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28

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9063	Clathrin-IN-1	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Clathrin-IN-1 是一种网格蛋白抑制剂，可通过与网格蛋白的末端域相关联来抑制网格蛋白介导的内吞作用，有潜力用于抗癌的研究。
T6822	Hydroxy-Dynasore Dyngo-4a	Dynamin	Cytoskeletal Signaling
	Hydroxy-Dynasore (Dyngo-4a) 是 Dynasore 结构模拟类似物，是一种改进的，低细胞毒性的 dynamin 通用抑制剂，抑制 dynamin 依赖性转铁蛋白的内吞作用的 IC50为 5.7 μM，对大脑重组 dynamin I 和重组鼠 dynamin II 的 IC50值分别为 0.38 μM 和 2.3μM。
T8513	Spastazoline	Others	Others
	Spastazoline 是spastin(一种微管切断AAA 蛋白) 的选择性抑制剂，对人 spastin 的IC50值为 99 nM。它不能影响重组人 VPS4 的 ATPase 活性。
T0192	Levetiracetam 左乙拉西坦,UCB L059,SIB-S1	DNA Methyltransferase; Others; Calcium Channel	Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; Others
	Levetiracetam (SIB-S1) 是一种化学增敏剂，增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平，最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药，可结合突触小泡蛋白 SV2A。
T20789	S-23 (S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide,S23	Androgen Receptor	Endocrinology/Hormones
	S-23 ((S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide) 是口服选择性雄激素受体调节剂(Ki:1.7 nM)。它能够诱导 CV-1 细胞雄激素受体介导的转录激活，提高去势大鼠前列腺、精囊和肛提肌重量。
T74305	14:0 PEG2000 PE DMPE-PEG2000	Others	Others
	14: 0 PEG2000 PE (DMPE-PEG2000) 是一种聚乙二醇（PEG）-磷脂偶联物，可在制备囊泡制剂时阻止囊泡聚集，可用于制备纳米结构脂质载体。
T26357	Pitstop 2	Apoptosis	Apoptosis
	Pitstop2 是一种选择性的两性蛋白结合的网格蛋白末端结构域抑制剂，IC50 值为 12 μM。 Pitstop2 严重干扰受体介导的内吞作用、HIV 进入和突触小泡循环。
T0719	Tetrabenazine Xenazine,丁苯那嗪,Ro 1-9569	Others; Dopamine Receptor; Monoamine Transporter	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience; Others
	Tetrabenazine (Ro 1-9569) 是 VMAT 抑制剂，用作抗精神病药和治疗各种运动障碍。
T7724	Tepoxalin RWJ-20485,RWJ20485,ORF20485,替泊沙林,ORF-20485,RWJ 20485,ORF 20485	Lipoxygenase; COX	Immunology/Inflammation; Metabolism; Neuroscience
	Tepoxalin (RWJ 20485) 是有效的5-脂氧合酶和环氧合酶抑制剂，表现出强大的抗炎活性和较小的胃肠道刺激性。
T3534	Tetrabenazine Racemate Nitoman,丁苯那嗪外消旋体,丁苯那嗪,Ro 1-9569 Racemate,Rubigen,TETRABENAZINE	Monoamine Transporter	Membrane transporter/Ion channel
	Tetrabenazine Racemate (Rubigen) 是一种选择性和可逆的囊泡单胺转运蛋白 2(VMAT-2) 抑制剂。它阻断神经递质吸收到肾上腺素能储存囊泡中，并已被用作囊泡运输系统的高亲和力标记。
T14855	Calcein Fluorexon,钙黄绿素	Others	Others
	Calcein (Fluorexon) 是一种荧光染料和自灭探针，是一种脂囊泡渗漏的指示剂，也是一种 EDTA 钙离子滴定和荧光测定钙离子的络合指示剂。
T76251L	Ac-FEID-CMK TFA	Pyroptosis	Apoptosis; Immunology/Inflammation
	Ac-FEID-CMK TFA 是一种选择性斑马鱼 GSDMEb 衍生肽抑制剂，可减少感染性休克的死亡率和肾损伤。Ac-FEID-CMK TFA 在体内可抑制焦亡，缓解败血性 AKI (急性肾损伤)，抑制 caspy2 介导的非典型炎症小体通路发挥作用。
T6887	MCC950 sodium CRID3 sodium salt,CP-456773,CP-456773 sodium,MCC950	NOD-like Receptor (NLR); NOD	Immunology/Inflammation; NF-κB
	MCC950 sodium (CP-456773 sodium) 是一种炎症小体 NLRP3 的抑制剂 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs)，具有高效选择性。MCC950 sodium 对其他炎症小体，如 AIM2、 NLRC4 或 NLRP1 没有作用。
T37020	Endosidin-2 ES2,Endosidin 2
	Endosidin-2是一种囊外囊抑制剂,具有细胞渗透性的亚苄基苯甲酰肼，可与外囊复合体70 kDa（EXO70）亚基的外囊成分结合（Kd = 253 μM，EXO70A1）。Endosidin-2会破坏蛋白质在内质体和质膜之间的转运，从而促进蛋白质转运至液泡降解。它还能抑制 HeLa 细胞中内吞转铁蛋白向质膜的再循环，并能靶向哺乳动物 EXO70的多种异构体，导致外泌失调。Endosidin2 可作为工具分子研究胞吐。
T35856	BMS-986176	AAK1 (AP2 associated kinase 1)	Neuroscience
	BMS-986176 是一种有效的AAK1 抑制剂，IC50为 2.2 nM。BMS-986176在神经退行性疾病中有研究的价值。
T69069	Endosidin1
	Endosidin1 is a natural vesicle trafficking inhibitor.
T39069	UCB-J
	UCB-J is a radioligand for the synaptic vesicle protein 2A (SV2A), utilized in positron emission tomography (PET)[4].
T38407	RTIL 13
	RTIL 13 is a highly effective inhibitor of dynamin GTPase, exhibiting an IC50 value of 2.3 μM for dynamin I GTPase. Furthermore, it selectively interacts with the pleckstrin homology lipid binding domain. This compound effectively suppresses both receptor-mediated and synaptic vesicle endocytosis, demonstrating IC50 values of 9.3 μM and 7.1 μM, respectively.
T26260	Tetrabenazine methanesulfonate NSC169886,NSC 169886,NSC-169886
	Tetrabenazine methanesulfonate is a medicine formerly utilized as an antipsychotic and therapy for various movement disorders. Tetrabenazine methanesulfonate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affin
T41193	FFN 270
	FFN 270 is a fluorescent false neurotransmitter (FFN). Fluorescent substrate for NET and VMAT2. Labels noradrenergic neurons and their synaptic vesicles, and enables imaging of synaptic vesicle content release from specific axonal sitesin vivo. Selectively labels NA neurons over other monoamine and CNS targets. Exhibits two resolved absorption/excitation maxima depending on solvent pH (excitation maxima: 320 nm or 365 nm, emission maxima: 475 nm).
T62182	NIC-0102
	NIC-0102 是一种口服具有活力的蛋白酶体 (proteasome) 抑制剂 (pIC50:7.55)，对 NLRP3 炎症小体激活表现出特异性抑制作用。NIC-0102 对 DSS 诱导的溃疡性结肠炎模型表现出有效的体内抗炎活性。NIC-0102 对前 IL-1β 的产生具有抑制作用。
T36912	17α,20β-Dihydroxy-4-pregnen-3-one 17α,20β-dihydroxy Progesterone,17α,20β-DHP,17α,20β-Dihydroxy-4-pregnen-3-one
	17α,20β-Dihydroxy-4-pregnen-3-one (17α,20β-DHP) is an endogenous, maturation-inducing steroid that stimulates oocyte maturation in females of several teleost species. For example, 1 μg/ml of 17α,20β-DHP applied to Persian sturgeon oocytes has been shown to effectively induce germinal vesicle breakdown, an essential step during oocyte maturation.1 Gonadotropin-releasing hormone and the gonadotropins, follicle-stimulating hormone and luteinizing hormone, have been shown to stimulate the production...
T37691	Phosphatidic Acids (egg) (ammonium salt)
	Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular ...
T79756	Beclin1-ATG14L interaction inhibitor 1	Autophagy	Autophagy
	Beclin1-ATG14L interaction inhibitor 1 (com 19) 作为一种选择性抑制剂，特定抑制脂质激酶VPS34的复合物 I 中Beclin1与ATG14L的相互作用，而对Beclin 1-UVRAG作用重要的VPS34复合物 II 无影响。由此，其阻断VPS34复合物 I 形成，抑制自噬过程，但不干扰复合物 II 介导的囊泡运输。
T83891	Sulfonadyn-47
	Sulfonadyn-47是一种dynamin抑制剂，能在无细胞测定中抑制dynamin的GTP酶活性（IC50 = 3.5 µM）。在U2OS细胞中，Sulfonadyn-47抑制clathrin介导的内吞作用（IC50 = 27.3 µM），同时在分离的大鼠脑突触体中抑制由去极化刺激的FM4-64摄取，后者是突触小泡内吞（SVE）的标志（IC50 = 12.3 µM）。在体内，Sulfonadyn-47（30和60 mg/kg）在6 Hz角膜电引发小鼠癫痫模型中具有抗惊厥活性。
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
T35790	Palmitic acid-1,2,3,4-13C4 Palmitic Acid-13C (C1, C2, C3, and C4 labeled)
	Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellula...
T37741	N-hexadecanoyl-L-Homoserine lactone C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone
	Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which...

化合物

Cat.No: T9063

Target: HIV Protease

Hydroxy-Dynasore

Cat.No: T6822

Synonym: Dyngo-4a

Target: Dynamin

Cat.No: T8513

Target: Others

Cat.No: T0192

Synonym: 左乙拉西坦,UCB L059,SIB-S1

Target: DNA Methyltransferase, Others, Calcium Channel

Cat.No: T20789

Synonym: (S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide,S23

Target: Androgen Receptor

14:0 PEG2000 PE

Cat.No: T74305

Synonym: DMPE-PEG2000

Target: Others

Cat.No: T26357

Target: Apoptosis

Cat.No: T0719

Synonym: Xenazine,丁苯那嗪,Ro 1-9569

Target: Others, Dopamine Receptor, Monoamine Transporter

Cat.No: T7724

Synonym: RWJ-20485,RWJ20485,ORF20485,替泊沙林,ORF-20485,RWJ 20485,ORF 20485

Target: Lipoxygenase, COX

Tetrabenazine Racemate

Cat.No: T3534

Synonym: Nitoman,丁苯那嗪外消旋体,丁苯那嗪,Ro 1-9569 Racemate,Rubigen,TETRABENAZINE

Target: Monoamine Transporter

Cat.No: T14855

Synonym: Fluorexon,钙黄绿素

Target: Others

Ac-FEID-CMK TFA

Cat.No: T76251L

Target: Pyroptosis

Cat.No: T6887

Synonym: CRID3 sodium salt,CP-456773,CP-456773 sodium,MCC950

Target: NOD-like Receptor (NLR), NOD

Cat.No: T37020

Synonym: ES2,Endosidin 2

Cat.No: T35856

Target: AAK1 (AP2 associated kinase 1)

Cat.No: T69069

Cat.No: T39069

Cat.No: T38407

Tetrabenazine methanesulfonate

Cat.No: T26260

Synonym: NSC169886,NSC 169886,NSC-169886

Cat.No: T41193

Cat.No: T62182

17α,20β-Dihydroxy-4-pregnen-3-one

Cat.No: T36912

Synonym: 17α,20β-dihydroxy Progesterone,17α,20β-DHP,17α,20β-Dihydroxy-4-pregnen-3-one

Phosphatidic Acids (egg) (ammonium salt)

Cat.No: T37691

Beclin1-ATG14L interaction inhibitor 1

Cat.No: T79756

Target: Autophagy

Cat.No: T83891

AMK (hydrochloride)

Cat.No: T36176

Palmitic acid-1,2,3,4-13C4

Cat.No: T35790

Synonym: Palmitic Acid-13C (C1, C2, C3, and C4 labeled)

N-hexadecanoyl-L-Homoserine lactone

Cat.No: T37741

Synonym: C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone

Cat. No.	Product Name	Target	Signaling Pathways
T19711	Desmosterol Desmesterol,24-Dehydrocholesterol	Endogenous Metabolite	Metabolism
	Desmosterol(24-Dehydrocholesterol) 是一种胆固醇生物合成中间体，抑制巨噬细胞炎症小体活化，防止血管炎症和动脉粥样硬化。
T4969	Guanosine 5'-triphosphate trisodium salt 鸟苷-5'-三磷酸三钠盐,GTP Trisodium salt,5'-GTP trisodium salt	Endogenous Metabolite	Metabolism
	Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) 为G蛋白(G proteins)信号转导过程中的活化剂。

天然产物

Cat.No: T19711

Synonym: Desmesterol,24-Dehydrocholesterol

Target: Endogenous Metabolite

Guanosine 5'-triphosphate trisodium salt

Cat.No: T4969

Synonym: 鸟苷-5'-三磷酸三钠盐,GTP Trisodium salt,5'-GTP trisodium salt

Target: Endogenous Metabolite

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