46
7
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T19483 | Notch 1 TFA | Others | Others |
Notch 1 TFA encodes a member of the NOTCH family of proteins. | |||
T16341 |
Notch inhibitor 1
|
Others | Others |
Notch inhibitor 1 is an effective Notch inhibitor (IC50s: 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively). Notch inhibitor 1 is also used in the research of cancer. | |||
T3540 |
IMR-1A
|
Gamma-secretase; Drug Metabolite | Metabolism; Neuroscience; Proteases/Proteasome; Stem Cells |
IMR-1A 是 IMR-1 的酸代谢物。IMR-1A 是 Notch 抑制剂,IC50=0.5 μM。IMR-1A 相对于 IMR-1 的效力提高了 50 倍。 | |||
T6861 |
IMR-1
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
IMR1 是一种Notch 抑制剂,IC50=26 μM。它能够阻止 Maml1 募集到染色质上的 Notch 三元复合体 (NTC),抑制 Notch 靶基因转录,具有抗肿瘤活性。 | |||
T3075 |
FLI-06
FLI 06 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
FLI-06 是一种 Notch 信号传导的抑制剂,EC50=2.3 μM。 | |||
T12246 |
CB-103
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
CB-103 是口服具有活性的蛋白相互作用抑制剂,靶向 NOTCH 转录复合体,具有抗肿瘤作用。 | |||
T6063 |
LY-411575
LY411575 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
LY-411575 是一种高效的γ-secretase 抑制剂,能够抑制 Aβ40 蛋白的产生,在膜中的 IC50 为 0.078 nM,在细胞中为 0.082 nM。 它还抑制 Notch 切割,IC50 为 0.39 nM。 | |||
T6249 |
Avagacestat
BMS-708163 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Avagacestat (BMS-708163) 是一种有效的γ-secretase 抑制剂,抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。 | |||
T3633 |
Crenigacestat
LY3039478 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Crenigacestat (LY3039478) 是一种口服具有活性的Notch 和γ-secretase 的抑制剂,其在多种肿瘤细胞中的IC50为 ∼1nM。 | |||
T6274 |
RO4929097
RG-4733 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
RO4929097 (RG-4733) 是 γ secretase 抑制剂,IC50=4 nM,能够抑制细胞内 Aβ40 (EC50:14 nM) 的产生和 Notch (EC50:5 nM) 活性。 | |||
T6125 |
Semagacestat
LY450139,塞美司他 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Semagacestat (LY450139) 是一种γ-secretase 抑制剂,抑制β-amyloid(Aβ42),Aβ38和Aβ40,IC50分别为 10.9,12 和 12.1 nM,可用于研究阿尔茨海默病。 | |||
T13410 |
ZLDI-8
|
Apoptosis; Phosphatase; Gamma-secretase; Immunology/Inflammation related | Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience; Proteases/Proteasome; Stem Cells |
ZLDI-8 是 Notch 激活/裂解酶 ADAM-17 的抑制剂,可抑制 Notch 蛋白裂解,并降低促存活/抗凋亡和上皮-间质转化相关蛋白的表达。它还是竞争性不可逆酪氨酸磷酸酶抑制剂,以IC50为 5.32 μM 抑制 MHCC97-H 细胞的生长。 | |||
T6202 |
DAPT
LY-374973,GSI-IX |
Apoptosis; Beta Amyloid; Gamma-secretase; Autophagy | Apoptosis; Autophagy; Neuroscience; Proteases/Proteasome; Stem Cells |
DAPT (LY-374973) 是一种 γ 分泌酶抑制剂,抑制总 Aβ 和 Aβ42 (IC50=115/200 nM),具有口服活性。DAPT 也是一种 Notch 抑制剂。DAPT 可以诱导细胞分化、诱导细胞自噬和凋亡。 | |||
T6135 |
YO-01027
gamma-Secretase Inhibitor XX,Dibenzazepine,DBZ,二苯并氮卓 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
YO-01027 (DBZ) 是一种高效的 γ-分泌酶抑制剂,能够裂解 Notch (IC50:2.92 nM) 和 APPL (IC50:2.64 nM)。 | |||
T6935 |
Nirogacestat
PF-03084014,PF-3084014,PF03084014,PF 03084014 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
Nirogacestat (PF 03084014) 是一种具有口服活性的,可逆的,非竞争性的,选择性γ-secretase 抑制剂,IC50为 6.2 nM。它抑制 Notch 信号通路,可研究 Notch 受体依赖性肿瘤。 | |||
T22678 |
3,5-Bis(4-nitrophenoxy)benzoic acid
3,5-二(4-硝基苯氧基)苯甲酸,Compound W |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
3,5-Bis(4-nitrophenoxy)benzoic acid (Compound W) 是 γ-secretase 抑制剂。它导致 Aβ42 和 notch-1 Aβ-like peptide 25 (Nβ25) 的释放水平降低。它是母体血清中 3,3’-diiodothyronine sulfate (T2S) 的交叉反应物质,可作为胎儿甲状腺功能减退的标志物。 | |||
T1602 |
Valproic acid sodium salt
丙戊酸钠,Sodium Valproate |
Mitophagy; Gamma-secretase; HIV Protease; GABA Receptor; HDAC; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells |
Valproic acid sodium salt (Sodium Valproate) 是一种HDAC 抑制剂,可抑制HDAC1的活性,诱导HDAC2的降解。它激活Notch1信号并抑制小细胞肺癌细胞的增殖。它可研究癫痫、偏头痛和双相情感障碍等。 | |||
T6474 |
Divalproex Sodium
Valproate semisodium,Epival,双丙戊酸钠 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Divalproex Sodium (Valproate semisodium) 结合并抑制 γ-氨基丁酸 (GABA) 转氨酶,其抗惊厥活性可通过增加 GABA 脑浓度和抑制分解 GABA 或阻止 GABA 再摄取到神经胶质和神经末梢的酶来发挥。它也是一种 HDAC 抑制剂。由丙戊酸钠和丙戊酸组成,具有抗惊厥和抗癫痫活性。 Divalproex 还可以通过抑制电压敏感的钠通道来抑制重复的神经元放电。 | |||
TP1540 |
Jagged-1 (188-204)
Jagged-1 188-204 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Jagged-1 (188-204) 是 JAG-1 蛋白的一个片段。其中 JAG-1 能够诱导单核细胞衍生的人树突状细胞成熟,是一种在培养的和原发性多发性骨髓瘤细胞中高度表达的 Notch 配体。 | |||
T3521 |
γ-Secretase-IN-1
Compound E |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
γ-Secretase-IN-1 是一种高效的 γ-secretase 抑制剂,对T-47D 细胞显示部分抗增殖活性且抑制 β-amyloid(40),β-amyloid(42),和Notch γ-分泌酶裂解。 | |||
T14680 |
BMS-906024
Osugacestat,AL-101,BM-0018 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
BMS-906024 (Osugacestat) 是一种可口服且具有选择性的γ 分泌酶抑制剂,是一种小分子 Notch 抑制剂。BMS-906024 对多种人类癌症异种移植具有广谱抗肿瘤活性。BMS-906024 可阻止所有四种 Notch 受体的激活,对 Notch1、-2、-3 和 -4 受体的 IC50 分别为 1.6、0.7、3.4 和 2.9 nM。 | |||
T31987 |
Gossypolone
|
Wnt/beta-catenin; Gamma-secretase | Cytoskeletal Signaling; Neuroscience; Proteases/Proteasome; Stem Cells |
Gossypolone 是一种棉酚主要代谢物。 Gossypolone 减少 Notch/Wnt 信号并诱导细胞凋亡。 | |||
T9015 |
LY900009
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
LY900009 是一种通过选择性抑制 γ-分泌酶蛋白来抑制 Notch 信号传导的小分子抑制剂。 | |||
T21890 |
JLK6
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
JLK-6 是一种γ分泌酶抑制剂,选择性作用于 HEK293细胞的淀粉样β前体蛋白(APP)的γ-分泌酶裂解 APP,抑制 Aβ的生成,但对不 Notch 受体的裂解无影响。 | |||
T35566 |
RBPJ Inhibitor-1
RIN1 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
RBPJ Inhibitor-1 (RIN1)是一个 RBPJ 抑制剂,它能阻断 RBPJ 与 SHARP 的功能性相互作用。RBPJ Inhibitor-1可抑制依赖于 NOTCH 的肿瘤细胞增殖。 | |||
T24159 |
IHR-1
IHR 1 |
Smo | Stem Cells |
IHR-1 是一种Smo 拮抗剂,不能透过细胞膜。 | |||
T76788 |
Demcizumab
OMP 21M18 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Demcizumab (OMP 21M18) 是一种抗 DLL4 单克隆抗体。Demcizumab 是一种有效的 Notch 通路抑制剂。Demcizumab 在多种癌症模型中无论使单独还联合化疗试剂使用都是有效的。 | |||
T11718 |
JI051
JI-051 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
JI051 具有抗肿瘤作用,能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用,通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞,抑制HEK293 细胞和胰腺癌细胞增殖。 | |||
TP1293 |
Jagged-1 (188-204) TFA(219127-21-6 free base)
Jagged-1 (188-204) TFA |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Jagged-1 (188-204) TFA(219127-21-6 free base) 是 JAG-1 蛋白的一个片段。 JAG-1 是 Notch 配体,是一种在皮肤中表达最明显的肽。 JAG-1 诱导表皮成熟。将淹没的角质形成细胞单层暴露于钙浓度升高的 JAG-1 会产生具有 loricrin 表达和 NF-alphaB 激活的分层。 | |||
T12277 |
NVS-ZP7-4
|
Others | Others |
NVS-ZP7-4 是一种能探测内质网锌水平影响的化学分子,是一种锌转运体 SLC39A7(ZIP7)的抑制剂,研究ZIP7 作为Notch 通路中的一种新的药物节点。 | |||
T2003 |
ISX-9
Isoxazole 9,Isoxazole 9 (ISX-9) |
Calcium Channel; Wnt/beta-catenin | Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells |
ISX-9 (Isoxazole 9) 是一种神经干细胞分化的有效诱导剂,可诱导 Notch 激活的心外膜衍生细胞(NEC) 的心肌分化。它可通过电压门控的 Ca2+通道和 NMDA 受体来激活 Ca2+流入,并增加 NeuroD 表达。 | |||
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。 | |||
T15184 |
E 2012
(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亚苄基]哌啶-2-酮 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
E 2012 是一种γ 分泌酶调节剂,不会影响 Notch 加工,在胆固醇生物合成的末步抑制 3β-羟基固醇 Δ24-还原酶。它能够减少淀粉样蛋白 β-42 减少阿兹海默氏病,并在大鼠多次重复给药后诱发白内障。 | |||
TP2117 |
SAHM1
|
||
Notch pathway inhibitor - stabilized hydrocarbon-stapled alpha helical peptide. Targets the protein-protein interface and prevents Notch complex assembly. | |||
T76054 |
SAHM1 TFA
|
||
SAHM1 TFA is a chemical compound that acts as a Notch pathway inhibitor by stabilizing a hydrocarbon-stapled alpha helical peptide. It specifically targets the protein-protein interface, effectively preventing the assembly of the Notch complex. | |||
T35546 | Yhhu 3792 | ||
Notch signaling pathway activator; enhances the self-renewal capability of neural stem cells (NSCs) via Notch signaling pathway activation in vitro and in vivo. Promotes the expression of Notch target genes, Hes3 and Hes5. Expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) after chronic administration in mice. Increases the spatial and episodic memory in mice. | |||
T24210 |
JNJ-40418677
|
||
JNJ-40418677 is a γ-secretase modulator that selectively blocks γ-site cleavage of the APP without affecting the processing of Notch. | |||
T13917 |
tCFA15
|
Others | Others |
tCFA15, a trimethyl cyclohexenonic long-chain fatty alcohol with a 15-carbon atom side chain, may regulate Notch signaling and promote neuronal differentiation. | |||
T14683 | BMS-983970 | Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers. | |||
T17281 |
Z-Ile-Leu-aldehyde
Z-IL-CHO,GSI-XII,γ-Secretase inhibitor XII |
Others | Others |
Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch. | |||
T76023 |
Jagged-1 (188-204) (TFA)
|
||
Jagged-1 (188-204) TFA 是 JAG-1 蛋白的一个片段,具有Notch 激动剂活性。JAG-1 是一种在培养的和原发性多发性骨髓瘤 (MM) 细胞中高度表达的Notch 配体。JAG-1 诱导单核细胞衍生的人树突状细胞成熟。 | |||
T73485 | BT-GSI | ||
BT-GSI 是一种 γ-分泌酶抑制剂 (GSI) 和骨靶向 Notch 抑制剂。BT-GSI 具有双重抗骨髓瘤和抗吸收特性,可用于多发性骨髓瘤及相关骨病的研究。BT-GSI 抑制肿瘤生长和溶骨性疾病进展。 | |||
T12634 |
(R)-NVS-ZP7-4
|
Others | Others |
(R)-NVS-ZP7-4 是 NVS-ZP7-4 的 R 型异构体。 NVS-ZP7-4 是一个报道用于探测内质网锌水平影响的化学分子,是一种锌转运体 SLC39A7(ZIP7)的抑制剂,并研究 ZIP7 作为 Notch 通路中的一种新的可成药节点。 | |||
T61930 | Yhhu-3792 | ||
Yhhu-3792 激活 Notch 信号通路并促进 Hes3 和 Hes5 的表达。Yhhu-3792 增强神经干细胞 (NSC) 的自我更新能力,扩大了 NSC 池并促进了小鼠海马齿状回部分 (DG) 的内源性神经形成。Yhhu-3792 可提高小鼠的情景和空间记忆能力。 Yhhu-3792 在记忆障碍相关 DG 功能障碍中具有研究潜力。 | |||
T68980 | MRK003 | ||
MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel... | |||
T80615 |
Enoticumab
REGN421 |
||
Enoticumab(REGN421,SAR153192)是一种针对人类Dll4的IgG1κ类型抗体。DLL4为Notch信号通路中的关键配体,其功能通过巨胞饮作用依赖的非转录调控机制影响长链脂肪酸的摄取。该抗体在卵巢癌异种移植模型中展示出明确的体内活性,其中EGN421(2.5mg/kg,周剂量)在小鼠皮下TOV-112D及腹膜内A2780人类肿瘤异种移植模型中实现了分别达到86%和83%的肿瘤生长抑制效果。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TWS2045 |
Bruceine D
鸦胆子素D,鸦胆子苦素D |
Apoptosis; Antiviral; Gamma-secretase; Parasite | Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells |
Bruceine D 是Notch 抑制剂,有抗癌活性,诱导几种人癌细胞调亡。它是一种有效的植物性昆虫拒食剂,有显著的系统特性和抑制害虫生长的作用。它具有较强的驱虫活性,抑制D. intermedius 的 EC50值为 0.57 mg/L。 | |||
T3399 |
Psoralidin
|
Others; Estrogen/progestogen Receptor; Reactive Oxygen Species; Lipoxygenase; Gamma-secretase; Akt; COX; Antibacterial | Cytoskeletal Signaling; Endocrinology/Hormones; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells |
Psoralidin 是COX-2和5-LOX 的抑制剂,有抗癌,抗菌和抗炎作用。它显著下调NOTCH1信号传导,还极大地诱导活化氧产生。 | |||
T4S1990 |
Carvacrol
香荆芥酚,Karvakrol,O-Thymol,cymophenol,香芹酚 |
Apoptosis; Others; Gamma-secretase; Endogenous Metabolite; Antifungal | Apoptosis; Metabolism; Microbiology/Virology; Neuroscience; Others; Proteases/Proteasome; Stem Cells |
Carvacrol (O-Thymol) 是唇形科植物中的一种单萜酚类天然产物,具有镇痛、抗焦虑、抗抑郁、抗氧化、抗炎和抗癌作用。 | |||
T2842 |
Tangeretin
NSC53909,Tangeritin,NSC618905,桔皮素 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
Tangeretin (NSC-618905) 是一种来自柑橘类水果果皮的类黄酮,是一种Notch-1抑制剂,具有抗炎,保护神经等作用。 | |||
T7064 |
Valproic Acid
Sodium valproate,2-Propylpentanoic Acid,丙戊酸,VPA,Depakine,2-Propylvaleric Acid |
Mitophagy; Gamma-secretase; HIV Protease; GABA Receptor; Sodium Channel; HDAC; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells |
Valproic Acid (2-Propylpentanoic Acid) 是一种 HDAC 抑制剂,可抑制 HDAC1 活性,诱导 HDAC2 降解,具有口服活性。Valproic Acid 可以用于癫痫和躁郁症的研究。 | |||
T7982 |
3,6-Dihydroxyflavone
|
Others | Others |
3,6-Dihydroxyflavone 是一种抗癌剂。它能够提高细胞内氧化应激和脂质过氧化。它是能够根据剂量和时间依赖性地降低细胞活力,并活化半胱天冬酶级联、切割聚 (ADP-核糖) 聚合酶 (PARP) 诱导细胞凋亡。 | |||
T3426 |
Bacoside A
|
MMP; Others; TNF; Dopamine Receptor; NOS; ROS | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others; Proteases/Proteasome |
Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of i... |