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18

抑制剂 & 化合物

9

天然产物

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Cat. No. Product Name Target Signaling Pathways
T39785L TH5427

NUDIX hydrolase Metabolism
TH5427 在 NUDT5 活性和 ADP-核糖代谢中有研究的价值。它阻断孕激素依赖性、PAR 衍生的核 ATP 合成以及随后的乳腺癌细胞染色质重塑、基因调控和增殖。NUDT5是乳腺癌细胞激素依赖性基因调控和增殖的变阻器。
T16290 NIK SMI1

NF-κB NF-κB
NIK SMI1 是 NF-κB 诱导激酶 (NIK) 的选择性抑制剂,能够抑制 NIK 催化的 ATP 水解为 ADP,IC50=0.23±0.17 nM。
T7424 NDI-091143

ATP Citrate Lyase Metabolism
NDI-091143 是高亲和力人 ATP 柠檬酸裂解酶抑制剂,其IC50为 2.1 nM (ADP-Glo 分析),Ki 为 7.0 nM,Kd 为 2.2 nM。它能够稳定柠檬酸盐域中的大构象变化,间接抑制柠檬酸的结合和识别,进而抑制ACLY 催化变构反应。
T72060 Myosin V-IN-1

Myosin Cytoskeletal Signaling
Myosin V-IN-1是一种有效且具有选择性的 Myosin V 抑制剂,Ki 值为 6 μM。Myosin V-IN-1 抑制肌动蛋白 V 发生作用, 通过选择性抑制肌动球蛋白复合物释放 ADP 来减缓肌动蛋白激活的肌球蛋白 V ATP 酶。
T0993 Methoxamine hydrochloride

Methoxamine HCl,盐酸甲氧明

Adrenergic Receptor GPCR/G Protein; Neuroscience
Methoxamine hydrochloride (Methoxamine HCl) 是一种 alpha1 肾上腺素能受体的选择性激动剂。它通过 Prazosin 敏感机制在兔肺动脉显著增加 ATPADP 和 AMP 的溢出,但不增加腺苷的溢出。它引起血管收缩和外周血管阻力增加。
T76113 Creatine kinase (OcCK)

Creatine kinase (OcCK) 催化肌酸和 ATP 的可逆反应,形成磷酸肌酸和 ADP。Creatine kinase (OcCK) 是在快速能量周转期间维持恒定 ATP/ADP 比率的关键酶。
T76115 Pyruvate kinase

Pyruvate kinase 是一种糖酵解酶,催化磷酸烯醇式丙酮酸和 ADP 转化为丙酮酸和 ATP
T39890 8-Bromo-AMP

8-Bromoadenosine 5'-monophosphate,8-Bromo-AMP,8-Bromoadenylicacid

8-Bromo-AMP, also known as 8-Bromoadenosine 5'-monophosphate, is a membrane permeable cAMP analogue. It enhances cardiac recovery from ischemia and reperfusion by elevating ATP, ADP, and total adenine nucleotide concentrations.
T40455 8-NH2-ATP

8-Aminoadenosine-5'-O-triphosphate,8-NH2-ATP

8-NH2-ATP is an inactive derivative of adenosine triphosphate (ATP), synthesized from 8-NH2-Ado. It has been documented that 8-NH2-Ado exhibits potent properties, as evidenced by its ability to induce apoptosis-associated cleavage of poly(ADP-ribose) polymerase.
T75403 Glucuronokinase (AtGlcAK)

Glucuronokinase (AtGlcAK) 为GHMP激酶家族的一员。其对D-葡萄糖醛酸表现出独有的底物特异性,具有0.7 mM的Km值。Glucuronokinase (AtGlcAK) 能催化D-葡萄糖醛酸与ATP反应生成D-葡萄糖醛酸-1-磷酸和ADP
T83813 8-Azidoadenosine-5'-O-diphosphate sodium

8-azido-ADP,Click Tag™ 8-Azidoadenosine-5'-O-diphosphate

8-Azidoadenosine-5'-O-diphosphate(8-azido-ADP)是ATP前体和嘌呤受体配体ADP的可点击形式。8-azido-ADP的放射性标记形式已被用作各种蛋白质的光亲和标签,包括从牛脑中分离的谷氨酸脱氢酶(GDH)同工酶,以及从兔网织红细胞中分离的真核翻译起始因子2(eIF2)和鸟苷核苷酸交换因子(GEF)。
T76122 Phosphoglycerate kinase

Phosphoglycerate kinase(PGK),即磷酸甘油酸激酶,是一种糖酵解酶,常用于生化研究。Phosphoglycerate kinase 可以催化磷酸基团从1,3-二磷酸甘油酸(1,3-BPG)到ADP 的可逆转移,从而产生 3-磷酸甘油酸(3-PG) 和 ATP。同时也可以参与糖异生,催化相反的反应产生 1,3BPGA 和ADP。Phosphoglycerate kinase 参与了能量代谢、与核酸的相互作用、肿瘤发生进展、细胞死亡和病毒复制等相关过程。
T70335 Cangrelor free acid

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor’s immediate effect after infusion, and the therapeutic effects can be maintained with...
T83808 Sp-Adenosine-5'-O-(1-thiotriphosphate) sodium

Sp-ATP-α-S

Sp-Adenosine-5'-O-(1-thiotriphosphate) (Sp-ATP-α-S) 是一种含硫核苷酸衍生物 ATP-α-S 的异构体,也是嘌呤P2Y1受体的激动剂。在表达P2Y1受体的HEK293细胞中增加钙离子的流动(对人类受体的EC50 = 9.4 nM)。Sp-ATP-α-S 抑制了ADP诱导的孤立人类血小板聚集(Ki = 4 μM)。它还能引起经卡巴胆碱预收缩的豚鼠十二指肠松弛(EC50 = 426 nM)。
T74510 TFMU-ADPr

TFMU-ADPr作为监测聚ATP-核糖糖水解酶(PARG)活性的底物,以其释放的荧光团直接反映PAR水解酶总活性而常用。该化合物因具备优良的反应性、通用性、稳定性及易用性,成为体外评估小分子抑制剂及研究ATP-核糖基分解代谢酶调控的首选工具。
T74511 TFMU-ADPr triethylamine

TFMU-ADPr triethylamine 作为监测聚 ATP-核糖糖水解酶 (PARG) 活性的标准底物,能够通过释放荧光团直接报告 PAR 水解酶的总活性。其特点包括高反应性、广泛的通用性、稳定性以及便于使用,使其成为体外评估小分子抑制剂以及研究 ATP-核糖基分解代谢酶调控的优选工具。
T83807 Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium

Rp-ATP-α-S

Rp-Adenosine-5'-O-(1-thiotriphosphate)(Rp-ATP-α-S)是一种含硫核苷酸衍生物ATP-α-S的异构体,同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中,Rp-ATP-α-S能增加钙的动员(EC50 = 75 nM)。该化合物与洗涤的人类孤立血小板结合(Ki = 156 nM),抑制由ADP引发的人类富血小板血浆(PRP)的聚集(pA2 = 4.74),并且能够抑制前列腺素E1(PGE1)在人类孤立PRP中引发的cAMP产生(pA2 = 5.26)。同时,Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛(EC50 = 56 nM)。此外,Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。
T83785 2-Chloroadenosine-5'-O-diphosphate sodium

2-chloro ADP

2-Chloroadenosine-5'-O-diphosphate是一种腺苷5'二磷酸(ADP)的衍生物。它在浓度依赖性的方式下,促进了人类富含血小板的血浆中的聚集,并抑制了由前列腺素E2(PGE2)诱导的环磷酸腺苷(cAMP)的产生。2-Chloroadenosine-5'-O-diphosphate引起预收缩的孤立的豚鼠taenia coli条带放松(pD2 = 6.74),降低大鼠的动脉血压。此外,它还抑制了热休克蛋白70(Hsp70)家族成员mortalin的ATP酶活性(人类酶的表观Ki = 45.05 µM)。

化合物

TH5427
Cat.No: T39785L
Synonym:
Target: NUDIX hydrolase
NIK SMI1
Cat.No: T16290
Synonym:
Target: NF-κB
NDI-091143
Cat.No: T7424
Synonym:
Target: ATP Citrate Lyase
Myosin V-IN-1
Cat.No: T72060
Synonym:
Target: Myosin
Methoxamine hydrochloride
Cat.No: T0993
Synonym: Methoxamine HCl,盐酸甲氧明
Target: Adrenergic Receptor
Creatine kinase (OcCK)
Cat.No: T76113
Synonym:
Target:
Pyruvate kinase
Cat.No: T76115
Synonym:
Target:
8-Bromo-AMP
Cat.No: T39890
Synonym: 8-Bromoadenosine 5'-monophosphate,8-Bromo-AMP,8-Bromoadenylicacid
Target:
8-NH2-ATP
Cat.No: T40455
Synonym: 8-Aminoadenosine-5'-O-triphosphate,8-NH2-ATP
Target:
Glucuronokinase (AtGlcAK)
Cat.No: T75403
Synonym:
Target:
8-Azidoadenosine-5'-O-diphosphate sodium
Cat.No: T83813
Synonym: 8-azido-ADP,Click Tag™ 8-Azidoadenosine-5'-O-diphosphate
Target:
Phosphoglycerate kinase
Cat.No: T76122
Synonym:
Target:
Cangrelor free acid
Cat.No: T70335
Synonym:
Target:
Sp-Adenosine-5'-O-(1-thiotriphosphate) sodium
Cat.No: T83808
Synonym: Sp-ATP-α-S
Target:
TFMU-ADPr
Cat.No: T74510
Synonym:
Target:
TFMU-ADPr triethylamine
Cat.No: T74511
Synonym:
Target:
Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium
Cat.No: T83807
Synonym: Rp-ATP-α-S
Target:
2-Chloroadenosine-5'-O-diphosphate sodium
Cat.No: T83785
Synonym: 2-chloro ADP
Target:
Cat. No. Product Name Target Signaling Pathways
T3S0156 Atractyloside potassium salt

Atractyloside Dipotassium Salt,苍术苷钾盐,苍术苷二钾盐

Others Others
Atractyloside potassium salt (Atractyloside Dipotassium Salt) 是一种从苍术果实中分离出得到的二萜苷类化合物,具有毒性。它能抑制大鼠心脏线粒体膜的氯离子通道。它是高效、特异性的线粒体 ADP/ATP 转运 (ADP/ATP transport) 抑制剂。
T8170 Carboxyatractyloside

羧基苍术苷,Gummiferin,Carboxyatractyloside tripotassium salt

Others Others
Carboxyatractyloside (Carboxyatractyloside tripotassium salt) tripotassium salt 是一种 ADP/ATP 载体蛋白 (ADP/ATP carrier) 抑制剂,抑制线粒体 ADP/ATP 的转运。它是一种具有毒性的天然产物,
T4888 Phosphocreatine disodium hydrate

磷酸肌酸二钠盐,Phosphocreatine disodium salt hydrate

Others; Endogenous Metabolite Metabolism; Others
Phosphocreatine disodium hydrate 是内源性代谢产物的一种。
T5079 Adenosine 5'-diphosphate sodium salt

腺苷-5‘-二磷酸钠盐,Adenosine-5'-diphosphate trisodium salt,ADP sodium salt

Others; Endogenous Metabolite Metabolism; Others
Adenosine 5'-diphosphate sodium salt (ADP sodium salt) 是一种核苷二磷酸,是一种 ATP 酶对 ATP 去磷酸化的产物。它通过在 P2T-嘌呤受体上的作用诱导人血小板聚集并抑制刺激的腺苷酸环化酶。
T1723 Adenosine 5'-diphosphate

腺苷5'-二磷酸,Adenosine diphosphate,adenosine pyrophosphate,ADP

Endogenous Metabolite Metabolism
Adenosine 5'-diphosphate (ADP) 是一种嘌呤核糖核苷5'-二磷酸,是 ATPATP 酶作用下去磷酸化的产物。Adenosine 5'-diphosphate (adenosine pyrophosphate) 可诱导人血小板聚集并通过作用于P2T-嘌呤受体抑制受刺激的腺苷酸环化酶。
T4786 D-Ribose(mixture of isomers)

D-Ribose,D-(-)-Ribose,D-(-)-核糖

Others; Endogenous Metabolite Metabolism; Others
D-Ribose(mixture of isomers) (D-(-)-Ribose) 是 ATP 的糖部分,可作为能量增强剂,被广泛用作慢性疲劳综合症和心肌能量代谢的代谢疗法补充剂。它在蛋白质糖化中具有特性,能够 RAGE 依赖的方式诱导 NF-Κb 炎症。
T15721 Latrunculin A

LAT-A

Others Others
Latrunculin A is a toxin isolated from the red sea sponge Latrunculia magnifica. Latrunculin A binds to actin monomers and it also inhibits polymerization of actin (Kds: 0.1, 0.4, 4.7 μM, and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin, and G-actin, re
T37714 Fuscin

Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-...
T4883 Creatine

Methylguanidoacetic acid,肌酸

Endogenous Metabolite Metabolism
Creatine (Methylguanidoacetic acid) 是一种内源性氨基酸代谢物,在细胞能量中发挥重要作用,尤其是在肌肉和大脑中。

天然产物

Atractyloside potassium salt
Cat.No: T3S0156
Synonym: Atractyloside Dipotassium Salt,苍术苷钾盐,苍术苷二钾盐
Target: Others
Carboxyatractyloside
Cat.No: T8170
Synonym: 羧基苍术苷,Gummiferin,Carboxyatractyloside tripotassium salt
Target: Others
Phosphocreatine disodium hydrate
Cat.No: T4888
Synonym: 磷酸肌酸二钠盐,Phosphocreatine disodium salt hydrate
Target: Others, Endogenous Metabolite
Adenosine 5'-diphosphate sodium salt
Cat.No: T5079
Synonym: 腺苷-5‘-二磷酸钠盐,Adenosine-5'-diphosphate trisodium salt,ADP sodium salt
Target: Others, Endogenous Metabolite
Adenosine 5'-diphosphate
Cat.No: T1723
Synonym: 腺苷5'-二磷酸,Adenosine diphosphate,adenosine pyrophosphate,ADP
Target: Endogenous Metabolite
D-Ribose(mixture of isomers)
Cat.No: T4786
Synonym: D-Ribose,D-(-)-Ribose,D-(-)-核糖
Target: Others, Endogenous Metabolite
Latrunculin A
Cat.No: T15721
Synonym: LAT-A
Target: Others
Fuscin
Cat.No: T37714
Synonym:
Target:
Creatine
Cat.No: T4883
Synonym: Methylguanidoacetic acid,肌酸
Target: Endogenous Metabolite
TargetMol Loading
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