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39

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T79011	TrkB-IN-1	Trk receptor	Tyrosine Kinase/Adaptors
	TrkB-IN-1为一种有效的口服活性TrkB激动剂，展现出优良的药代动力学特性。该化合物能够逆转AD模型小鼠的认知功能缺陷，适用于阿尔茨海默病的研究。
T12731	RIPK1-IN-7	RIP kinase	Apoptosis; NF-κB
	RIPK1-IN-7 是一种选择性有效的 RIPK1 抑制剂，Kd 值为 4 nM，IC50值为 11 nM。在实验性 B16 黑色素瘤肺转移模型中表现出优异的抗转移活性。
T0678	Amitriptyline hydrochloride Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin	Trk receptor; Sigma receptor; 5-HT Receptor; Serotonin Transporter; Sodium Channel; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
	Amitriptyline hydrochloride (Annoyltin) 是血清素再摄取转运体和去甲肾上腺素再摄取转运体抑制剂，还与多巴胺再摄取转运体结合，其Ki 为 2.58 μM。它也抑制肾上腺素能受体、毒蕈碱受体、组胺受体、5-羟色胺受体。它是TrkA 和TrkA 受体的激动剂，具有强神经营养活性和有抗抑郁作用。
T4349	Sitravatinib MG516,MGCD516	Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效，且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)	Trk receptor	Tyrosine Kinase/Adaptors
	Cyclotraxin B acetate(1203586-72-4 free base) 是 TrkB 受体的拮抗剂；抑制 BDNF 诱导的 TrkB 活性 (IC50 = 0.30 nM)。变构改变 TrkB 受体构象但不改变 BDNF 结合。防止 BDNF 引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。
T6097	GNF-5837 GNF 5837	Trk receptor; PDGFR; c-Kit	Angiogenesis; Tyrosine Kinase/Adaptors
	GNF-5837 是一种选择性的，有效的，口服生物利用的泛TRK 抑制剂，在 Ba/F3 细胞中显示出抗增殖作用 (对Tel-TrkC,Tel-TrkB 和Tel-TrkA 的IC50值分别为 7 nM，9 nM 和 11 nM)。
T7568	LM22A-4	Trk receptor	Tyrosine Kinase/Adaptors
	LM22A-4 是特异性的tyrosine kinase receptor B 激动剂，常用于研究神经系统疾病。
T2359	ANA-12 ANA 12,ANA12	Trk receptor	Tyrosine Kinase/Adaptors
	ANA-12 是一种选择性TrkB 拮抗剂，对高亲和力和低亲和力位点的IC50分别为45.6 nM 和41.1 μM。
T5635	CH7057288	Trk receptor	Tyrosine Kinase/Adaptors
	CH7057288 是选择性TRK 抑制剂。
T14363	AZ-23 AZ 23,AZ23	Trk receptor	Tyrosine Kinase/Adaptors
	AZ-23是一种 ATP-竞争性的，口服具有活性的 Trk 激酶 A/B/C 抑制剂，IC50值分别为2 nM (TrkA)，8 nM (TrkB)，24 nM (FGFR1)，52 nM (Flt3)，55 nM (Ret)，84 nM (MuSk)，99 nM (Lck)。
T73397	ENT-C225	Trk receptor	Tyrosine Kinase/Adaptors
	ENT-C225 是一种高效的 TrkB 神经营养素受体（TrkBR）激活剂，具有神经保护活性，可用于研究阿尔茨海默病和帕金森病。
T4496	LM22B-10 LM22B10	ERK; Trk receptor; Akt	Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	LM22B-10 是TrkB/TrkC 神经营养因子受体激活剂，诱导体内外TrkB、TrkC、AKT 和ERK 的活化。
T4257	Belizatinib TSR-011	Trk receptor; ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	Belizatinib (TSR-011) 是可口服的ALK 和 TRKA、TRKB、TRKC 双重抑制剂，对野生型重组 ALK 的IC50值为0.7 nM。
T3678	Entrectinib RXDX-101,恩曲替尼,NMS-E628	Trk receptor; ROS; ALK; Autophagy; ROS Kinase	Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂，具有抗肿瘤和中枢神经活性，抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。
T5524	Aurora kinase inhibitor-3 Aurora Kinase Inhibitor III	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) 是一种有效的，选择性 Aurora A 激酶抑制剂，IC50为 42 nM。
T41224	CG 428	Trk receptor	Tyrosine Kinase/Adaptors
	CG 428 是一种有效的原肌球蛋白受体激酶 (TRK) 降解剂 (uSMITETM)，DC50 为 0.36 nM。 CG 428 包含泛 TRK 抑制剂 GNF-8625 的类似物，通过接头连接到 cereblon E3 连接酶配体泊马度胺。 CG 428 对 TRKA 的选择性优于 TRKC 和 TRKB，Kd 为 1nM、4.2 nM 和 28 nM。 CG 428 抑制 KM12 结肠癌细胞的生长，IC50 为 2.9 nM。
T2349	BMS-754807	Trk receptor; c-Met/HGFR; IGF-1R	Tyrosine Kinase/Adaptors
	BMS754807 是一种可逆的IGF-1R 抑制剂 (IC50:1.8 nM，Ki<2 nM)，也是一种可逆的IR 抑制剂 (IC50:7 nM，Ki<2 nM)。它也抑制 Met (IC50:6 nM)，RON (IC50:44 nM)，TrkA (IC50:7 nM)，TrkB (IC50:4 nM)，AurA (IC50:9 nM) 和 AurB (IC50:25 nM) 的活性。
T2638	Gandotinib LY2784544	VEGFR; FGFR; FLT; JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Gandotinib (LY2784544) 是一种JAK2抑制剂，IC50为 3 nM。它也抑制FLT3、FLT4、FGFR2、TYK2 和 TRKB，IC50分别为 4、25、32、44 和 95 nM。
T38260	SP 600125, negative control JNK Inhibitor II, negative control
	SP 600125, negative control 是 SP 600125 的甲基化类似物，可用作SP 600125的阴性对照，对 DTP3和GADD45β/MKK7（生长停滞和 DNA 损伤诱导型 β/介原活化蛋白激酶激酶 7）具有抑制作用，能够恢复活化。SP 600125, negative control 对 JNK2 和 JNK3 的 IC50s 分别为 18 和 24 μM。
T17169	Trk-IN-4 PF-6683324 isomer	Trk receptor	Tyrosine Kinase/Adaptors
	Trk-IN-4 is an effective pan-Trk inhibitor in cell-based assays (IC50s: 1.9 nM, 2.6 nM, and 1.1 nM for TrkA, TrkB, and TrkC, respectively).
T68403	AZD-6918
	AZD6918 is a novel potent and selective inhibitor of the Trk tyrosine kinases. AZD-6918 attenuates the BDNF/TrkB-induced protection of neuroblastoma cells from etoposide in vitro and in vivo. AZD6918 inhibited wild-type TrkB-induced cell migration and cell growth.
T17170	PF-06737007	Trk receptor	Tyrosine Kinase/Adaptors
	PF-06737007 is an effective inhibitor of pan-Trk in cell-based assays (IC50s: 7.7 nM, 15 nM, and 3.9 nM for TrkA, TrkB, and TrkC, respectively).
T12925	Sitravatinib malate MGCD516 malate,MG-516 malate	TAM Receptor	Tyrosine Kinase/Adaptors
	Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
T13207	PF-06733804	Trk receptor	Tyrosine Kinase/Adaptors
	PF-06733804 is a potent inhibitor of pan-Trk in cell-based assays (IC50s: 8.4 nM, 6.2 nM, and 2.2 nM for TrkA, TrkB, and TrkC) with anti-hyperalgesic effect.
T75832	Cyclotraxin B TFA
	Cyclotraxin B TFA 是一种环肽，是一种高效且选择性的 TrkB 抑制剂，且不会改变 BDNF 的结合。Cyclotraxin B TFA 非竞争性地抑制 BDNF 诱导的 TrkB 活性，IC50值为 0.30 nM。Cyclotraxin B TFA 可以穿越血脑屏障，并具有止痛和抗焦虑的行为作用。
T14921	CE-245677	Tie-2; Trk receptor	Tyrosine Kinase/Adaptors
	CE-245677 是可逆的Tie2和TrkA/B 抑制剂，在细胞体系下的IC50值分别为 4.7 和 1 nM。
T61443	Trk-IN-7
	Trk-IN-7 (compound I-6) is a highly potent inhibitor of TRK, exhibiting IC50 values ranging from 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. In addition, Trk-IN-7 demonstrates notable inhibition against EML4-ALK (IC50 <15 nM), as well as ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50 = 5-50 nM) [1].
TP2068	Cyclotraxin B
	Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p
T22318	Taletrectinib DS-6051b,AB-106	Trk receptor; ROS; ROS Kinase	Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Taletrectinib (AB-106) 是具有口服活力的、选择性的 ROS1/NTRK 抑制剂。它对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用，IC50值分别为 0.207、0.622、2.28 和 0.98 nM。它还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。
T61551	Trk-IN-20
	Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1].
T37081	HIOC
	Selective TrkB receptor agonist. Protects neurons from excitotoxicity. Protects retinas from light-induced retinal degeneration (LIRD) in vivo. Blood brain barrier and blood-retinal barrier penetrant.
T73306	TrkA-IN-3
	TrkA-IN-3 是一种有效和亚选择性的TrkA 变构抑制剂，IC50值为 22.4 nM。TrkA-IN-3 对TrkA 的选择性超过TrkB 和TrkC8000 倍。TrkA-IN-3 可用于研究疼痛。
T73033	TRK II-IN-1	Trk receptor	Tyrosine Kinase/Adaptors
	TRKII-IN-1 是一种有效的 II 型TRK抑制剂，对TRKA/B/C及TRKAG667C的IC50分别为3.3、6.4、4.3 和 9.4 nM。此外，TRKII-IN-1 对FLT3、RET和VEGFR2也具有抑制作用，其IC50分别为1.3、9.9 和 71.1 nM。TRKII-IN-1 主要用于TRK驱动的癌症研究。
TP2069	BDNF (human)
	Member of the neurotrophin growth factor family that binds and activates TrkB and p75 neurotrophin receptors. Enhances the survival, growth and differentiation of neurons. BDNF expression is altered in neurodegenerative disorders such as Parkinson's and A
T63076	IHMT-TRK-284
	IHMT-TRK-284 (Compound 34) 是一种有效的、口服具有活力的 type II TRK kinase 抑制剂，能够作用于 TRKA (IC50: 10.5 nM)、TRKB (IC50: 0.7 nM)、TRKC (IC50: 2.6 nM)。IHMT-TRK-284 在激酶组中表现出良好的选择性，体内具有良好的抗肿瘤作用。
T70276	Roridin E
	Roridin E inhibits the receptor tyrosine kinases FGFR3, IGF-1R, PDGFRβ, and TrkB (IC50s = 0.4, 0.4, 1.4, and 1 μM, respectively) and induces cytotoxicity in multiple breast cancer cell lines (IC50s = 0.02-0.05 nM). It also inhibits proliferation in a panel of additional cancer cell lines (IC50s = <0.01 μM).
T64070	Pan-Trk-IN-3
	Pan-Trk-IN-3 是一种有效的广谱 Trk 及其耐药突变体抑制剂，能够作用于 TrkA (IC50: 2 nM)、TrkB (IC50: 3 nM)、TrkC (IC50: 2 nM)、TrkAG595R (IC50: 21 nM)、TrkAG667C (IC50: 26 nM)、TrkAG667S (IC50: 5 nM)、TrkAF589L (IC50: 7 nM) 和 TrkCG623R (IC50: 6 nM)。Pan-Trk-IN-3 能够诱导细胞凋亡 (apoptosis)，具有显著的抗肿瘤效果。
T37582	Ganglioside GM1 Mixture (ovine) (ammonium salt)
	Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium i...
T13208	TrkA-IN-1	Trk receptor	Tyrosine Kinase/Adaptors
	TrkA-IN-1 is a potent and selective inhibitor of Tropomyosin-related kinase A (TrkA) (IC50: 99 nM in a cell-based assay) with analgesic activity.

化合物

Cat.No: T79011

Target: Trk receptor

Cat.No: T12731

Target: RIP kinase

Amitriptyline hydrochloride

Cat.No: T0678

Synonym: Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin

Target: Trk receptor, Sigma receptor, 5-HT Receptor, Serotonin Transporter, Sodium Channel, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor

Cat.No: T4349

Synonym: MG516,MGCD516

Target: Discoidin Domain Receptor (DDR), VEGFR, FLT, Trk receptor, TAM Receptor, c-Kit, Ephrin Receptor

Cyclotraxin B acetate(1203586-72-4 free base)

Cat.No: TP2068L

Target: Trk receptor

Cat.No: T6097

Synonym: GNF 5837

Target: Trk receptor, PDGFR, c-Kit

Cat.No: T7568

Target: Trk receptor

Cat.No: T2359

Synonym: ANA 12,ANA12

Target: Trk receptor

Cat.No: T5635

Target: Trk receptor

Cat.No: T14363

Synonym: AZ 23,AZ23

Target: Trk receptor

Cat.No: T73397

Target: Trk receptor

Cat.No: T4496

Synonym: LM22B10

Target: ERK, Trk receptor, Akt

Cat.No: T4257

Synonym: TSR-011

Target: Trk receptor, ALK

Cat.No: T3678

Synonym: RXDX-101,恩曲替尼,NMS-E628

Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase

Aurora kinase inhibitor-3

Cat.No: T5524

Synonym: Aurora Kinase Inhibitor III

Target: Aurora Kinase

Cat.No: T41224

Target: Trk receptor

Cat.No: T2349

Target: Trk receptor, c-Met/HGFR, IGF-1R

Cat.No: T2638

Synonym: LY2784544

Target: VEGFR, FGFR, FLT, JAK

SP 600125, negative control

Cat.No: T38260

Synonym: JNK Inhibitor II, negative control

Cat.No: T17169

Synonym: PF-6683324 isomer

Target: Trk receptor

Cat.No: T68403

Cat.No: T17170

Target: Trk receptor

Sitravatinib malate

Cat.No: T12925

Synonym: MGCD516 malate,MG-516 malate

Target: TAM Receptor

Cat.No: T13207

Target: Trk receptor

Cyclotraxin B TFA

Cat.No: T75832

Cat.No: T14921

Target: Tie-2, Trk receptor

Cat.No: T61443

Cat.No: TP2068

Cat.No: T22318

Synonym: DS-6051b,AB-106

Target: Trk receptor, ROS, ROS Kinase

Cat.No: T61551

Cat.No: T37081

Cat.No: T73306

Cat.No: T73033

Target: Trk receptor

Cat.No: TP2069

Cat.No: T63076

Cat.No: T70276

Cat.No: T64070

Ganglioside GM1 Mixture (ovine) (ammonium salt)

Cat.No: T37582

Cat.No: T13208

Target: Trk receptor

Cat. No.	Product Name	Target	Signaling Pathways
T1354	N-Acetyl-5-hydroxytryptamine Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin	Trk receptor; Endogenous Metabolite	Metabolism; Tyrosine Kinase/Adaptors
	N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) 是褪黑激素的直接前体，能够有效激活TrkB 受体。
T2816	7,8-Dihydroxyflavone 二羟基黄酮水合物,7,8-DHF	Apoptosis; Trk receptor	Apoptosis; Tyrosine Kinase/Adaptors
	7,8-Dihydroxyflavone (7,8-DHF) 是一种选择性有效的TrkB 激动剂，其模拟脑源性神经营养因子的生理作用。它有潜力研究各种神经疾病。
T1704	Diosmetin Luteolin 4-methyl ether,香叶木素	P450; Trk receptor	Metabolism; Tyrosine Kinase/Adaptors
	Diosmetin (Luteolin 4-methyl ether) 是一种天然类黄酮，能够抑制人CYP1A 酶活性，在HepG2细胞的IC50值为40 μM。

天然产物

N-Acetyl-5-hydroxytryptamine

Cat.No: T1354

Synonym: Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin

Target: Trk receptor, Endogenous Metabolite

7,8-Dihydroxyflavone

Cat.No: T2816

Synonym: 二羟基黄酮水合物,7,8-DHF

Target: Apoptosis, Trk receptor

Cat.No: T1704

Synonym: Luteolin 4-methyl ether,香叶木素

Target: P450, Trk receptor

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