gsk3β inhibitor 1

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。

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

GSK-3β inhibitor19 (compound 36) 作为一种有效的GSK-3β抑制剂，其IC50为70 nM，主要应用于抗炎及阿尔茨海默病的相关研究领域。

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。

(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。

GSK3β-IN-1 (compound 1) 是一款糖原合酶激酶-3β (GSK-3β) 抑制剂，其 IC50 为65 nM，适用于阿尔兹海默病研究。

Ro 31-8220 formic 是一种高效PKC抑制剂，其对PKCα、PKCβI、PKCβII、PKCγ、PKCε和大鼠大脑PKC的抑制IC50值分别为 5、24、14、27、24 和 23 nM。此外，Ro 31-8220 formic 还抑制 MAPKAP-K1b、MSK1、S6K1 和 GSK3β，IC50值分别为 3、8、15、38 nM。此化合物亦抑制 MKP-1 的表达，诱导 c-Jun 表达并激活 JNK，同时这些作用显示出不依赖于PKC的药理特性。

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks.References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019). YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks. References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019).

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

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].

APN/AKT-IN-1 is a potent dual inhibitor of aminopeptidase N (APN) and protein kinase B (AKT), exhibiting IC50 values of 0.21 μM and 0.27 μM for APN and AKT inhibition, respectively. This compound effectively suppresses the phosphorylation of glycogen synthase kinase 3 beta (GSK3β), which serves as an intracellular substrate of AKT [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)。

GNF2133 hydrochloride 是一种选择性的、有效的、口服具有活力的 DYRK1A 抑制剂，能够作用于 DYRK1A (IC50: 0.0062 μM) 和 GSK3β (IC50> 50 μM)。GNF2133 hydrochloride 对大鼠和人原代 β 细胞表现出良好的增殖能力和功效。GNF2133 hydrochloride 明显提升葡萄糖处理能力，增多胰岛素分泌。GNF2133 hydrochloride 具有潜力进行 1 型糖尿病的研究。

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。

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

PIM1-IN-4（Compound 8）为PIM1高效抑制剂，对SGK-1、PKA、CaMK-1、GSK3β及MSK1五种酶亦展现出显著抑制效应，表现出其在癌症疾病研究中的应用潜力。

hAChE-IN-6（化合物51）是一种能够穿透血脑屏障的AChE抑制剂，具有0.16 μM的IC50。该化合物同时对hBuChE与GSK3β显示出抑制活性，其IC50分别为0.69 μM和0.26 μM。hAChE-IN-6亦能抑制tau蛋白与Aβ1-42的自聚集，适用于阿尔茨海默病（AD）的相关研究。

hAChE-IN-5（化合物49）是一种同时针对hAChE和hBuChE的有效抑制剂，其IC50值均为0.17 μM。此外，hAChE-IN-5对GSK3β同样展现出良好的抑制活性，IC50值为0.21 μM。作为tau蛋白聚集和Aβ1-42自聚集的抑制剂，hAChE-IN-5能够结合PAS，进而阻止Aβ依赖的神经毒性。其能穿透血脑屏障（BBB），显示出成为多靶点抗阿尔茨海默病药物研究的潜力。

(rel)-Tivantinib (Compound 9) 是一种有效并具有高选择性的 c-MET 受体酪氨酸激酶抑制剂，同时针对 GSK3α 和 GSK3β 这两个新靶点，这在非小细胞肺癌 (NSCLC) 的细胞机制中扮演着关键角色。

“(3S,4S)-Tivantinib 为高效、高选择性c-MET受体酪氨酸激酶抑制剂，同时作用于新靶点GSK3α和GSK3β，这些在非小细胞肺癌(NSCLC)的细胞机制中具有关键作用。”

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。