65
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21956 |
GSK3β inhibitor II
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
GSK3β inhibitor II 是 GSK3β 的抑制剂。GSK3β inhibitor II 可用于研究阿尔茨海默病 (AD)。 | |||
T36088 |
GSK3β Inhibitor XI
GSK3β Inhibitor XI |
Others | Others |
GSK3β Inhibitor XI 具有GSK3β抑制作用。 | |||
T35556 |
GSK-3β inhibitor 8
GSK3β Inhibitor XVIII |
GSK-3; Wnt/beta-catenin | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII)是具有有效和选择性的 GSK-3β 抑制剂 ,IC50值为 64 nM。GSK-3β inhibitor 8 是一种噻吩嘧啶衍生物,负调控 Wnt 信号通路,刺激 β 细胞增殖。 | |||
T63851 |
CDK9/10/GSK3β-IN-1
|
Others | Others |
CDK9/10/GSK3β-IN-1 是一种激酶抑制剂 (Flavopiridol 类似物),能有效抑制 HsGSK3β、HsCDK9/CyclinT、HsCDK5/p25 和 HsCDK2/CyclinA,其 IC50 值分别为 59 nM、64 nM、1.093 μM 和 1.725 μM。CDK9/10/GSK3β-IN-1 表现出相当或高于 Flavopiridol 的抗癌细胞活性,在体外对多达七种癌细胞系表现出高抗增殖活性。 | |||
T62719 |
AChE/BACE1/GSK3β-IN-1
|
Others | Others |
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)。 | |||
T73270 |
GSK3-IN-2
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
GSK3-IN-2 是一种有效的 GSK3抑制剂。 | |||
T35554 |
GSK-3β inhibitor 3
|
Apoptosis; GSK-3 | Apoptosis; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-3β inhibitor 3 是一种糖原合成酶激酶 3β(GSK-3β)共价抑制剂 ( IC50 : 6.6 μM),具有强效性、选择性和不可逆性。GSK-3β inhibitor 3 可用于研究急性早幼粒细胞白血病。 | |||
T2423 |
P7C3-A20
|
Others | Others |
P7C3-A20 是促神经原性和神经保护活性的 P7C3 衍生物。它具有抗抑郁活性,能够透过血脑屏障,并可用于研究脑损伤。 | |||
T39341 |
FCPR03
|
PDE | Metabolism |
FCPR03 是一种特异性磷酸二酯酶 4 (PDE4) 抑制剂,对 PDE4B1、PDE4D7 和 PDE4 催化结构域的 IC50 分别为 31 nM、47 nM 和 60 nM。 FCPR03 具有神经保护、抗炎和抗抑郁样作用。 | |||
T22012 |
7BIO
|
FLT; DYRK; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
7BIO 是靛玉红的衍生物,抑制细胞周期蛋白依赖性激酶5 和糖原合酶激酶-3β。它抑制 Aβ 寡聚体诱导的神经炎症、突触损伤、tau 过度磷酸化、星形胶质细胞和小胶质细胞的活化,并减轻 Aβ 寡聚体诱导的小鼠认知障碍。 | |||
T11467 |
GSK-3β inhibitor 1
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
GSK-3β inhibitor 1 是一种糖原合成酶激酶 3β (GSK-3β)的抑制剂,其 IC50=4.9 nM,可用于糖尿病的研究。 | |||
T11471 |
GSK-3β inhibitor 2
GSK-3β 抑制剂 2,5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy- |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) 是一种特异性的 GSK-3β 抑制剂 (IC50 = 1.1 nM)。 GSK-3β inhibitor 2 可用于阿尔茨海默病的研究。 | |||
T8376 |
PKCβ inhibitor 1
KUN79359 |
Apoptosis; PKC | Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling |
PKCβ inhibitor 1 (KUN79359) 是一种 ATP 竞争性和选择性PKCβ抑制剂,对人 PKCβ1 和 PKCβ2 的IC50分别为 21 和 5 nM。 | |||
T8605 |
GS87
4-[5-[[(3-Phenyl-1,2,4-oxadiazol-5-yl)methyl]thio]-1,3,4-oxadiazol-2-yl]pyridine |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
GS87 是 GSK3(糖原合酶激酶 3)的高度特异性抑制剂,可诱导 AML 细胞的广泛分化。 | |||
T9178 |
(E/Z)-GSK-3β inhibitor 1
GSK-3β inhibitor 1 |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
(E/Z)-GSK-3β inhibitor 1 是 (E)-GSK-3β inhibitor 1 和 (Z)-GSK-3β inhibitor 1 的消旋体。它是一种糖原合成酶激酶 3β (GSK-3β)的抑制剂,可其对 GSK-3β 的 IC50=4.9 nM,用于糖尿病的研究。 | |||
T76088 |
GSK3 Substrate, α, β subunit
|
||
GSK3 Substrate, α, β subunit 是糖原合酶激酶-3 (GSK-3) 的肽底物,可用于测量GSK-3活性。 | |||
T1764 |
Adezmapimod
PB 203580,4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)-1H-咪唑,RWJ 64809,SB203580 |
Mitophagy; p38 MAPK; Autophagy | Autophagy; MAPK |
Adezmapimod (SB 203580) 是一种 p38 MAPK 抑制剂 (IC50=0.3-0.5 μM),具有选择性和 ATP 竞争性。Adezmapimod 具有自噬和线粒体自噬的激活活性。Adezmapimod 显示出比 PKB、LCK 和 GSK-3β 高 100 倍以上的选择性。 | |||
T1830 |
BX795
|
IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy | Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
BX795 是一种选择性PDK1抑制剂,也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1,Akt,PKCδ 和 GSK3β 的磷酸化,可调节自噬。 | |||
T2052 |
KY02111
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
KY02111 是典型的 WNT 信号抑制剂,能够促进人多潜能干细胞向心肌细胞分化,可用于研究人类心肌细胞再生。 | |||
T17019 |
TCS 21311
NIBR3049 |
GSK-3; JAK; PKC | Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells |
TCS 21311 (NIBR3049) 是一种高选择性JAK3抑制剂,IC50为 8 nM,它的选择性是 JAK1、JAK2 和 TYK2 的100倍以上,还抑制PKCα、PKCθ和GSK3β,IC50值分别为 13、68 和 3 nM。 | |||
T9025 |
KY19382
2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382,A3051 |
Others; GSK-3; Wnt/beta-catenin | Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling; Stem Cells |
KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) 是一种具有口服活性的 CXXC5-DVL (IC50:19 nM) 和 GSK3β (IC50:10 nM) 的双重抑制剂。它通过对 CXXC5-DVL 相互作用和 GSK3β 活性的抑制作用激活 Wnt/β-catenin 信号传导。它可用于高脂饮食诱发的代谢性疾病的研究。 | |||
T11447 |
GNF4877
|
GSK-3; DYRK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
GNF4877 是一种 DYRK1A (IC50:6 nM) 和 GSK3β (IC50:16 nM) 抑制剂。 它导致激活 T 细胞核因子核输出的阻断和 β 细胞增殖细胞增加。 | |||
T1881 |
AR-A014418
AR 0133418,GSK-3beta Inhibitor VIII,AR 014418,GSK 3β inhibitor VIII |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
AR-A014418 (GSK 3β inhibitor VIII) 是选择性的,ATP 竞争性的 GSK3β抑制剂 ,其 IC50=104 nM,Ki=38 nM。 | |||
T5600 |
Darovasertib
LXS196 |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Darovasertib (LXS196) 是一种有效的、选择性的和具有口服活性的蛋白激酶C(PKC) 抑制剂,有用于葡萄膜黑素瘤的研究潜力,对 PKCα、PKCθ 和 GSK3β 的 IC50值分别为 1.9、0.4 和 3.1 μM。 | |||
T23601 |
ABC1183
ABC 1183,ABC-1183 |
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
ABC1183是一种抑制GSK3α, GSK3β和CDK9的新型二氨基噻唑。ABC1183通过诱导G2/M 阻滞和改变GSK3、糖原合成酶、β-catenin 磷酸化和MCL1表达降低细胞存活率来抑制多种癌细胞株的生长,并具有口服活性。 | |||
T6643 |
Ro 31-8220 Mesylate
Ro 31-8220 methanesulfonate,Bisindolylmaleimide IX,Bisindolylmaleimide IX mesylate |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) 是PKC 抑制剂,对 PKCα、PKCβI、PKCβII、PKCγ、PKCε 和大鼠大脑 PKC 的IC50值为 5、24、14、27、24 和 23 nM。它还抑制 MAPKAP-K1b、MSK1、S6K1 和 GSK3β,IC50为3、8、15 和 38 nM。 | |||
T6435 |
CCT129202
2-[4-[6-氯-2-(4-二甲基氨基苯基)-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]-N-(噻唑-2-基)乙酰胺 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
CCT129202 是一种 ATP 竞争性泛极光激酶抑制剂,作用于 Aurora A、Aurora B 和 Aurora C,IC50 分别为 0.042 μM、0.198 μM 和 0.227 μM。 | |||
T14034 |
3CAI
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
3CAI 是特异性的AKT1和AKT2抑制剂。 | |||
T5200 |
Indirubin-3'-monoxime
靛玉红-3' -单肟,Indirubin-3'-oxime |
GSK-3; Lipoxygenase; CDK | Cell Cycle/Checkpoint; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
Indirubin-3'-monoxime (Indirubin-3'-oxime) 是一种有效的 GSK3β 抑制剂,IC50值为 22 nM。它对 CDK5/p25、CDK1/cyclin B 和CDk2/cyclin E 也有作用,IC50值分别为 100、180 和 250 nM。 | |||
T10606 |
BRD0705
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
BRD0705 是一种具有旁系选择性的、口服具有活性的GSK3α抑制剂,其 IC50=66 nM,Kd=4.8 μM。 它与 GSK3β (其 IC50=515 nM) 相比,对GSK3α的选择性更高 (8 倍)。它可用于研究急性髓细胞性白血病。 | |||
T11573 |
HPN-01
|
Others | Others |
HPN-01 is a selective IKK inhibitor (pIC50s: 6.4, 7.0, and <4.8 for IKK-α, IKK-β, and IKK-ε). HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, ErbB2, EGFR, GSK3β, Src, PLK1, and VEGFR-2. | |||
T12901 |
SHIP2-IN-1
|
Phosphatase | Metabolism |
SHIP2-IN-1 是一种 SHIP2 抑制剂,IC50=2 µM。它能够使 GSK3β 的 Ser9 位点磷酸化,抑制 GSK3β 的活化。它可用于研究阿尔滋海默症。 | |||
T1953 |
L-779450
L 779450 |
Raf; Autophagy | Autophagy; MAPK |
L-779450 是一种有效的 ATP 竞争性 Raf 激酶抑制剂,IC50为 10 nM,Kd 为 2.4 nM。 | |||
T3684 |
CP21R7
CP21 |
GSK-3; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
CP21R7 (CP21) 是一种 GSK-3β抑制剂,其 IC50=1.8 nM。它也是一种 PKCα抑制剂,其 IC50=1900 nM。 | |||
T10608 |
BRD5648
(R)-BRD0705 |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
BRD5648 是 BRD0705 的 阴性对照,BRD0705 是旁系选择性和口服有效的 GSK3α 抑制剂,Kd为 4.8 μM,IC50为 66 nM。与 GSK3β (IC50为 515 nM) 相比,BRD0705 对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病。 | |||
T1741 |
AZD1080
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
AZD1080 是一种选择性GSK3抑制剂。它抑制重组人GSK3α和GSK3β,pKi(IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。 | |||
T12664 |
(Rac)-BRD0705
|
Others | Others |
(Rac)-BRD0705 是 BRD0705 的活性较低的外消旋体。 BRD0705 是一种有效的特异性 GSK3α 抑制剂。 | |||
T2506 |
AZD-5438
AZD5438 |
CDK | Cell Cycle/Checkpoint |
AZD-5438 有效抑制 CDK1,CDK2,CDK9,IC50值分别为 16 nM, 6 nM, 20 nM,但它对 GSK3β,CDK5,CDK6 的抑制作用较弱。 | |||
T25650 |
LDN-193665
LDN 193665,LDN193665 |
Others | Others |
LDN-193665 is a potent inhibitor of tau kinase. It acts by targeting CDK5/p25 and GSK3β. | |||
T69904 |
Dihydronarwedine
|
Others | Others |
Dihydronarwedine is a metabolite of Galanthamine, an inhibitor of glycogen synthase kinase 3β (GSK3β) | |||
T61578 |
BRD3731
|
Others | Others |
BRD3731 is a selective inhibitor of GSK3β, demonstrating an IC50 value of 15 nM for GSK3β and 215 nM for GSK3α. Due to its inhibitory properties, BRD3731 holds promise for investigating various medical conditions, including post-traumatic stress disorder (PTSD), psychiatric disorders, diabetes, and neurodegenerative disorders [1]. | |||
T74033 |
6-Me-ATP
|
Others | Others |
6-Me-ATP(N6-Methyl-ATP)为ATP的N6修饰衍生物。该化合物与GSK3β结合亲和力显著,能有效作为GSK3β催化底物肽磷酸化的磷酸基团供体。 | |||
T39457 |
(R)-BRD3731
(R)-BRD3731 |
Others | Others |
(R)-BRD3731, a GSK3 inhibitor, specifically compound example 273. It exhibits inhibitory activity with respective IC50 values of 1.05 μM for GSK3β and 6.7 μM for GSK3α. | |||
T3074L |
CHIR98014 HCl (252935-94-7 free base)
CT-98014,CHIR-98014 hydrochloride,CHIR-98014,CHIR98014 HCl,CHIR98014,CHIR 98014 |
Others | Others |
CHIR98014 is a reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC50s: 0.65 and 0.58 nM). Through its effects on GSK3, CHIR98014 stimulates glycogen synthase in cells (EC50: 106 nM), potentiates insulin-dependent glucose transport in isolated musc | |||
TP2293 |
TCS 183
|
Others | Others |
TCS 183 可以模拟 GSK3β 上的 Akt 磷酸化位点,阻止 LTD 的调节。 | |||
T74034 |
6-Me-ATP trisodium
|
Others | Others |
6-Me-ATP trisodium (N6-Methyl-ATP) 是N6-修饰的ATP衍生物,展现对GSK3良好的结合亲和力,可作为GSK3β磷酸化底物肽的磷酸基团供体。 | |||
T84913 |
PT-65
|
Others | Others |
PT-65是一种高效且具选择性的GSK3降解剂,对SH-SY5Y细胞中的GSK3α(DC50=28.3 nM)和GSK3β(DC50=34.2 nM)表现出最强的降解活性。该化合物主要用于研究阿尔茨海默病。 | |||
T30266 |
AZD8926
AZD 8926,AZD-8926 |
Others | Others |
AZD8926 is a potent and selective inhibitor of GSK3β(glycogen synthase kinase-3β). AZD8926 is potential for treating Alzheimer’s disease (AD), schizophrenia, and chronic as well as acute neurodegenerative diseases. | |||
T66175 |
Ceftriaxone Sodium
|
GSK-3; Antibiotic; Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells |
Ceftriaxone Sodium 是一种广谱 β-内酰胺类三代头孢菌素类抗生素 (antibiotic),具有抗炎、抗肿瘤、抗菌和抗氧化活性。Ceftriaxone Sodium 是一种共价 GSK3β和 Aurora B 抑制剂, 可用于研究败血症和感染性心内膜炎。 | |||
T40792 |
Cu(II)GTSM
|
Others | Others |
Cu(II)GTSM, a cell-permeable copper-complex, effectively inhibits GSK3β and shows inhibitory effects against Amyloid-β oligomers (AβOs) while reducing tau phosphorylation. Additionally, Cu(II)GTSM decreases the abundance of Amyloid-β trimers. With its potential as an anticancer and antimicrobial agent, Cu(II)GTSM exhibits promising therapeutic capabilities. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2P2810 |
Methyl Linoleate
Linoleic acid methyl ester,亚油酸甲酯,Telfairic Acid methyl ester |
Antioxidant | oxidation-reduction |
Methyl Linoleate (Telfairic Acid methyl ester) 是一种 Sageretia thea 果实的主要活性成分,能够下调小眼畸形相关转录因子和酪氨酸酶相关蛋白,是一种主要的抗黑色素生成化合物。 | |||
T6S1529 |
Cynarin
Cyclohexanecarboxylic acid, 1,3-bis[[3-(3,4-dihydroxyphenyl)-1-oxo-2-propen-1-yl]oxy]-4,5-dihydroxy-, (1R,3R,4S,5R)-,Cynarine,1,5-Dicaffeoylquinic acid,洋蓟素,金银花 |
Antioxidant; Antiviral; Influenza Virus; Reactive Oxygen Species | Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB; oxidation-reduction |
Cynarin (1,5-Dicaffeoylquinic acid) 是一种抗窒息剂,具有抗氧化、抗组胺和抗病毒等多种生物活性。 | |||
TN2091 |
Polygalacin D
|
Apoptosis; IAP | Apoptosis |
Polygalacin D 是从桔梗中分离的一种天然产物,具有抗癌和抗增殖特性。它通过 PI3K/Akt 途径诱导凋亡。它抑制 IAP 蛋白家族的表达,并通过抑制 GSK3β,Akt 的磷酸化和 PI3K 的表达来阻断 PI3K/Akt 途径。 | |||
TN6469 |
Biatractylolide
|
||
Biatractylolide has a neuroprotective effect on glutamate-induced injury in PC12 and SH-SY5Y cells through a mechanism of the PI3K-Akt-GSK3β-dependent pathways. The molecular mechanisms of inhibitory activities of biatractylolide on AChE are not only thro | |||
TN3319 |
9-Hydroxycanthin-6-one
|
Potassium Channel; GSK-3; Calcium Channel; Wnt/beta-catenin | Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α. | |||
TN2775 |
2-Methoxystypandrone
|
MMP; BCL; IκB/IKK; GSK-3; TNF; NOS; NF-κB; Wnt/beta-catenin; COX; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells |
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant |