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26

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5102	TGN-020 TGN020	Aquaporin; PROTAC Linker	Membrane transporter/Ion channel; PROTAC
	TGN-020 是一种属于 alkyl chain 类的 PROTAC linker，可用于 PROTAC 的合成分子。TGN020 是一种选择性水通道蛋白 4 (AQP4) 抑制剂，IC50为 3.1 μM。TGN020 减轻大鼠脊髓压迫损伤后的水肿并抑制神经胶质瘢痕的形成。
T10624	BT-13	c-RET	Apoptosis; Tyrosine Kinase/Adaptors
	BT-13 是一种胶质细胞源性神经营养因子 (GDNF) 受体 RET 的选择性激动剂，独立于 GDNF 配体发挥作用，能够促进体外感觉神经元神经突生长，减少大鼠神经病变的发生。
T73286	SRI-42127	HuR	Chromatin/Epigenetic
	SRI-42127 是一种新型 RNA 调节因子 HuR 的小分子抑制剂，抑制肿瘤生长，可减弱脂多糖诱导的神经炎症模型中的神经胶质活化，通过抑制神经炎症反应来减轻神经损伤后的神经性疼痛。
T33535	MW01-2-151SRM MW 151,MW-151,MW012151SRM,MW151,MW01 2 151SRM	Others	Others
	MW01-2-151SRM 是一种新型可穿过血脑屏障的小分子小胶质细胞活化抑制剂，具有抗神经炎作用，可减弱神经炎症模型中的神经胶质细胞因子上调，可用研究创伤性脑损伤、阿尔茨海默病和海藻氨酸毒性。
T3515	TRC051384 HCl	HSP	Cytoskeletal Signaling; Metabolism
	TRC051384 HCl 是热休克蛋白 Hsp70 的诱导剂，可激活热休克因子-1 并增强神经元和神经胶质细胞中 Hsp72 的表达。
T77092	Nadecnemab REGN-5069	Others	Others
	Nadecnemab 是一种靶向胶质细胞源性神经营养因子家族受体 GFRA3 的 IgG4κ 抗体。Nadecnemab 可用于膝骨关节炎和神经系统疾病。
T67733	BT44	Others	Others
	BT44是一种新的、第二代神经胶质细胞系衍生的神经营养因子模拟物，具有改善的生物活性，是治疗神经退行性疾病的先导化合物。
T13587	BT18	Others	Others
	BT18 是一种功能类似于胶质细胞源神经营养因子的分子模拟物。它能够影响 GDNF 家族受体 GFRα1 和 RET 受体酪氨酸激酶 RetA 的功能。
T3527	TRC051384 TRC 051384	HSP	Cytoskeletal Signaling; Metabolism
	TRC051384 是一种热休克蛋白70 (HSP70) 诱导剂，可减少中风相关的神经元损伤并增加短暂性缺血性中风大鼠模型的存活率，激活热休克因子-1 并导致分子伴侣和抗炎活性升高，增强神经元和神经胶质细胞中 Hsp72 的表达。
T23454	TFB-TBOA	Others	Others
	glial glutamate transporter EAAT1 and EAAT2 inhibitor
T29021	TT-301 MW 189,MW189,TT301,TT 301,MW 189 ;MW189,MW-189
	TT-301 is a cytokine inhibitor and glial cell inhibitor.
T22913	L-CCG-lll	Others	Others
	inhibitor of both glial and neuronal uptake of glutamate, aspartate and cysteate.
T76238	Zilganersen
	Zilganersen (ION373) 为GFAP抑制剂，属于反义寡核苷酸类。适用于亚历山大病(AxD)的研究。
T38202	PAQ
	PAQ is a neuroprotective agent. It protects dopaminergic neurons from cell death without inhibiting glial cell proliferation in a rat midbrain culture model of Parkinson's disease when used at a concentration of 10 μM. PAQ (25 or 50 mg/kg, twice per day) prevents loss of dopaminergic neurons in the substantia nigra in a mouse model of Parkinson's disease induced by MPTP.
T37699	Org 24598
	Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 \|Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibi...
T60344	L-Cytidine
	L-Cytidine 是Cytidine 的 L-构型形式。L-Cytidine 是一种嘧啶核苷，是RNA 的组成部分。Cytidine 可控制神经胶质谷氨酸循环，影响脑磷脂代谢，儿茶酚胺的合成和线粒体功能。
T64036	5-HT6R/MAO-B modulator 1
	5-HT6R/MAO-B modulator 1 是一种 5-HT6R 在 Gs 信号传导处的拮抗剂和不可逆的MAO-B 抑制剂，表现出胶质保护活性。5-HT6R/MAO-B modulator 1 对东莨菪碱诱导的记忆缺陷表现出诱导作用。
T39343	MW-150 hydrochloride MW01-18-150SRM hydrochloride,MW-150 hydrochloride
	MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T71174	PBT434 HBr
	PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is g...
T37898	UDP-α-D-Glucose (sodium salt hydrate)
	UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14receptor (EC50= 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.1It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.2 1.Jacobson, K.A., Ivanov, A.A., de Castro, S., et al.Development of selective agonists and antagonists of P2Y receptorsPurin...
T63293	Axl-IN-7
	Axl-IN-7 是 AXL 的有效抑制剂。Axl-IN-7 能够用于研究 Axl 相关疾病，如癌症(如急性髓系白血病、乳腺癌、黑色素瘤、胰腺癌和神经胶质肿瘤)、免疫系统紊乱、肾脏疾病和心血管疾病。
T71576	SIM010603
	SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Mor...
T35553	Ganglioside GQ1b Mixture (sodium salt)
	Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes throu...
T36188	Ceramide Phosphoethanolamines (bovine)
	Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi...
T76014	IGF-I (24-41) (TFA)
	IGF-I (24-41) TFA（Insulin-like Growth Factor I (24-41) TFA）是类胰岛素生长因子I的一个氨基酸片段，覆盖24至41位点。作为一种70个氨基酸组成的多肽激素，IGF-I TFA对神经元和神经胶质细胞具有营养作用，而且在调节全身生长激素（GH）活性中扮演关键角色。它还具备合成代谢、抗氧化、抗炎及细胞保护功能，对躯体生长及行为发育调节作用显著。

化合物

Cat.No: T5102

Synonym: TGN020

Target: Aquaporin, PROTAC Linker

Cat.No: T10624

Target: c-RET

Cat.No: T73286

Target: HuR

Cat.No: T33535

Synonym: MW 151,MW-151,MW012151SRM,MW151,MW01 2 151SRM

Target: Others

Cat.No: T3515

Target: HSP

Cat.No: T77092

Synonym: REGN-5069

Target: Others

Cat.No: T67733

Target: Others

Cat.No: T13587

Target: Others

Cat.No: T3527

Synonym: TRC 051384

Target: HSP

Cat.No: T23454

Target: Others

Cat.No: T29021

Synonym: MW 189,MW189,TT301,TT 301,MW 189 ;MW189,MW-189

Cat.No: T22913

Target: Others

Cat.No: T76238

Cat.No: T38202

Cat.No: T37699

Cat.No: T60344

5-HT6R/MAO-B modulator 1

Cat.No: T64036

MW-150 hydrochloride

Cat.No: T39343

Synonym: MW01-18-150SRM hydrochloride,MW-150 hydrochloride

Reduced Haloperidol

Cat.No: T37167

Cat.No: T71174

UDP-α-D-Glucose (sodium salt hydrate)

Cat.No: T37898

Cat.No: T63293

Cat.No: T71576

Ganglioside GQ1b Mixture (sodium salt)

Cat.No: T35553

Ceramide Phosphoethanolamines (bovine)

Cat.No: T36188

IGF-I (24-41) (TFA)

Cat.No: T76014

Cat. No.	Product Name	Target	Signaling Pathways
T4S0498	Glaucocalyxin A 蓝萼甲素,Wangzaozin B,Leukamenin F	Apoptosis; Akt; Caspase; PI3K	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。
T5287	N-Acetyl-L-aspartic acid AC-ASP-OH,N-Acetylaspartic acid,N-乙酰-L-天门冬氨酸	Others; Endogenous Metabolite	Metabolism; Others
	N-Acetyl-L-aspartic acid (AC-ASP-OH) 是天冬氨酸的衍生物，是由氨基酸天冬氨酸和乙酰辅酶 A 在神经元中合成的。
T3S2259	Methyl eugenol 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。
T35605	Apoptolidin
	Apoptolidin is an apoptosis inducer originally isolated from Nocardiopsis bacteria. It inhibits the mitochondrial F1FO ATPase (Ki = 4-5 μM). Apoptolidin selectively kills transformed glial cells without significantly affecting untransformed cells. It also has antibiotic and antifungal actions.

天然产物

Glaucocalyxin A

Cat.No: T4S0498

Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F

Target: Apoptosis, Akt, Caspase, PI3K

N-Acetyl-L-aspartic acid

Cat.No: T5287

Synonym: AC-ASP-OH,N-Acetylaspartic acid,N-乙酰-L-天门冬氨酸

Target: Others, Endogenous Metabolite

Cat.No: T3S2259

Synonym: 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚

Target: GABA Receptor

Cat.No: T35605

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