49
15
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39484 |
BACE1-IN-6
BACE1-IN-6 |
||
BACE1-IN-6 is a BACE1 inhibitor with an IC 50 value of 1.5 nM. | |||
T10450 |
BACE1-IN-1
|
BACE | Neuroscience |
BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2). | |||
T10452 |
BACE1-IN-4
|
BACE | Neuroscience |
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), more selective at BACE1 over BACE2. | |||
T10453 | BACE1-IN-5 | Beta Amyloid; BACE | Neuroscience |
BACE1-IN-5 (Compound 15) 是一种 BACE1抑制剂,IC50为 9.1 nM。BACE1-IN-5还可抑制细胞 Aβ,IC50为 0.82 nM。并且,BACE1-IN-5 具有改善 hERG 抑制和 P-gp 外排的药物化学作用。 | |||
T10451 | BACE1-IN-2 | BACE | Neuroscience |
BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM). | |||
T61956 | BACE1/2-IN-1 | ||
BACE1/2-IN-1 (化合物 34) 是有效的BACE1和BACE2抑制剂,IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 具有较低的 Pgp 外排比和改善的被动渗透率。BACE1/2-IN-1 在肝脏微粒体中代谢稳定性降低。 | |||
T63867 |
BACE1-IN-12
|
||
BACE1-IN-12 是能够透过血脑屏障的、有效的 BACE1 抑制剂 (IC50: 8.9 μM)。BACE1-IN-12 能够选择性的抑制 BuChE(丁基胆碱酯酶) 的活性 (IC50: 3.2 μM)。BACE1-IN-12 表现出较好的抗氧化活性,对 DPPH 的 IC50 值为 10.2 μM。BACE1-IN-12 具有潜力进行抗阿尔茨海默病的研究。 | |||
T73076 |
BACE1-IN-10
|
Beta-Secretase | Neuroscience |
BACE1-IN-10为高效的BACE1抑制剂,对重组BACE1(rBACE1)显示出亚微摩尔级别的抑制活性。 | |||
T79022 |
BACE1-IN-13
|
Beta-Secretase | Neuroscience |
BACE1-IN-13 (Compound 36)为一种BACE1抑制剂,展现出口服活性,IC50为2.9 nM。该化合物在hAβ42细胞中显示出强效 (IC50=1.3 nM),证实了其心血管安全性,并在小鼠与狗的动物模型中有效降低Aβ42水平。 | |||
T64074 |
BACE1-IN-8
|
||
BACE1-IN-8 是 BACE1 (β 位 APP 裂解酶 1) 的有效抑制剂 (IC50: 3.9 μM)。 | |||
T62719 | AChE/BACE1/GSK3β-IN-1 | ||
AChE/BACE1/GSK3β-IN-1 是一种口服具有活力的、可透过血脑屏障的、生物利用度适中的 AChE/BACE1/GSK3β的三重抑制剂。AChE/BACE1/GSK3β- IN -1 能够抑制 AChE (IC50: 1.0 μM)、BACE1 (IC50: 20 μM) 和 GSK3β (IC50: 15 μM)。AChE/BACE1/GSK3β-IN-1 能够用于研究阿尔茨海默 (AD)。 | |||
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。 | |||
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。 | |||
T10449 | BACE-1 inhibitor 1 | Others | Others |
BACE-1 inhibitor 1 (Compound 8a) is an effective BACE-1 inhibitor (IC50: 56 nM). | |||
TQ0238 |
Lanabecestat
LY3314814,AZD3293 |
BACE | Neuroscience |
Lanabecestat (AZD3293) 是一种具有高效性和高渗透性、口服活性且可穿过血脑屏障的 BACE1 抑制剂(Ki:0.4 nM),Lanabecestat 可用于研究像阿尔茨海默症类的神经系统疾病。 | |||
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。 | |||
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。 | |||
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。 | |||
T3161L |
BACE-IN-1 acetate
BACE-IN-1 acetate (350228-37-4,Free base) |
BACE | Neuroscience |
BACE-IN-1 acetate (BACE-IN-1 acetate (350228-37-4,Free base)) 已被用作 BACE1 抑制剂测定中的 β 位淀粉样前体蛋白 (APP) 裂解酶-1 (BACE1) 抑制剂。 β-位点淀粉样前体蛋白 (APP) 切割酶-1 (BACE1)是一种天冬氨酸蛋白酶,属于蛋白酶家族,由六个腔内半胱氨酸残基组成。这些残基有助于形成三个分子间二硫键和 N-连接的糖基化位点。 | |||
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。 | |||
T14338 |
Atabecestat
JNJ-54861911 |
BACE | Neuroscience |
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction and it is tolerated and displays a sustained pharmacokinetic (PK) and | |||
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。 | |||
T12429 |
PF-06751979
|
BACE | Neuroscience |
PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay). | |||
T10292 |
AM-6494
|
BACE | Neuroscience |
AM-6494 is a potent and orally active BACE1 inhibitor (IC50: 0.4 nM) with in vivo selectivity over BACE2 (IC50: 18.6 nM). | |||
T25610 |
Lanabecestat camsylate
LY 3314814 camsylate,LY-3314814 camsylate,LY3314814 camsylate |
||
Lanabecestat camsylate is used as a BACE1 Inhibitor. | |||
T71098 |
AZ3971
|
||
AZ3971 is a potent BACE1 inhibitor. AZ3971 blocks BACE1-mediated cleavage of APP and inhibits Aβ42 production HEK cells overexpressing the APP protein which carries the Swedish mutation (HEK.APPswe). | |||
T28915 |
TAK-070
TAK070 |
||
TAK-070 is a non-competitive inhibitor of BACE1. | |||
T39955 |
JNJ-67569762
|
||
JNJ-67569762 is a selective BACE1 inhibitor targeting the S3 pocket ( IC 50 = 2.7 nM). | |||
T80128 |
RE(EDANS)EVNLDAEFK(DABCYL)R
|
Beta-Secretase | Neuroscience |
RE(EDANS)EVNLDAEFK(DABCYL)R为具有EDANS和DABCYL双标记的肽,作为BACE1的荧光底物(Em=360nm,Ex=528nM)。该化合物主要用于评估BACE1酶活性,其活性水平正相关于荧光产生的强度。 | |||
T79422 |
BuChE-IN-8
|
||
BuChE-IN-8 (compound 19c) 为有效抑制 BuChE 的化合物,IC50 值为 559 nM;展现对 BACE1 及 Aβ40 聚集的抑制活性,亦具有显著的抗遗忘特性。 | |||
T62455 | β-Secretase Inhibitor III | ||
β-Secretase Inhibitor III 是一种高度选择性的 BACE1 抑制剂,其 Ki 值为 0.13 nM。 | |||
T26715 |
AZD-3289
AZD 3289 |
||
AZD-3289, a potent BACE1 inhibitor, is used potentially for the treatment of Alzheimer's disease. | |||
T70366 | PF-06663195 | ||
PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1). | |||
T62573 |
AMG-8718
|
||
AMG-8718 是一种选择性的、口服具有活力的、有效的 BACE1 抑制剂,能够作用于 BACE1 (IC50: 0.0007 μM) 和 BACE2 (IC50:0.005 μM)。AMG-8718 能够明显减少 CSF 和大脑中的 Aβ40水平。 | |||
T10014 |
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293 |
Others | Others |
(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzymel (BACE1) inhibitor, and has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively. | |||
T68377 | GRL-8234 | ||
GRL-8234 is a small-molecule BACE1 inhibitor that reverses memory impairments and age-related cognitive decline. | |||
T40393 |
OM99-2
OM99-2 |
||
OM99-2 is an eight-residue peptidomimetic with a high affinity for human brain memapsin 2, exhibiting a Ki value of 9.58 nM. This compound represents a significant advancement in the development of BACE1 inhibitors and holds potential for the study of Alzheimer's disease. | |||
T70711 |
AZD-3839 hemifumarate
|
||
AZD-3839 hemifumarate is a potent and selective BACE1 inhibitor and clinical candidate for the treatment of Alzheimer's disease. | |||
T37661 |
LY 2886721 Hydrochloride
|
||
Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model. | |||
T70800 | Elenbecestat free base | ||
Elenbecestat,also known as E2609 is a BACE1 inhibitor. By inhibiting BACE, a key enzyme in the production of Aβ peptides, E2609 decreases the formation of these peptides which can aggregate into toxic oligomers and protofibrils and eventually form amyloid plaques in the brain. Elenbecestat has been shown to reduce Aβ levels in cerebrospinal fluid, was investigated in two global phase 3 studies in early AD. | |||
T70807 |
Lanabecestat HCl
|
||
Lanabecestat, also known as AZD3293 and LY3314814, is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. | |||
T71899 |
Verubecestat TFA
|
||
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. | |||
T79423 |
BuChE-IN-9
|
||
BuChE-IN-9 (compound 22a) 作为eqBuChE的抑制剂,表现出相当的效力,具有173 nM的IC50值。除此之外,BuChE-IN-9对人BACE1、Aβ聚集及小鼠mGAT1和mGAT4也具有抑制作用,并且显示出显著的抗遗忘特性。 | |||
T40165 |
OM99-2 TFA
OM99-2 TFA |
||
OM99-2 TFA is an eight-residue peptidomimetic compound, functioning as a tight-binding inhibitor of human brain memapsin 2. It exhibits a high affinity for the target with a Ki value of 9.58 nM, making it a promising candidate in the development of BACE1 inhibitors. Due to its potential, OM99-2 presents opportunities for further research in the field of Alzheimer's disease. | |||
T35975 |
6,9-Dichloro-1,2,3,4-tetrahydroacridine
|
||
6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylchol... | |||
T70104 |
Verubecestat tosylate
|
||
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. | |||
T78739 |
PD07
|
||
PD07是一种口服AChE抑制剂,对hAChE的IC50为0.29 μM。体外实验表明PD07也能抑制ChE、BACE1(IC50:13.42 μM)和Aβ1-42的聚集。作为抗氧化剂,PD07显示出DPPH抑制活性(IC50:26.46 μM),能改善因Scopolamine诱导而失忆的大鼠的记忆和认知功能。该化合物适用于阿尔茨海默病的研究。 | |||
T61049 | AChE-IN-11 | ||
AChE-IN-11 (compound 5C) 可用于阿尔茨海默病的研究,它具有神经保护作用和良好的抗氧化活性 (ORAC = 2.5 eq) 。AChE-IN-11 是一种很好的多功能剂,其对于AChE、MAO-B 和 BACE1 的 IC 50 值分别为 7.9 μM、9.9 μM 和 8.3 μM。AChE-IN-11 具有混合型 AChE 抑制作用,可与结合AChE 的 CAS 和 PAS 结合。AChE-IN-11 也是一种选择性金属离子螯合剂。 | |||
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). |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1472 |
Cassiaside
|
Beta-Secretase; BACE | Neuroscience |
Cassiaside 是一种萘甲酮糖苷,抑制 BACE1 (IC50= 4.45 μM; Ki=9.85 μM)。Cassiaside 对半乳糖胺损伤具有明显的肝脏保护作用, 具有潜在的抗阿尔茨海默病 (AD) 活性。 | |||
TN1799 |
Isorubrofusarin-6-O-β-gentiobioside
Isorubrofusarin 10-gentiobioside |
BACE; AChR | Neuroscience |
Isorubrofusarin-6-O-β-gentiobioside 来源于 Cassia obtusifolia Linn 种子,对 AChE 和 BACE1 具有良好的抑制活性。 | |||
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。 | |||
TN1343 |
8-Geranyloxypsoralen
8-香叶草氧基补骨脂素 |
Anti-infection; P450; BACE | Metabolism; Microbiology/Virology; Neuroscience |
8-Geranyloxypsoralen 是一种呋喃香豆素,分离自葡萄柚,是 P450 3A4 的有效抑制剂(IC50:3.93 μM)。 | |||
T3394 |
Timosaponin BII
知母皂苷BII,Prototimosaponin A III |
Beta Amyloid; Others; BACE | Neuroscience; Others |
Timosaponin BII (Prototimosaponin A III) 是一种甾体皂苷,发现于知母根茎中,具有神经保护、抗炎和抗氧化作用。 | |||
T4115 |
Auraptene
橙皮油内酯,7-geranyloxycoumarin,橙皮油素 |
MMP; BACE | Neuroscience; Proteases/Proteasome |
Auraptene 是一种丰富的天然香叶氧基香豆素。它能够抑制基质金属蛋白酶 2 以及关键炎症因子,包括 IL-6,IL-8 和趋化因子 (C-C 基序) 配体-5 (CCL5)的分泌。 | |||
T3914 |
Saikosaponin C
柴胡皂苷C,柴胡皂苷 C |
Beta Amyloid; Caspase | Apoptosis; Neuroscience; Proteases/Proteasome |
Saikosaponin C 是一种柴胡中的活性成分,能够抑制 Aβ1-40 和 Aβ1-42 的释放,抑制异常 tau 蛋白的磷酸化,但对 BACE1 的活性和表达无作用。它在阿尔滋海默症中主要靶作用于amyloid beta 和tau 蛋白。 | |||
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。 | |||
T6S1683 |
Demethoxycurcumin
Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin |
Apoptosis; Antioxidant; Antibacterial; Autophagy | Apoptosis; Autophagy; Microbiology/Virology; oxidation-reduction |
Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分,有抗炎和抗癌作用。 | |||
T2759 |
Loganin
Loganoside,马钱子苷 |
Apoptosis; NF-κB; BACE; AChR; AChE | Apoptosis; Neuroscience; NF-κB |
Loganin (Loganoside) 是山茱萸中的主要环烯醚萜苷类天然产物,具有抗炎、抗休克的作用。 | |||
T8306 |
Epiberberine chloride
表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱 |
Reactive Oxygen Species; Beta-Secretase; BACE; AChR; AChE | Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
Epiberberine chloride (Epiberberine (chloride)) 是一种从黄连中得到的生物碱,是一种AChE 和BChE 抑制剂,和非竞争性的BACE1抑制剂。它具有抗氧化作用,能够清除 ONOO-,可用于研究阿尔滋海默症和糖尿病。 | |||
TN2131 |
Questin
|
BACE; Antibacterial; AChR; AChE | Microbiology/Virology; Neuroscience |
Questin 是一种从花样黄曲霉中提取出来的抗菌剂,具有抗菌活型,对V. harveyi,V. anguillarum,V. cholerae 和 V. parahemolyticus 具有抑制作用,MIC 值分别为 31.25 µg/mL,62.5 µg/mL,62.5 µg/mL 和 125 µg/mL。Questin 对AChE、BChE 和BACE1有很好的抑制潜力,它可能被用于开发阿尔茨海默病的治疗或预防药物。 | |||
TN4399 | Kushenol C | SGLT; NF-κB; ROS; BACE; Antifection | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB |
Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan | |||
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。 |