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Search Results for " gsk-a-1 "

49

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T27499	GSK-A1	HCV Protease; PI4K	Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	GSK-A1 是 III 型磷脂酰肌醇 4-激酶 PI4KA 选择性抑制剂，pIC50为 8.5-9.8，抑制 PtdIns(4,5)P2 再合成，IC50约为 3 nM。GSK-A1有效降低 PtdIns(4)P 的水平，而对 PtdIns(4,5)P2 没影响。GSK-A1在抗丙型肝炎病毒方面有研究的潜力。
T1906	Molibresib GSK 525762A,GSK525762,(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂卓-4-乙酰胺,I-BET 762	Epigenetic Reader Domain	Chromatin/Epigenetic
	Molibresib (GSK525762) 是一种 BET 溴结构域抑制剂，IC50为32.5在42.5 nM 之间。
T7361	Verucerfont NBI77860,3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺,GSK561679	CRFR	GPCR/G Protein
	Verucerfont (NBI77860) 是促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，作用于 CRF1(IC50:6.1 nM)，CRF2 (IC50>1000 nM)和 CRF-BP (IC50>1000 nM)。
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。
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。
T61809	GSK-3β inhibitor 11	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK-3β inhibitor 11（compound 21）是一种强效的糖原合成酶激酶-3β（GSK-3β）抑制剂，其抑制浓度（IC50）为10.02 μM。该化合物在神经退行性疾病研究领域展示了潜在的应用价值[1]。
T6358	1-Azakenpaullone 1-氮杂坎帕罗酮,azakenpaullone	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂，其 IC50=18 nM。
T6129	GSK-1070916 GSK-1070916A,GSK1070916	Apoptosis; Tie-2; FLT; AMPK; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	GSK-1070916 (GSK-1070916A) 是一种选择性，ATP 竞争型的极光激酶B/C 抑制剂，Ki 值分别为0.38和1.5 nM。
T14613	BIP-135	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	BIP-135 是一个高效、选择性的，ATP 竞争性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 作用的 IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。
T2622	GSK 650394 GSK650394	SGK; Influenza Virus	Metabolism; Microbiology/Virology
	GSK 650394 是一种新颖的 SGK 抑制剂，可抑制流感病毒复制。它还是一种血清和糖皮质激素调节的激酶 1 抑制剂。
T6003	GSK1904529A GSK 4529	Apoptosis; Raf; VEGFR; IGF-1R; Syk	Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors
	GSK1904529A (GSK 4529) 是一种选择性，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体和胰岛素受体抑制剂，IC50值分别为 27 和 25 nM。它具有抗肿瘤活性。
T61360	ARN25068	GSK-3; DYRK; Microtubule Associated; Src	Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	ARN25068是三种蛋白激酶(GSK-3β、FYN和DYRK1A)的亚微摩尔抑制剂，可用于治疗tau相关神经系统疾病。
T2310L	CHIR-99021 HCl CT99021 HCl,Laduviglusib HCl	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂，IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性，对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外，CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外，它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外，拉杜维格西单盐酸盐诱导自噬[1][2][3]。
T16850	SB-265610 GSK-CXCR2	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SB-265610 (GSK-CXCR2) 是竞争性非肽变构CXCR2选择性拮抗剂，可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性，IC50分别为 3.7 和 70 nM。
T6285	GSK-690693 GSK690693	Serine Protease; Akt; PKC; AMPK; Autophagy	Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	GSK-690693 是一种泛 Akt 抑制剂，对 Akt1、Akt2和 Akt3的 IC50分别为 2 nM、13 nM 和9 nM。它也是一种 AMPK 的抑制剂，影响 ULK1 的活性，并能显著抑制 STING 依赖的 IRF3 的激活。
T22341	GSK-114	Others	Others
	GSK 114 是口服有活性的、高选择性的TNNI3K 抑制剂 (IC50= 25 nM)。其中TNNI3K (又称 CARK) 是酪氨酸样激酶家族的成员，选择性在心脏组织中表达。它对 TNNI3K 的选择性是 B-Raf 激酶的 40 倍 (IC50= 1 µM)。
T6458	CYC-116 噻氯匹定	VEGFR; FLT; CDK; S6 Kinase; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	CYC116是一种有效的极光激酶 A 和 B 的抑制剂，Ki 值分别为8和9 nM。
T60485	DIF-3
	DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
T2378	RGB-286638 free base	GSK-3; MEK; JAK; CDK	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	RGB-286638 free base 是一种新型 CDK 抑制剂，抑制cyclin T1-CDK9、cyclin B1-CDK1、cyclin E-CDK2、cyclin D1-CDK4、cyclin E-CDK3和p35-CDK5活性，IC50分别为 1、2、3、4、5 和 5 nM。它也抑制 GSK-3β、TAK1、Jak2 和 MEK1，IC50值分别为 3、5、50和 54 nM。
T11468	GSK-3 inhibitor 1	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	GSK-3 inhibitor 1 is a GSK-3 inhibitor.
T22157	TCS 2002
	GSK-3β inhibitor 9 (Compound 9b) 是一种具有高选择性、口服有效的 GSK-3β抑制剂，IC50为 35 nM。GSK-3β inhibitor 9 显示出良好的药代动力学特征，包括良好的血脑屏障渗透。GSK-3β inhibitor 9 可用于阿尔茨海默病的研究。
T64143	AChE/GSK-3β-IN-1
	AChE/GSK-3β-IN-1 是一种有效的、能透过血脑屏障的双重AChE/GSK-3β抑制剂，能够作用于 hAChE (IC50: 1.2 nM)、hBChE (IC50: 149.8 nM) 和 hGSK-3β (IC50: 22.4 nM)。AChE/GSK-3β-IN-1 能够占据 DYRK1A 的 ATP 结合位点。AChE/GSK-3β-IN-1 对 CMGC 激酶家族表现出较高的激酶选择性。AChE/GSK-3β-IN-1 能够抑制 ROS 表达，减少氧化应激。AChE/GSK-3β-IN-1 能够用于研究阿尔兹海默症。
T27488	GSK-690 GSK 690
	GSK-690 is a potent, reversible and selective inhibitors of Lysine Specific Demethylase 1.
T70965	GSK-2245035 maleate
	GSK-2245035 maleate is a selective Toll-like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties.
T61804	GSK-3β inhibitor 6
	GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β, with an IC50 value of 24.4 μM. It demonstrates significant enhancement of hepatocyte glucose uptake (38%). This compound holds great potential for studying various diseases including diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].
T27442	GSK 224876 GSK-224876,GSK224876
	GSK 224876 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.
T11473	GSK-5498A	Others	Others
	GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
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。
T24969	18BIOder 18 BIOder,18-BIOder
	18BIOder is a neuroprotective inhibitor of GSK-3β, highly selectively inhibiting HIV-1. It is the second generation derivative of 6BIO.
T70724	GSK-2256098 HCl
	GSK-2256098 HCl is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.
T11503	GSK 690 Hydrochloride	Histone Demethylase	Chromatin/Epigenetic
	GSK 690 (Hydrochloride) 是一种可逆的赖氨酸特异性去甲基化酶1 (LSD1)抑制剂，Kd 值为 9 nM，IC50值为 37 nM。
T27445	GSK-1004723 GSK 1004723
	GSK-1004723 is a novel antagonist of histamine H(1) and H(3) receptor. It represents a potential novel therapy for allergic rhinitis.
T41232	GSK 2833503A
	GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.
T27446	GSK-1034702 GSK-1034702 HCl,GSK 1034702
	GSK-1034702 is a selective M(1) receptor allosteric agonist, it may have therapeutic benefits in disorders of impaired learning including Alzheimer's disease.
T68855	Hymenialdisine Analogue #1
	Hymenialdisine Analogue #1 is the indole derivative of Hymenialdisine, a potent inhibitor of a variety of kinases including MEK-1, GSK-3Β, and CKI. It also exhibits inhibition of the G2 cell cycle checkpoint at the micromolar concentrations.
T27461	GSK2336805 GSK 2336805,GSK-2336805,JNJ-56914845,GSK-805,GSK805
	GSK-2336805 is a HCV NS5A inhibitor. GSK2336805 retained activity on chimeric replicons containing NS5A patient sequences from genotype 1 and patient and consensus sequences for genotypes 4 and 5 and part of genotype 6.
T11466	GSK-2793660	Others	Others
	GSK-2793660 是一种具有口服活性并且不可逆的组织蛋白酶 C (Cathepsin C；CTSC) 抑制剂。GSK-2793660 是一种生物活性肽，可用于支气管扩张的研究。
T77156	Depemokimab
	Depemokimab (GSK-3511294) 是一种长效的抗IL-15单克隆抗体。Depemokimab 可用于哮喘研究。
T69986	BMS-955176 HCl
	GSK-3532795 is a second generation inhibitor of hiv-1 maturation, exhibiting a broader spectrum of antiviral effect in vitro and in clinical studies than the prototypical maturation inhibitor bevirimat
T80124	C-Peptide 1 (rat)	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	C-Peptide 1 (rat) 为肽类化合物，作为β-catenin/GSK-3β激活剂，具有调节Wnt/β-catenin信号通路的功能，常用于癌症研究领域。
T60748	ZDWX-25
	ZDWX-25 是 GSK-3β和 DYRK1A 的高效双重抑制剂，它对 SH-SY5Y 和 HL-7702 细胞显示出显著的细胞毒性。ZDWX-25 可用于研究阿尔茨海默症，其对 GSK-3β 的 IC50值为 71 nM。。
T11960	MBM-55	GSK-3; MAPK; DYRK; Akt; Chk; Bcr-Abl; CDK; S6 Kinase; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	MBM-55 是一种有效的中心体相关激酶 2 (NEK2) 抑制剂，IC50 为 1 nM。 MBM-55 通过诱导细胞周期停滞和凋亡有效抑制癌细胞的增殖。
T11961	MBM-55S	GSK-3; MAPK; Akt; Bcr-Abl; CDK; S6 Kinase; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	MBM-55S 是一种有效的 Nek2 抑制剂，IC50 为 1 nM。 MBM-55S 抑制细胞周期停滞和凋亡，从而抑制癌细胞的增殖。 MBM-55S 表现出抗肿瘤作用。
T81692	Nelistotug
	Nelistotug (GSK 6097608; GSK6097608) 是一种针对CD96的人源化IgG1κ抗体。CD96属于免疫球蛋白超家族，被认为是潜在的免疫检查点靶标。
T75808	Phospho-Glycogen Synthase Peptide-2(substrate) TFA
	Phospho-Glycogen Synthase Peptide-2 (底物)为糖原合酶激酶-3 (GSK-3) 的特异性肽底物，适用于蛋白丝氨酸激酶的亲和纯化。
T79693	PIMPC	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	PIMPC为具抗氧化及金属螯合性能之化合物，新型糖原合成酶激酶3（GSK-3）抑制剂，潜在抗阿尔茨海默病作用。
T80587	Alunacedase alfa HrsACE2,GSK 2586881	SARS-CoV	Microbiology/Virology
	Alunacedase alfa (HrsACE2; GSK 2586881) 是一种人源重组的可溶性血管紧张素转化酶 2（hrsACE2）。作为转基因可溶性形态的 ACE2，Alunacedase alfa 能够减少 SARS-CoV-2 与细胞膜结合 ACE2 的竞争性进入，因此具有研究 SARS-CoV-2 的可能性。
T35560	SAR502250
	SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2]. SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2]. SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mic...
T73196	RGB-286638
	RGB-286638 是一种有效的 CDK 抑制剂，抑制cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3和p35-CDK5活性，IC50分别为 1，2，3，4，5 和 5 nM；同时可抑制GSK-3β，TAK1，Jak2和MEK1，IC50值分别为 3，5，50，和 54 nM。

化合物

Cat.No: T27499

Target: HCV Protease, PI4K

Cat.No: T1906

Synonym: GSK 525762A,GSK525762,(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂卓-4-乙酰胺,I-BET 762

Target: Epigenetic Reader Domain

Cat.No: T7361

Synonym: NBI77860,3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺,GSK561679

Target: CRFR

(E/Z)-GSK-3β inhibitor 1

Cat.No: T9178

Synonym: GSK-3β inhibitor 1

Target: GSK-3

Cat.No: T64366

Target: GSK-3

GSK-3β inhibitor 11

Cat.No: T61809

Target: GSK-3

1-Azakenpaullone

Cat.No: T6358

Synonym: 1-氮杂坎帕罗酮,azakenpaullone

Target: GSK-3

Cat.No: T6129

Synonym: GSK-1070916A,GSK1070916

Target: Apoptosis, Tie-2, FLT, AMPK, Aurora Kinase

Cat.No: T14613

Target: GSK-3

Cat.No: T2622

Synonym: GSK650394

Target: SGK, Influenza Virus

Cat.No: T6003

Synonym: GSK 4529

Target: Apoptosis, Raf, VEGFR, IGF-1R, Syk

Cat.No: T61360

Target: GSK-3, DYRK, Microtubule Associated, Src

Cat.No: T2310L

Synonym: CT99021 HCl,Laduviglusib HCl

Target: GSK-3

Cat.No: T16850

Synonym: GSK-CXCR2

Target: CXCR

Cat.No: T6285

Synonym: GSK690693

Target: Serine Protease, Akt, PKC, AMPK, Autophagy

Cat.No: T22341

Target: Others

Cat.No: T6458

Synonym: 噻氯匹定

Target: VEGFR, FLT, CDK, S6 Kinase, Aurora Kinase

Cat.No: T60485

RGB-286638 free base

Cat.No: T2378

Target: GSK-3, MEK, JAK, CDK

GSK-3 inhibitor 1

Cat.No: T11468

Target: GSK-3

Cat.No: T22157

AChE/GSK-3β-IN-1

Cat.No: T64143

Cat.No: T27488

Synonym: GSK 690

GSK-2245035 maleate

Cat.No: T70965

GSK-3β inhibitor 6

Cat.No: T61804

Cat.No: T27442

Synonym: GSK-224876,GSK224876

Cat.No: T11473

Target: Others

GSK3 Substrate, α, β subunit

Cat.No: T76088

Cat.No: T24969

Synonym: 18 BIOder,18-BIOder

GSK-2256098 HCl

Cat.No: T70724

GSK 690 Hydrochloride

Cat.No: T11503

Target: Histone Demethylase

Cat.No: T27445

Synonym: GSK 1004723

Cat.No: T41232

Cat.No: T27446

Synonym: GSK-1034702 HCl,GSK 1034702

Hymenialdisine Analogue #1

Cat.No: T68855

Cat.No: T27461

Synonym: GSK 2336805,GSK-2336805,JNJ-56914845,GSK-805,GSK805

Cat.No: T11466

Target: Others

Cat.No: T77156

Cat.No: T69986

C-Peptide 1 (rat)

Cat.No: T80124

Target: GSK-3

Cat.No: T60748

Cat.No: T11960

Target: GSK-3, MAPK, DYRK, Akt, Chk, Bcr-Abl, CDK, S6 Kinase, Aurora Kinase

Cat.No: T11961

Target: GSK-3, MAPK, Akt, Bcr-Abl, CDK, S6 Kinase, Aurora Kinase

Cat.No: T81692

Phospho-Glycogen Synthase Peptide-2(substrate) TFA

Cat.No: T75808

Cat.No: T79693

Target: GSK-3

Alunacedase alfa

Cat.No: T80587

Synonym: HrsACE2,GSK 2586881

Target: SARS-CoV

Cat.No: T35560

Cat.No: T73196

Cat. No.	Product Name	Target	Signaling Pathways
T6S0653	Linarin Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷	TNF; AChE	Apoptosis; Neuroscience
	Linarin (Acacetin-7-O-rutinoside) 是一种选择性的乙酰胆碱酯酶 (AChE) 抑制剂，从薄荷花提取物中分离得到。
TN5171	Tricetin	Apoptosis; Others; Nrf2	Apoptosis; Immunology/Inflammation; Others
	Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用（PPI）的强效竞争性抑制剂，通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路，保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1（PS-1）表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症，保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。
T38441	Manzamine A hydrochloride
	Manzamine A hydrochloride is an orally active beta-carboline alkaloid that exhibits specific inhibitory effects on GSK-3β (IC50 = 10.2 μM) and CDK-5 (IC50 = 1.5 μM). Additionally, it targets vacuolar ATPases, leading to the inhibition of autophagy in pancreatic cancer cells. Manzamine A hydrochloride possesses antimalarial and anticancer properties, and also demonstrates potent activity against HSV-1[4].

天然产物

Cat.No: T6S0653

Synonym: Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷

Target: TNF, AChE

Cat.No: TN5171

Target: Apoptosis, Others, Nrf2

Manzamine A hydrochloride

Cat.No: T38441

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