GSK-3β 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S6085 KY19382 (A3051)

KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively.

Selective GSK3β, IC50: 10 nM
S8696 2-D08

2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

Selective GSK3β, IC50: 11 nM
S1590 TWS119

TWS119是一种GSK-3β抑制剂,在无细胞试验中IC50为30 nM;能够诱导神经细胞的分化,并且有助于干细胞生物学的研究。

Selective GSK-3β, IC50: 30 nM
S7435 AR-A014418

AR-A014418是一种ATP竞争性和选择性的GSK3β抑制剂,无细胞试验中IC50Ki为104 nM和38 nM,而对被测试的其他26种激酶没有显著抑制作用。

Selective GSK-3β, Ki: 38 nM; GSK-3β, Ki: 38 nM
S7566 IM-12

IM-12是一种选择性的GSK-3β抑制剂,其IC50为53 nM,增强了Wnt信号通路。

Selective GSK-3β, IC50: 53 nM
S2823 Tideglusib (NP031112)

Tideglusib是一种不可逆的,非ATP竞争性的GSK-3β抑制剂,无细胞试验中IC50为60 nM,不能抑制位于活性位点的同源于 Cys-199的 Cys激酶。Phase 2。

Selective GSK-3β, IC50: 60 nM
S1524 AT7519

AT7519是多种CDK抑制剂,作用于CDK1, 2, 4, 6和9时,IC50为10-210 nM,对CDK3作用效果稍弱,对CDK7几乎没有抑制活性。Phase 2。

Selective GSK-3β, IC50: 89 nM
S2386 Indirubin (NSC 105327)

Indirubin是一种有效的细胞周期依赖性激酶和GSK-3β抑制剂,IC50约为 5 μM和0.6 μM。

Selective GSK-3β, IC50: 0.6 μM
S2926 TDZD-8

TDZD-8是一种非ATP竞争性GSK-3β抑制剂,IC50为2 μM;对CDK1, casein kinase II, PKA和PKC具有最低限度的抑制效果。

Selective GSK-3β, IC50: 2 μM
S0765 MAZ51

MAZ51 is a potent and selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase with antitumor activity. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 blocks proliferation and induces apopto䲧甿Ỵ畀㧀甾膉病璞蹸ੲᝠŐੲĀ

Selective
S7954 CP21R7 (CP21)

CP21R7(CP21)是一种有效的、选择性的GSK-3β抑制剂,能有效激活经典Wnt信号通路。

Selective
S3238 Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 exp

Selective
S2745 CHIR-98014

CHIR-98014是一种有效的GSK-3α/β抑制剂,无细胞试验中IC50为0.65 nM/0.58 nM,作用于GSK-3比作用于其最密切的同源物Cdc2 和 ERK2选择性高。

Pan GSK-3β, IC50: 0.58 nM
S7063 LY2090314

LY2090314是一种有效的GSK-3抑制剂,作用于GSK-3α/βIC50为1.5 nM/0.9 nM;可提高以铂类为基础的化疗方案的疗效。LY2090314对GSK3具有高选择性,对其他大多数激酶的抑制活性低。

Pan GSK-3β, IC50: 0.9 nM
S0354 Alsterpaullone

Alsterpaullone is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50 of both 4 nM. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

Pan GSK-3β, IC50: 4 nM
S1263 CHIR-99021 (CT99021)

CHIR-99021 (CT99021)是一种GSK-3αGSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性,对GSK-3β的选择性是对CDKs选择性的350倍。

Pan GSK-3β, IC50: 6.7 nM
S2924 CHIR-99021 (CT99021) HCl

CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂,IC50为10 nM/6.7 nM。 其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。

Pan GSK-3β, IC50: 6.7 nM
S7915 BIO-acetoxime

BIO-acetoxime是一种有效的双重GSK3α/β抑制剂,IC50为10 nM,选择性比 CDK5/p25,CDK2/cyclin A 和 CDK1/cyclin B高240倍以上。

Pan GSK-3β, IC50: 10 nM
S7193 1-Azakenpaullone

1-Azakenpaullone是一种高度选择性GSK-3β抑制剂,IC50为18 nM, 其选择性高于CDK1/cyclin B 和 CDK5/p25 100倍。

Pan GSK-3β, IC50: 18 nM
S7145 AZD1080

AZD1080是一种口服生物有效的,选择性的,可透过大脑的GSK3抑制剂,抑制人类GSK3α和GSK3β,Ki分别为6.9 nM和31 nM,比作用于CDK2, CDK5, CDK1和Erk2选择性高14倍以上。

Pan GSK-3β, IC50: 31 nM
S1075 SB216763

SB216763是一种有效的,选择性GSK-3α抑制剂,IC50为34.3 nM;对GSK-3β具有同样的抑制作用。

Pan GSK-3β, IC50: ~34.3 nM
S2729 SB415286

SB415286是一种有效的GSK3α抑制剂,IC50/Ki为78 nM/31 nM,也等效抑制GSK-3β。

Pan GSK-3β, IC50: ~78 nM
S9638 BRD0705

BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).

Pan GSK3β, Kd: 515 nM