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37

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22355	L-Thyroxine sodium 左旋甲状腺素钠,LT4 sodium,Levothyroxine sodium,L-T4 sodium	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	L-Thyroxine sodium (LT4 sodium) 是一种合成的甲状腺激素，用于研究甲状腺功能减退症。DIO 酶能够将Levothyroxine 转化成具有生物活性的三碘甲状腺氨酸 (T3)。
T19572	T4-ATA (S-isomer)	Others	Others
	T4-ATA S-isomer, the active form of the thyroid hormone, represents the S-isomer of T4-ATA.
T33576	N-Acetylthyroxine N-Acetyl-L-thyroxine,N-Acetyl-T4
	N-Acetylthyroxine is a kind of Thyroxine analogue for the treatment of diagnosing and treating diabetes.
T79925	T4 UvsX Recombinase	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	T4 UvsX Recombinase 促进双链DNA模板上DNA复制的启动，通过催化模板DNA与同源单链DNA引物间的突触形成。此酶显著增强了T4 DNA聚合酶全酶在线性单链DNA模板上进行的回跳（发夹引物）DNA合成反应。
T79924	T4 RNA ligase	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	T4 RNA ligase为一RNA连接酶，催化单链DNA分子的连接作用。该酶在酶促低核糖核苷酸合成及RNA 3'端标记过程中应用。
T69555	XUN49524
	XUN49524 also known as Vezf1-IN-T4, is an inhibitor of the pro-angiogenic activity of the zinc finger transcription factor Vezf1. XUN49524 was first reported in Molecules (2018), 23(7), 1615/1-1615/15 . This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).
T3110	PRT4165 NSC600157,PRT 4165	BMI-1; Others; E1/E2/E3 Enzyme	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; Ubiquitination
	PRT4165 (NSC600157) 是有效的 PRC1介导 H2A 泛素化的抑制剂。
T10169	5-HT4 antagonist 1	5-HT Receptor	GPCR/G Protein; Neuroscience
	5-HT4 antagonist 1 是 5-HT4 的拮抗剂 (pKi = 9.6)。
T5508	PF-AKT400 (S)-N-[[3-氨基-1-(5-乙基-7H-吡咯并[2,3-D]嘧啶-4-基)吡咯烷-3-基]甲基]-2,4-二氟苯甲酰胺,AKT protein kinase inhibitor	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	PF-AKT400 (AKT protein kinase inhibitor) 是 ATP 竞争性的、选择性的 Akt 抑制剂，对 PKBα(IC50=0.5 nM) 的选择性比 PKA(IC50=450 nM) 高 900 倍。
T77730	QST4	Antifungal	Microbiology/Virology
	QST4 具有抗结核、抗真菌活性，在结核分枝杆菌 Mycobacterium tuberculosis H37Rv 中的 MIC 值为 6.25 μM。
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。
T32036	GYKI-T412 GYKI-T 412,GYKI-T-412
	GYKI-T412 is small molecule agent with potential bioactivity. Detail information has not been published.
T14015	ST4206	Others	Others
	ST4206 is an antagonist of adenosine A2A. For adenosine A2A receptor and adenosine A1 receptor, the Kis values are 12 nM and 197 nM , respectively.
T70003	I-BET469
	I-BET469 is a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose.
T68378	PRMT4-IN-1	Histone Methyltransferase	Chromatin/Epigenetic
	PRMT4-IN-1为PRMT4高选择性抑制剂(IC50=3.2 nM)，能有效降低MCF7细胞的相对活力。
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...
T81399	PRMT4-IN-2
	PRMT4-IN-2（化合物55）是一种针对蛋白质精氨酸甲基转移酶（PRMT）系列的抑制剂，其半抑制浓度（IC50s）分别对应PRMT4为92 nM，PRMT6为436 nM，PRMT1为460 nM，PRMT8为823 nM，PRMT3为1.386 μM。
T79208	Oct4 inducer-2
	Oct4 inducer-2, 作为OCT4诱导剂，维持hiPSC形成通过促进内源性OCT4表达，适用于抗衰老研究。
T79516	BT424	Src	Angiogenesis; Tyrosine Kinase/Adaptors
	BT424是一种特异性HCK抑制剂，能够调节体外巨噬细胞的活化及自噬，并在UUO模型中改善炎症和肾纤维化。
T11420	GLUT4 activator 1	Others	Others
	GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).
T61695	GLUT4-IN-2
	GLUT4-IN-2 是一种有效的选择性 GLUT4抑制剂，对 GLUT1 和 GLUT4 的 IC50s 分别为 11.4 μM 和 6.8 μM。GLUT4-IN-2 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。GLUT4-IN-2 显示出有效的抗肿瘤活性。
T72280	PBT434 methanesulfonate
	PBT434 methanesulfonate 为一种有效、口服活性并能穿透血脑屏障的α-synuclein aggregation抑制剂，同时担任铁螯合剂和跨细胞铁运输的调节剂。该化合物抑制铁介导的氧化还原活性及α-synuclein聚集，可有效防止SNpc神经元丢失，显示出在PD研究中的应用潜力。
T37824	MCT4-IN-1 MCT4-IN-1
	MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1].
T70319	ANT431
	ANT431 is a novel metallo-β-lactamase inhibitor for the treatment of carbapenem-resistant enterobacteriaceae infections
T60836	PT4
	PT4 可治疗皮肤利什曼病 (CL) ，它通过降低线粒体膜电位并增加活性氧的产生，从而寄生虫死亡。PT4 对两种利什曼原虫均产生效果，其对L. amazonensis 和L. braziliensis 的 IC50值分别为 125.18 和 233.18 μM。PT4 同时在体内具有有效的抗炎活性。
T73390	I-BET432
	I-BET432 是一种BET 抑制剂。I-BET432 抑制BRD4的 N 端溴化域 (BD1) 和 C 端溴化域 (BD2) 的pIC50值分别为 7.5 和 7.2。I-BET432 可作为多种肿瘤和炎症疾病研究的口服候选分子。
T82464	eNOS pT495 decoy peptide
	eNOSpT495 decoy peptide是一种特异性肽，旨在阻止T495磷酸化从而减少eNOS解偶联和线粒体再分布，该肽常用于研究呼吸机诱导的肺损伤。
T79355	PRMT4-IN-3	Histone Methyltransferase	Chromatin/Epigenetic
	PRMT4-IN-3 (compound 56) 作为一种针对 I 类蛋白质精氨酸甲基转移酶 (PRMT) 的抑制剂，对 PRMT4 具有高效抑制作用，表现出对PRMT4(IC50: 37 nM) 和PRMT6(IC50: 253 nM) 的选择性。
T69438	MT477
	MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.
T1604	Tiratricol 3,3',5-Triiodothyroacetic acid,替拉曲可	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	Tiratricol (3,3',5-Triiodothyroacetic acid) 是 T3 和 T4 甲状腺激素的代谢物；促进高脂血症、局部脂肪营养不良和肥胖。它已用于研究 Allan-Herndon-Dudley 综合征治疗的试验。
T1669	Liothyronine sodium 3,3',5-Triiodo-L-thyronine sodium,Triostat,T3 Sodium salt,三碘代甲状腺素钠盐,Sodium L-3,3',5-triiodothyronine,Cytomel	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	Liothyronine sodium (3,3',5-Triiodo-L-thyronine sodium) 是甲状腺激素，能够结合并激活 β1 甲状腺激素受体。
T31475	Dihydropteroyl hexaglutamate
	Dihydropteroyl hexaglutamate is a link binding together sub-structures of the tail of Escherichia coli bacteriophage T4.
T25411	Fenclofenac R 67408,Rx 67408,R67408,Flenac
	Fenclofenac is a non-steroidal anti-inflammatory agent that competitively supresses the binding of thyroxine(T4) and triiodothyronine (T3) by thyroxine-binding globulin(TBG).
T15699	L-Thyroxine sodium salt pentahydrate 左旋甲状腺素钠五水合物,Sodium levothyroxine pentahydrate,Levothyroxine,L-甲状腺素钠五水合物	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	L-Thyroxine sodium salt pentahydrate (Levothyroxine) 是一种合成的甲状腺激素，用于甲状腺功能减退症的研究。
T82879	Biotin-hexanamide-(L-Thyroxine)
	Biotin-hexanamide-(L-Thyroxine)为生物素化L-Thyroxine化合物。该化合物中的L-Thyroxine（即Levothyroxine；T4）作为一种合成甲状腺激素，广泛用于甲状腺功能减退症的研究中。
T32500	L6Y TTR stabilizer L6
	L6Y is a transthyretin (TTR) stabilizer which binds to the T4 binding pocket of TTR and prevents the dissociation of TTR to monomer.
T80621	Semzuvolimab UB421
	Semzuvolimab是靶向T细胞表面抗原T4/Leu-3，即p55 (CD4)的鼠IgG1κ类抗体。该CD4抗体具备中和HIV感染的能力，潜在用于抑制HAART稳定型HIV感染。

化合物

L-Thyroxine sodium

Cat.No: T22355

Synonym: 左旋甲状腺素钠,LT4 sodium,Levothyroxine sodium,L-T4 sodium

Target: Thyroid hormone receptor(THR)

T4-ATA (S-isomer)

Cat.No: T19572

Target: Others

N-Acetylthyroxine

Cat.No: T33576

Synonym: N-Acetyl-L-thyroxine,N-Acetyl-T4

T4 UvsX Recombinase

Cat.No: T79925

Target: DNA/RNA Synthesis

Cat.No: T79924

Target: DNA/RNA Synthesis

Cat.No: T69555

Cat.No: T3110

Synonym: NSC600157,PRT 4165

Target: BMI-1, Others, E1/E2/E3 Enzyme

5-HT4 antagonist 1

Cat.No: T10169

Target: 5-HT Receptor

Cat.No: T5508

Synonym: (S)-N-[[3-氨基-1-(5-乙基-7H-吡咯并[2,3-D]嘧啶-4-基)吡咯烷-3-基]甲基]-2,4-二氟苯甲酰胺,AKT protein kinase inhibitor

Target: Akt

Cat.No: T77730

Target: Antifungal

Cat.No: T67733

Target: Others

Cat.No: T32036

Synonym: GYKI-T 412,GYKI-T-412

Cat.No: T14015

Target: Others

Cat.No: T70003

Cat.No: T68378

Target: Histone Methyltransferase

Cat.No: T71174

Cat.No: T81399

Cat.No: T79208

Cat.No: T79516

Target: Src

GLUT4 activator 1

Cat.No: T11420

Target: Others

Cat.No: T61695

PBT434 methanesulfonate

Cat.No: T72280

Cat.No: T37824

Synonym: MCT4-IN-1

Cat.No: T70319

Cat.No: T60836

Cat.No: T73390

eNOS pT495 decoy peptide

Cat.No: T82464

Cat.No: T79355

Target: Histone Methyltransferase

Cat.No: T69438

Cat.No: T1604

Synonym: 3,3',5-Triiodothyroacetic acid,替拉曲可

Target: Thyroid hormone receptor(THR)

Liothyronine sodium

Cat.No: T1669

Synonym: 3,3',5-Triiodo-L-thyronine sodium,Triostat,T3 Sodium salt,三碘代甲状腺素钠盐,Sodium L-3,3',5-triiodothyronine,Cytomel

Target: Thyroid hormone receptor(THR)

Dihydropteroyl hexaglutamate

Cat.No: T31475

Cat.No: T25411

Synonym: R 67408,Rx 67408,R67408,Flenac

L-Thyroxine sodium salt pentahydrate

Cat.No: T15699

Synonym: 左旋甲状腺素钠五水合物,Sodium levothyroxine pentahydrate,Levothyroxine,L-甲状腺素钠五水合物

Target: Thyroid hormone receptor(THR)

Biotin-hexanamide-(L-Thyroxine)

Cat.No: T82879

Cat.No: T32500

Synonym: TTR stabilizer L6

Cat.No: T80621

Synonym: UB421

Cat. No.	Product Name	Target	Signaling Pathways
T0864	L-Thyroxine Levothyroxine,NSC 36397,L-甲状腺素,T4	Thyroid hormone receptor(THR); Endogenous Metabolite	Endocrinology/Hormones; Metabolism
	L-Thyroxine (NSC 36397) 是一种合成的甲状腺激素，用于甲状腺功能减退症的研究。在 DIO 酶作用下，L-Thyroxine (NSC 36397) 转化成具有生物特性的三碘甲状腺氨酸(T3)。
T20557	Thyroxine sulfate T4 Sulfate
	Thyroxine sulfate is a sulfoconjugated derivative of Thyroxine and is also a metabolite of Thyroxine.
T21383L	Dextrothyroxine sodium Dextrotiroxina sodica,Lisolipin,D-T4 sodium
	Dextrothyroxine sodium is the dextrorotary isomer of thyroxine.
T21383	D-Thyroxine Dethyrona,Detyroxin,Dextroid,Dextrothyroxine;Biotirmone,Dextroxin,Biotirmone,Debetrol,Dextrothyroxine	Others	Others
	D-Thyroxine (Dextroxin) 是一种甲状腺激素，对 TSH 的分泌具有抑制作用，可用于研究高胆固醇血症。
T36715	Tetrac Tetraiodothyroacetic acid,3,3',5,5'-Tetraiodothyroacetic acid	Apoptosis; EGFR	Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Tetrac (Tetraiodothyroacetic acid)是L-甲状腺素(T4)的衍生物，是一种甲状腺整合素受体拮抗剂。Tetrac通过阻断EGFR介导的结直肠癌细胞信号传导来诱导抗增殖。Tetrac 可阻断 T4 和 3,5,3'-triiodo-L-thyronine (T3)在细胞表面甲状腺素整合素 αvβ3 受体上的作用。Tetra 具有抗血管生成、抗肿瘤活性和促凋亡活性。
T2760	(S)-2-Amino-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid dihydrate Iodogorgoic acid,apothyrin,jodgorgon,3,5-Diiodotyrosine Dihydrate,双碘酪氨酸	Others; Endogenous Metabolite	Metabolism; Others
	(S)-2-Amino-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid dihydrate (jodgorgon) 是内源性代谢产物的一种。
T4893	Spermidine N-(3-Aminopropyl)-1,4-diaminobutane,亚精胺,N-(4-Aminobutyl)-1,3-diaminopropane	Endogenous Metabolite	Metabolism
	Spermidine (N-(3-Aminopropyl)-1,4-diaminobutane) 能够维持细胞膜稳定性，提高抗氧化酶活性，改善光系统 II 以及相关基因表达。它结合并激活 NMDA，并已显示以浓度依赖性方式增强 NMDA 诱导的电流。
T11843	Levothyroxine acyl glucuronide Thyroxine acyl-β-D-glucuronide	Others	Others
	Levothyroxine acyl glucuronide (Thyroxine Acyl-β-D-glucuronide), the acyl glucuronide formation of thyroxine (T4), an endogenous metabolite.
TN3968	Epifriedelanol acetate	Others	Others
	Epifriedelanol exhibits antibacterial activities. It also can reduce cellular senescence in human primary cells and may be used to develop dietary supplements or cosmetics that modulate tissue aging or aging-associated diseases. Epifriedelanol and friedel

天然产物

Cat.No: T0864

Synonym: Levothyroxine,NSC 36397,L-甲状腺素,T4

Target: Thyroid hormone receptor(THR), Endogenous Metabolite

Thyroxine sulfate

Cat.No: T20557

Synonym: T4 Sulfate

Dextrothyroxine sodium

Cat.No: T21383L

Synonym: Dextrotiroxina sodica,Lisolipin,D-T4 sodium

Cat.No: T21383

Synonym: Dethyrona,Detyroxin,Dextroid,Dextrothyroxine;Biotirmone,Dextroxin,Biotirmone,Debetrol,Dextrothyroxine

Target: Others

Cat.No: T36715

Synonym: Tetraiodothyroacetic acid,3,3',5,5'-Tetraiodothyroacetic acid

Target: Apoptosis, EGFR

(S)-2-Amino-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid dihydrate

Cat.No: T2760

Synonym: Iodogorgoic acid,apothyrin,jodgorgon,3,5-Diiodotyrosine Dihydrate,双碘酪氨酸

Target: Others, Endogenous Metabolite

Cat.No: T4893

Synonym: N-(3-Aminopropyl)-1,4-diaminobutane,亚精胺,N-(4-Aminobutyl)-1,3-diaminopropane

Target: Endogenous Metabolite

Levothyroxine acyl glucuronide

Cat.No: T11843

Synonym: Thyroxine acyl-β-D-glucuronide

Target: Others

Epifriedelanol acetate

Cat.No: TN3968

Target: Others

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