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Search Results for " gsk3 "

Targets Recommended: GSK-3

71

抑制剂 & 化合物

2

天然产物

3

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T64366	GSK3-IN-4	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK3-IN-4是一种 GSK-3抑制剂，对 GSK-3α和 GSK-3β的IC50值为 0.101-1 μM。
T9987	GSK3-IN-1	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK3-IN-1是一种 GSK3B-糖原合酶激酶3β抑制剂。
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。
T73331	GSK3-IN-3	Mitophagy; GSK-3	Autophagy; PI3K/Akt/mTOR signaling; Stem Cells
	GSK3-IN-3 是一种线粒体自噬 (mitophagy) 诱导剂和GSK-3 抑制剂（IC50 ： 3.01 μM），可诱导帕金依赖性线粒体自噬。 GSK3-IN-3 具有非 ATP 和非底物竞争性，对 6-OHDA 有神经保护作用。
T24111	GSK3i XIII GSK3 inhibitor XIII,GSK3iXIII,GSK3i-XIII	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK3i XIII (GSK3 inhibitor XIII) 是ATP 竞争性GSK-3抑制剂(Ki: 24 nM)。
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)。
T11468	GSK-3 inhibitor 1	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK-3 inhibitor 1 is a GSK-3 inhibitor.
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。
T36088	GSK3β Inhibitor XI GSK3β Inhibitor XI
	GSK3β Inhibitor XI 具有GSK3β抑制作用。
T63851	CDK9/10/GSK3β-IN-1
	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
	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)。
T35555	GSK-3/CDK5/CDK2-IN-1 GSK-3/CDK5/CDK2-IN-1
	GSK-3/CDK5/CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].
T27478	GSK3987	Liver X Receptor	Metabolism
	GSK3987 是广谱LXRα/β激动剂，EC50分别为 50 nM 和 40 nM。GSK3987增加 ABCA1 和 SREBP-1c 蛋白的表达，诱导细胞甘油三酯的积累和胆固醇流出。
T15558	GSK319347A	IκB/IKK	NF-κB
	GSK319347A 是一种具有选择性和有效性的 TBK1 和 IKKε 的双重抑制剂，具有潜在的抗肿瘤活性，对 IKK2 活性有抑制作用，可用于研究膀胱癌和肺腺癌。
T77671	GSK3a-IN-38	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK3a-IN-38 是一种对GSK-3a有抑制作用的新型小分子化合物。
T27475	GSK356278 GSK-356278,GSK 356278	PDE	Metabolism
	GSK356278 是一种有效的特异性磷酸二酯酶 4 (PDE4) 抑制剂，对人 PDE4A、PDE4B 和 PDE4D 的 pIC50 分别为 8.6、8.8 和 8.7。 GSK356278 具有抗炎、抗焦虑和增强认知的作用。
T24109	GSK329 GSK 329,GSK-329	Others	Others
	GSK329 是一种有效的选择性 TNNI3 相互作用激酶 (TNNI3K) 抑制剂。 GSK329 在缺血/再灌注心脏损伤模型中表现出积极的心脏保护作用。
T15440	GSK376501A	PPAR	DNA Damage/DNA Repair; Metabolism
	GSK376501A 是一种具有选择性和有效性的的过氧化物酶体增殖物激活受体 γ (PPARγ) 调节剂，可用于研究 2 型糖尿病。
T1941	GSK3787	PPAR	DNA Damage/DNA Repair; Metabolism
	GSK3787 是选择性过氧化物酶体增殖物激活受体 δ (PPARδ) 的一种不可逆拮抗剂，pIC50为 6.6。
T5745	GSK3326595 EPZ015938	Histone Methyltransferase	Chromatin/Epigenetic
	GSK3326595 (EPZ015938) 是一种选择性可逆的蛋白精氨酸甲基转移酶 5 抑制剂，IC50为6.2 nM，具有广谱的抗增殖活性。
T7195	GSK369796 Dihydrochloride N-tert-butylisoquine	Potassium Channel; Parasite	Membrane transporter/Ion channel; Microbiology/Virology
	GSK369796 Dihydrochloride (N-tert-butylisoquine) 是一种抗疟药，可抑制 hERG 钾离子通道复极化，IC50值为 7.5 μM。
T15438	GSK3186899 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide,DDD-853651	Parasite	Microbiology/Virology
	GSK3186899 是 Cdc2 相关激酶 12 的抑制剂，对 L. donovani 的 EC50 为 1.4 μM。
T15437	GSK3145095	RIP kinase	Apoptosis; NF-κB
	GSK3145095 是一种口服有效的 RIPK1 抑制剂，IC50 为 5 nM，具有潜在的免疫调节活性和抗肿瘤活性。
T5491	GSK3179106	c-RET	Apoptosis; Tyrosine Kinase/Adaptors
	GSK3179106 是选择性的、具有口服活性的RET 激酶抑制剂，对人和大鼠 RET 的 IC50 分别为 0.4 nM 和 0.2 nM。它能够减轻炎症后和应激引起的内脏超敏反应，对肠易激综合征具有潜在的应用价值。
T6059	GSK343	Histone Methyltransferase; Autophagy	Autophagy; Chromatin/Epigenetic
	GSK343 是一种特异性且有效的 EZH2 抑制剂，IC50为 4 nM。它对 EZH1 的特异性活性是 60 倍。
T9573	GSK3685032	DNA Methyltransferase	Chromatin/Epigenetic
	GSK-3685032 是一种非时间依赖、非共价、选择性的、可逆的DNMT1抑制剂，IC50=0.036 μM。它诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
T11500L	GSK3368715 dihydrochloride EPZ019997 dihydrochloride,GSK3368715 2HCl,EPZ019997 2HCl	Histone Methyltransferase	Chromatin/Epigenetic
	GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 是一种具有口服活性和高效性的 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，具有抗癌和抗肿瘤活性，抑制PRMT1，PRMT3，PRMT4，PRMT6，PRMT8的活性，可用于研究晚期实体肿瘤。
T72629	PfGSK3/PfPK6-IN-2
	PfGSK3/PfPK6-IN-2 是一种有效的 PfGSK3/PfPK6(PlasmodiumfalciparumGSK3/PK6) 双重抑制剂 (IC50分别为 172 nM 和 11 nM)。PfGSK3/PfPK6-IN-2 可用于疟疾的研究。
T27477	GSK366A
	GSK366A is an anti-TB agent against Mycobacterium bovis BCG and Mycobacterium tuberculosis, targeting MmpL3 and inhibiting EchA6.
T32009	GSK321 GSK 321,GSK-321
	GSK321 is an effective and selective IDH1 mutation inhibitor, which can effectively inhibit the production of 2-HG in HT-1080 cells, and induce IDH1 mutant cells to differentiate into bone marrow at the level of leukemia blasts and more stem cells.
T74887	GSK3735967
	GSK3735967为选择性、可逆的非核苷类DNMT1抑制剂，具备平面二氰基吡啶核心，专一性嵌入DNMT1所结合的半甲基化CpG双核苷酸中。该化合物包含三个结合位点，其中之一可与组蛋白H4K20me3相结合。
T24110	GSK340 GSK=340,GSK 340
	GSK340 is a BET inhibitor.
T11494	GSK3532795 BMS-955176	Others	Others
	GSK3532795 is a potent, orally active, second-generation HIV-1 maturation inhibitor (EC50s: 10.2, 1.9, 2.7, and 13 nM for HIV-1 WT(human serum), HIV-1 WT, HIV-1 V370A, and HIV-1 ΔV370).
T15439	GSK3395879	TRP/TRPV Channel	Membrane transporter/Ion channel
	GSK3395879 is a selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) (IC50: 1 nM for hTRPV4).
T27476	GSK360A GSK-360A,GSK 360A
	GSK360A is a novel prolyl hydroxylase (PHD) domain-containing enzyme inhibitor.
T22342	GSK3368715 3HCl EPZ019997 3HCl,GSK3368715(EPZ019997)	Histone Methyltransferase	Chromatin/Epigenetic
	GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
T27472	GSK317354A GSK 317354A,GSK-317354A
	GSK317354A is a GRK2 inhibitor.
T35838	GSK3182571
	GSK3182571 is a non-speci c kinase inhibitor[1].
T11493	GSK3004774	Others	Others
	GSK3004774 is a nonabsorbable agonist of CaSR (pEC50: 7.3, 6.6, and 6.5 for human, mouse, and rat CaSR). GSK3004774 shows an EC50 of 50 nM for human CaSR.
T11500	GSK3368715 EPZ019997	Histone Methyltransferase	Chromatin/Epigenetic
	GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
T73929	(S,S)-GSK321
	(S,S)-GSK321 是 GSK321 的 (S,S)-对映异构体。
T79021	GSK3839919A
	GSK3839919A为高效HIV-1整合酶抑制剂。
T63977	GSK3739936
	GSK3739936 是 HIV-1 变构整合酶 (HIV-1 allosteric integrase) 的有效抑制剂 (IC50: 11.1 nM, EC50: 1.7 nM)。GSK3739936 也是一种 CYP 的弱抑制剂，其IC50>24.3 μM。GSK3739936 在实验动物中具有良好的药代动力学特性，吸收快、清除率低至中等，以及口服生物利用度良好。
T69784	GSK3527497 HCl
	GSK3527497 is a potent and selective inhibitor of Transient Receptor Potential Vanilloid‑4 (TRPV4) with IC50 = 12 nM) for the treatment of heart failure and respiratory diseases. GSK3527497 is a preclinical candidate suitable for oral and iv administration that is projected to inhibit TRPV4 effectively in patients from a low daily clinical dose.
T27473	GSK334429 GSK-334429,GSK 334429
	GSK334429 is an antagonist of histamine H3 receptor.
T62080	GSK3494245
	GSK3494245 (DDD01305143) 是一种有效的、选择性的、口服具有活力的、可在夹在 β4 和 β5 亚基之间的位点结合寄生虫蛋白酶体 (proteasome) 的糜蛋白酶样活性抑制剂，能够作用于 WTL.donovani 蛋白酶体，其 IC50 值为 0.16μM。GSK3494245 表现出良好的生物安全特性。GSK3494245 对人蛋白酶体的糜蛋白酶样活性具有适当的抑制作用 (IC50: 26S=13 μM；富集的 THP-1 提取物 IC50=40 μM)。
T69786	GSK3491943
	GSK3491943 is a potent TRPV4 inhibitor with IC50 = 3.2 nM. GSK3491943 is a potential agent for the treatment of heart failure and respiratory diseases.
T69785	GSK3527497
	GSK3527497 is a novel potent and selective inhibitor of transient receptor potential vanilloid-4 (TRPV4).
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)。
T26894	BRD0209 BRD-0209,BRD 0209	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	BRD0209 是一种有效、选择性的 GSK3α/β 抑制剂

化合物

Cat.No: T64366

Target: GSK-3

Cat.No: T9987

Target: GSK-3

Cat.No: T73270

Target: GSK-3

Cat.No: T73331

Target: Mitophagy, GSK-3

Cat.No: T24111

Synonym: GSK3 inhibitor XIII,GSK3iXIII,GSK3i-XIII

Target: GSK-3

GSK3β inhibitor II

Cat.No: T21956

Target: GSK-3

GSK-3 inhibitor 1

Cat.No: T11468

Target: GSK-3

GSK3 Substrate, α, β subunit

Cat.No: T76088

GSK3β Inhibitor XI

Cat.No: T36088

Synonym: GSK3β Inhibitor XI

CDK9/10/GSK3β-IN-1

Cat.No: T63851

AChE/BACE1/GSK3β-IN-1

Cat.No: T62719

GSK-3/CDK5/CDK2-IN-1

Cat.No: T35555

Synonym: GSK-3/CDK5/CDK2-IN-1

Cat.No: T27478

Target: Liver X Receptor

Cat.No: T15558

Target: IκB/IKK

Cat.No: T77671

Target: GSK-3

Cat.No: T27475

Synonym: GSK-356278,GSK 356278

Target: PDE

Cat.No: T24109

Synonym: GSK 329,GSK-329

Target: Others

Cat.No: T15440

Target: PPAR

Cat.No: T1941

Target: PPAR

Cat.No: T5745

Synonym: EPZ015938

Target: Histone Methyltransferase

GSK369796 Dihydrochloride

Cat.No: T7195

Synonym: N-tert-butylisoquine

Target: Potassium Channel, Parasite

Cat.No: T15438

Synonym: 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide,DDD-853651

Target: Parasite

Cat.No: T15437

Target: RIP kinase

Cat.No: T5491

Target: c-RET

Cat.No: T6059

Target: Histone Methyltransferase, Autophagy

Cat.No: T9573

Target: DNA Methyltransferase

GSK3368715 dihydrochloride

Cat.No: T11500L

Synonym: EPZ019997 dihydrochloride,GSK3368715 2HCl,EPZ019997 2HCl

Target: Histone Methyltransferase

PfGSK3/PfPK6-IN-2

Cat.No: T72629

Cat.No: T27477

Cat.No: T32009

Synonym: GSK 321,GSK-321

Cat.No: T74887

Cat.No: T24110

Synonym: GSK=340,GSK 340

Cat.No: T11494

Synonym: BMS-955176

Target: Others

Cat.No: T15439

Target: TRP/TRPV Channel

Cat.No: T27476

Synonym: GSK-360A,GSK 360A

GSK3368715 3HCl

Cat.No: T22342

Synonym: EPZ019997 3HCl,GSK3368715(EPZ019997)

Target: Histone Methyltransferase

Cat.No: T27472

Synonym: GSK 317354A,GSK-317354A

Cat.No: T35838

Cat.No: T11493

Target: Others

Cat.No: T11500

Synonym: EPZ019997

Target: Histone Methyltransferase

Cat.No: T73929

Cat.No: T79021

Cat.No: T63977

GSK3527497 HCl

Cat.No: T69784

Cat.No: T27473

Synonym: GSK-334429,GSK 334429

Cat.No: T62080

Cat.No: T69786

Cat.No: T69785

Cat.No: T1741

Target: GSK-3

Cat.No: T26894

Synonym: BRD-0209,BRD 0209

Target: GSK-3

Cat. No.	Product Name	Target	Signaling Pathways
TN6508	Trachelogenin (-)-Trachelogenin	Virus Protease; c-Myc; HCV Protease; Wnt/beta-catenin	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Microbiology/Virology; Proteases/Proteasome; Stem Cells
	Trachelogenin ((-)-Trachelogenin) 分离自Combretum fruticosum，是一种 HCV 进入抑制剂具有抗增殖作用，其机制与影响β-Catenin 信号通路中的 β-Catenin、c-Myc 和 GSK3 等关键蛋白的磷酸化有关，且呈浓度依赖性。Trachelogenin具有抗病毒、抗炎和镇痛活性，在 HCVcc 和 HCVpp 模型中的 IC50 分别为 0.325 和 0.259 μg/mL。
T75621	Secalonic acid D
	Secalonic acid D 是一种抗肿瘤细胞的有毒化合物。Secalonic acid D 可以从Aspergillus aculeatus 的代谢产物中分离得到。Secalonic acid D 激活GSK3-β，并降解β-catenin。因此，Secalonic acid D 下调c-Myc 表达，使细胞周期停滞在 G1 期，诱导细胞凋亡 (apoptosis)。

天然产物

Cat.No: TN6508

Synonym: (-)-Trachelogenin

Target: Virus Protease, c-Myc, HCV Protease, Wnt/beta-catenin

Secalonic acid D

Cat.No: T75621

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-04439	GSK3B Protein, Mouse, Recombinant (His) GSK-3,7330414F15Rik,C861...	Mouse	Baculovirus Insect Cells
	GSK3B Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 49 kDa and the accession number is Q9WV60.
TMPY-04356	GSK3B Protein, Human, Recombinant (His) glycogen synthase kinase 3 beta,glycogen synthase k...	Human	Baculovirus Insect Cells
	GSK3B Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 50.4 kDa and the accession number is P49841-2.
TMPH-01405	GSK3B Protein, Human, Recombinant (E. coli, His)	Human	E. coli
	GSK3B Protein, Human, Recombinant (E. coli, His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 50.7 kDa and the accession number is P49841.

重组蛋白

GSK3B Protein, Mouse, Recombinant (His)

Cat.No: TMPY-04439

Species: Mouse

Expression System: Baculovirus Insect Cells

GSK3B Protein, Human, Recombinant (His)

Cat.No: TMPY-04356

Species: Human

Expression System: Baculovirus Insect Cells

GSK3B Protein, Human, Recombinant (E. coli, His)

Cat.No: TMPH-01405

Species: Human

Expression System: E. coli

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