蛋白前体 γ-分泌酶活性,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。它抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,可研究阿尔茨海默病和癌症。 | |||
T28390 |
PF9238
PF 9238,PF-9238 |
Others | Others |
PF9238 is an inhibitor of beta-secretase I. PF9238 has a CatD potency of 12 uM in vivo. | |||
T24924 |
Umibecestat HCl (1387560-01-1 free base)
CNP 520,Umibecestat HCl,Umibecestat hydrochloride,CNP520,CNP-520 |
Others | Others |
Umibecestat is a beta-secretase inhibitor. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. | |||
T71899 |
Verubecestat TFA
|
Others | Others |
Verubecestat TFA, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat TFA is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat TFA reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T70104 |
Verubecestat tosylate
|
Others | Others |
Verubecestat tosylate, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat tosylate is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat tosylate reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T69664 |
Umibecestat HCl
|
Others | Others |
Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S2361 |
Epiberberine
|
ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE | Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling |
Epiberberine 是一种从黄连中得到的生物碱,是AChE 和BChE 抑制剂,和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期,它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用,能够清除 ONOO-,可用于阿尔滋海默症和糖尿病的研究。 | |||
T3769 |
Tenuifolin
|
Others; Beta-Secretase; AChE | Neuroscience; Others |
Tenuifolin 是一种从远志中分离出的三萜,能够抑制β-secretase 以减少 Aβ 蛋白分泌,具有神经保护作用。 它可通过降低 AChE 活性来改善衰老小鼠的学习和记忆能力,有潜力用于阿尔茨海默氏病的研究。 | |||
T8179 |
Aloeresin D
芦荟新甙D,芦荟新苷 D |
Beta-Secretase; BACE | Neuroscience |
Aloeresin D 是一种从芦荟中分离得到的色原酮苷,能够抑制 β-分泌酶活性,IC50=39 μM。 | |||
TN2190 |
Scoulerine
|
Apoptosis; Beta-Secretase; BACE; Parasite | Apoptosis; Microbiology/Virology; Neuroscience |
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。 | |||
T8306 |
Epiberberine chloride
|
Antioxidant; BACE; AChR; AChE | Neuroscience; oxidation-reduction |
Epiberberine chloride 是一种来自Coptis chinensis Franch.的天然原小檗碱,是 AChE、 BChE 和 BACE1 抑制剂,IC50 值分别为 1.07,6.03 和 8.55 μM。Epiberberine chloride 具有抗氧化作用,抑制Ca9-22和FaDu细胞系的运动,可用于研究高脂血症、阿尔滋海默症和糖尿病。 | |||
T2S1181 |
Aloenin
Aloenin A,Aloearbonaside,芦荟宁 |
Beta-Secretase; AChR | Neuroscience |
Aloenin (Aloenin A) A 是一种具有清除过氧自由基作用的天然产物,对 β-分泌酶 (BACE) 具有中等抑制活性。 | |||
TN2217 |
Sophoflavescenol
槐苦参醇,槐黄醇 |
Others; Beta-Secretase; BACE; PDE; AChR; AChE | Metabolism; Neuroscience; Others |
Sophoflavescenol 是异戊烯基黄酮类化合物,能够抑制PDE5的活性,IC50=0.013 μM。它也抑制 RLAR,HRAR,BACE1,AChE 和 BChE,IC50值分别为 0.30 µM,0.17 µM,10.98 µM,8.37 µM 和 8.21 µM。 | |||
T3682 |
(-)-Catechin gallate
(-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate |
Others; COX | Immunology/Inflammation; Neuroscience; Others |
(-)-Catechin gallate ((-)-Catechin 3-O-gallate) 是绿茶儿茶素中的微量组分,可抑制COX-1和COX-2活性。它抑制人 Beta-secretase,对氯喹敏感的恶性疟原虫 NF54 和耐氯喹的恶性疟原虫 K1 具有抗疟原虫活性。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-03065 |
BACE2 Protein, Mouse, Recombinant (His)
CEAP1,BAE2,1110059C24Rik,β-site APP-cleaving enzyme 2,CDA13,... |
Mouse | HEK293 Cells |
BACE2, also known as beta secretase 2, belongs to the peptidase A1 family. It is a protease known to be an important enzyme involved in the cellular pathways. BACE2 has been shown to interact with GGA1 and GGA2. It is the major β-secretase in vivo. BACE2 is located on chromosome 21 and may play a role in alzheimer's disease pathogenesis in down syndrome(DS). Overexpression of BACE2 by lentivirus markedly reduced amyloid β protein production in primary neurons. Despite an extra copy of the BACE2 ... | |||
TMPJ-00358 |
DR6 Protein, Mouse, Recombinant (hFc & His)
BM-018,CD358,DR6,Tnfrsf21,Tumor necrosis factor receptor sup... |
Mouse | HEK293 Cells |
Tumor necrosis factor receptor superfamily member 21(DR6) is a single-pass type I membrane protein and contains 1 death domain and 4 TNFR-Cys repeats. The protein may activate NF-kappa-B and promote apoptosis and it may activate JNK and be involved in T-cell differentiation.It is required for both normal cell body death and axonal pruning. Trophic-factor deprivation triggers the cleavage of surface APP by beta-secretase to release sAPP-beta which is further cleaved to release an N-terminal fragm... | |||
TMPJ-00782 |
Amyloid Precursor Protein, Human, Recombinant (hFc)
Amyloid Precursor,Amyloid Precursor Protein 695,APP695 |
Human | HEK293 Cells |
Amyloid precursor protein (APP) is a type I membrane protein with several isoforms due to alternative splicing, performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Of the three major splice isoforms of APP (APP695, APP751, and APP770) APP695 is the predominant neuronal form from which Amyloid beta peptide and transcriptionally-active cleaved intracellular domain of APP (AICD) are preferentially generated by selective process... |