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32

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T72285	LC kinetic stabilizer-1
	LC kinetic stabilizer-1 为一种高效、选择性的淀粉样免疫球蛋白轻链动力学稳定剂，对 WIL-FL* 与 WIL-FL*T46L/F49Y 的EC50值分别为140 nM与74.1 nM。其中，WIL-FL 为一种淀粉样变FL-LC二聚体。
T72286	LC kinetic stabilizer-2
	LC kinetic stability-2 是一种有效的淀粉样免疫球蛋白轻链 (LC) 动力学稳定剂，EC50为 24 nM。
T0699	Sulfamonomethoxine 磺胺间甲氧嘧啶,磺胺间甲氧嘧啶钠	Antibacterial; Antibiotic	Microbiology/Virology
	Sulfamonomethoxine 是一种磺胺类抗菌剂。它可研究血液动力学，竞争性抑制剂二氢叶酸合成，从而阻断叶酸合成。
T18888	4-Methylumbelliferyl phosphate 4-甲基伞形酮磷酸酯,4-MUP	Others	Others
	4-Methylumbelliferyl phosphate (4-MUP) 是碱性磷酸酶的荧光底物。
T76306	Adipokinetic hormone I (Locusta migratoria)
	Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I) 是昆虫脂肪运动激素(AKH)类，可促进脂肪体内cAMP水平升高。AKH通过与AKH受体结合，并通过刺激性鸟嘌呤核苷酸结合蛋白(Gs)偶联，促进cAMP生成及糖原磷酸化酶活化，从而控制飞蝗动员脂肪体存储的碳水化合物和脂质。
T83165	Adipokinetic hormone (Manduca sexta) Manse-AKH
	Adipokinetic Hormone (Apis mellifera ligustica, Bombyx mori, Heliothis zea, Manduca sexta) 是昆虫肽类激素，能强烈诱导促脂肪/高海藻素反应，但不具备糖原动员功能，亦不能在脂肪体内有效储存及利用糖原。
T76304	Adipokinetic hormone II (Locusta migratoria)
	Adipokinetic hormone II (Locusta migratoria) (Lom-AKH-II)，一昆虫AKH，可提升脂肪体cAMP水平。AKHs通过其受体和Gs蛋白相互作用，增强cAMP生成与糖原磷酸化酶活性，从而直接调控飞蝗脂肪体中碳水化合物与脂质的动员。
TP1757	Adipokinetic Hormone (AKH) (24-32), locust
	Adipokinetic Hormone (AKH) (24-32), locust is a peptide hormone isolated from locusts.
T83167	Adipokinetic Hormone (AKH) (24-32), locust TFA
	Adipokinetic Hormone (AKH) (24-32), locust (TFA)，是从蝗虫心脏分离的一种神经激素，调节飞行过程中的脂质利用。
T76655	Prokineticin 2 Isoform 2 (human)
	Prokineticin 2 Isoform 2 (human) 为一下丘脑神经肽，能减少食物摄入，并在啮齿动物的体温调节与能量代谢中发挥作用。此外，Prokineticin 2 对高血糖、代谢综合征 (MetS) 及肥胖研究具有潜在价值。
T83166	Adipokinetic hormone (Gryllus bimaculatus) Grybi-AKH
	Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH) 是调节昆虫能量平衡的脂肪动力激素，主要功能是动员脂肪体内的脂质和碳水化合物。此外，Grybi-AKH也能增强双斑蟋蟀的运动活性，并在人体体重调节、体重减轻及糖原贮积障碍缓解的研究中具有应用潜力。
T9447	AG-10 Acoramidis	Others	Others
	AG-10 (Acoramidis) 是选择性的、口服有效的甲状腺素转运蛋白 (TTR (transthyretin)) 的稳定剂，显示出对野生型和 V1221 突变型均有效。
T39740	Acoramidis hydrochloride AG10 hydrochloride,Alxn2060 hydrochloride	Others	Others
	Acoramidis hydrochloride (Alxn2060 hydrochloride) 是具有口服活性的、选择性的甲状腺素转运蛋白 (TTR (transthyretin)) 的稳定剂，对野生型和 V1221 突变型均有效。Acoramidis hydrochloride 可用于转体甲状腺素淀粉样变性的研究。
T7582	tafamidis meglumine Fx-1006A,他发米帝司甲葡胺	Others	Others
	Tafamidis meglumine (Fx-1006A) 是transthyretin (TTR)的选择性稳定剂，对野生型 WT-TTR 和突变型同源四聚体 V30M-TTR，V122I-TTR 的活性相当，EC50值为 2.7-3.2 μM。它能够阻碍淀粉样蛋白的生成。
T9361	5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione 5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione	Others	Others
	5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione (5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) 是一种合成化合物。它已被用作催化剂以及酶动力学研究中的工具；还被用于酶抑制的研究，以及药物受体相互作用的研究。
T21537L	TMC647055 Choline Hydroxide Salt TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂，可用于治疗 HCV 感染。它具有纳摩尔级细胞效力（EC(50) 为 82 nM），相关细胞毒性较小（CC(50)>20 μM），在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。
T4565	Tafamidis 他发米帝司甲葡胺,氯苯唑酸,Fx-1006A	Others	Others
	Tafamidis (Fx-1006A) 是选择性的transthyretin (TTR)稳定剂，对野生型 WT-TTR 、突变型同源四聚体 V30M-TTR、V122I-TTR 的活性相当，它们的EC50值为2.7-3.2 μM。它对淀粉样蛋白的生成具有抑制作用。
T6707	Tiotropium Bromide hydrate BA-679 BR hydrate,BA 679BR,噻托溴铵一水合物	AChR	Neuroscience
	Tiotropium Bromide hydrate (BA-679 BR hydrate) 是长效的毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性气道疾病 (COPD)。
T24001	Diisopropyl tartrate Diisopropyl (+)-L-tartrate,L-DIPT,BRN 1727863
	Diisopropyl tartrate is a reagent for kinetic resolution of racemic allylic alcohols and α-furfuryl amides. It acts by enantioselective epoxidation.
T78233	Sulfamonomethoxine sodium	Antibiotic	Microbiology/Virology
	Sulfamonomethoxine sodium用作血液动力学研究中的竞争性抑制剂，通过抑制二氢叶酸合成，进而阻断叶酸的生成。
T68192	OK-1035
	OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.
T26964	CBS-3595 CBS3595
	CBS-3595 is a potent and dual Inhibitor of p38α MAPK/PDE-4 with a superior profile regarding its anti-inflammatory effects. CBS-3595 features moderate inhibition of p38α MAPK and PDE-4 in the higher nanomolar range in combination with excellent kinetic pr
T13032	Sulfamonomethoxine-d4	Others	Others
	Sulfamonomethoxine D4 is a deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is an agent of long acting sulfonamide antibacterial, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
T60255	α-Amylase/α-Glucosidase-IN-1
	α-Amylase/α-Glucosidase-IN-1 (compound 33) 是一种有效的α-淀粉酶/α-葡萄糖苷酶抑制剂，对α-淀粉酶和 α-葡萄糖苷酶的IC50值分别为 2.01、2.09 μM。动力学研究预测α-Amylase/α-Glucosidase-IN-1 具有抗高血糖的潜力。
T37797	Coumarin-Quinone Conjugate
	Coumarin-quinone conjugate is a fluorescent substrate for NADH:ubiquinone oxidoreductases.1It is comprised of a coumarin fluorophore conjugated to a ubiquinone analog that can be reduced by NADH:ubiquinone oxidoreductases. It has been used to measure the kinetic parameters of apoptosis-inducing factor mitochondria-associated 2/ferroptosis suppressor protein 1 (AIFM2/FSP1). 1.Doll, S., Freitas, F.P., Shah, R., et al.FSP1 is a glutathione-independent ferroptosis suppressorNature575(7784)693-698(20...
T70639	AM-9514
	AM-9514 is a novel, potent Glucokinase (GK) activator. AM-9514 showed a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in preclinical species, and robust efficacy in a rodent PD model. Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis.
T71000	RO-5328673
	RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of g...
T70538	PD-85639
	PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membr...
T35572	Adenosine 3',5'-diphosphate sodium salt 3'-Phosphoadenosine 5'-phosphate	Endogenous Metabolite	Metabolism
	Adenosine 3',5'-diphosphate sodium salt 是一种羟类固醇磺基转移酶 (hydroxysteroid sulfotransferases) 抑制剂，是一种腺嘌呤核苷酸，在戊糖核糖的 3'和 5'位置含有一个磷酸基团。Adenosine 3',5'-diphosphate (sodium salt)是 3'-phosphoadenosine 5'-phosphosulfonate (PAPS) 的产物，是磺基转移酶（SULTs）的辅助因子，已被用于研究 SULTs 的动力学特性和结构。
T37585	Ensartinib
	Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N...
T36679	Rp-cAMPS sodium salt
	Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t...
T35416	α-D-Glucose-1-phosphate (sodium salt hydrate)
	α-D-Glucose-1-phosphate is an intermediate in glycogen metabolism.1,2It is a precursor in the biosynthesis of UDP-glucose, the glucose donor in glycogen biosynthesis.2α-D-Glucose-1-phosphate can be formed during glycogen breakdownviaphosphorolytic cleavage of glycogen by glycogen phosphorylase.1It can be converted to glucose-6-phosphate by phosphoglucomutase. α-D-Glucose-1-phosphate is combined with CTP by α-D-glucose-1-phosphate cytidylyltransferase to form CDP-glucose in the first step of CDP-...

化合物

LC kinetic stabilizer-1

Cat.No: T72285

LC kinetic stabilizer-2

Cat.No: T72286

Sulfamonomethoxine

Cat.No: T0699

Synonym: 磺胺间甲氧嘧啶,磺胺间甲氧嘧啶钠

Target: Antibacterial, Antibiotic

4-Methylumbelliferyl phosphate

Cat.No: T18888

Synonym: 4-甲基伞形酮磷酸酯,4-MUP

Target: Others

Adipokinetic hormone I (Locusta migratoria)

Cat.No: T76306

Adipokinetic hormone (Manduca sexta)

Cat.No: T83165

Synonym: Manse-AKH

Adipokinetic hormone II (Locusta migratoria)

Cat.No: T76304

Adipokinetic Hormone (AKH) (24-32), locust

Cat.No: TP1757

Adipokinetic Hormone (AKH) (24-32), locust TFA

Cat.No: T83167

Prokineticin 2 Isoform 2 (human)

Cat.No: T76655

Adipokinetic hormone (Gryllus bimaculatus)

Cat.No: T83166

Synonym: Grybi-AKH

Cat.No: T9447

Synonym: Acoramidis

Target: Others

Acoramidis hydrochloride

Cat.No: T39740

Synonym: AG10 hydrochloride,Alxn2060 hydrochloride

Target: Others

tafamidis meglumine

Cat.No: T7582

Synonym: Fx-1006A,他发米帝司甲葡胺

Target: Others

5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione

Cat.No: T9361

Synonym: 5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

Target: Others

TMC647055 Choline Hydroxide Salt

Cat.No: T21537L

Synonym: TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)

Target: HCV Protease

Cat.No: T4565

Synonym: 他发米帝司甲葡胺,氯苯唑酸,Fx-1006A

Target: Others

Tiotropium Bromide hydrate

Cat.No: T6707

Synonym: BA-679 BR hydrate,BA 679BR,噻托溴铵一水合物

Target: AChR

Diisopropyl tartrate

Cat.No: T24001

Synonym: Diisopropyl (+)-L-tartrate,L-DIPT,BRN 1727863

Sulfamonomethoxine sodium

Cat.No: T78233

Target: Antibiotic

Cat.No: T68192

Cat.No: T26964

Synonym: CBS3595

Sulfamonomethoxine-d4

Cat.No: T13032

Target: Others

α-Amylase/α-Glucosidase-IN-1

Cat.No: T60255

Coumarin-Quinone Conjugate

Cat.No: T37797

Cat.No: T70639

Cat.No: T71000

Cat.No: T70538

Adenosine 3',5'-diphosphate sodium salt

Cat.No: T35572

Synonym: 3'-Phosphoadenosine 5'-phosphate

Target: Endogenous Metabolite

Cat.No: T37585

Rp-cAMPS sodium salt

Cat.No: T36679

α-D-Glucose-1-phosphate (sodium salt hydrate)

Cat.No: T35416

Cat. No.	Product Name	Target	Signaling Pathways
T4S0145	Corylifol A Corylinin,补骨脂异黄酮A	hCE; STAT; UGT	JAK/STAT signaling; Metabolism; Stem Cells
	Corylifol A (Corylinin) 是补骨脂中的一种天然产物，可抑制IL-6 诱导的STAT3激活和磷酸化，IC50值为0.81 μM。
T36448	(E)-Ajoene
	(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth...

天然产物

Cat.No: T4S0145

Synonym: Corylinin,补骨脂异黄酮A

Target: hCE, STAT, UGT

Cat.No: T36448

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