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23

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8500 VLX600

OXPHOS; Mitochondrial Metabolism; Autophagy Apoptosis; Autophagy; Metabolism
VLX600 是一种铁螯合氧化磷酸化抑制剂,是一种细胞渗透性抗癌剂。它通过减少肿瘤细胞中的线粒体氧化磷酸化起作用。
T3713 BAY-876

transporter Metabolism
BAY-876 是口服有效的,选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂(IC50= 2 nM)。BAY-876 对 GLUT1 选择性比 GLUT2,GLUT3 和 GLUT4 高(>130 倍)。BAY-876 对糖酵解代谢和卵巢癌生长也有有效的抑制作用。
T37985 D-Fructose-6-phosphate (sodium salt hydrate)

D-Fructose-6-phosphate (sodium salt hydrate) (643-13-0 free base)

D-Fructose-6-phosphate (sodium salt hydrate) 是由磷酸葡萄糖异构酶将 6-磷酸葡萄糖异构化产生的糖酵解途径的糖中间体,可用于研究癌症。
T0239 Lonidamine

AF1890,氯尼达明,DICA,Diclondazolic Acid

Apoptosis; Hexokinase; Mitochondrial Metabolism Apoptosis; Metabolism
Lonidamine (Diclondazolic Acid) 是一种抗肿瘤药物,是己糖激酶、线粒体丙酮酸载体和质膜单羧酸转运蛋白抑制剂,同时也抑制线粒体复合物 II。
T62758 PKM2 activator 2

PKM Metabolism
PKM2 activator 2是一种丙酮酸激酶 M2(PKM2)激活剂,AC 50 值为 66 nM。PKM2 activator 2具有抗肿瘤增殖和缓解沃伯格效应的作用,通过激活 PKM2 使细胞的糖酵解代谢恢复正常。
T36491 POMHEX

Glucokinase Metabolism
Pomhex 是一种具有抗癌活性的细胞渗透性强效烯醇化酶抑制剂,可用于癌症致死率的研究。Pomhex是一种外消旋混合物,是一种强效且具有选择性的ENO2抑制剂。
T40063 CBR-470-1

Nrf2 Immunology/Inflammation
CBR-470-1 是一种有效的糖酵解磷酸甘油酸激酶1 (PGK1) 抑制剂,通过增加甲基乙二醛的水平来激活 NRF2。 CBR-470-1 是一种非共价的 Nrf2 激活剂,具有神经保护活性,通过激活 Keap1-Nrf2 级联反应来保护 SH-SY5Y 神经元细胞免受 MPP+ 诱导的细胞毒性。
T17224 VER-246608

Dehydrogenase; PDK Metabolism; PI3K/Akt/mTOR signaling
VER-246608 是ATP 竞争性的丙酮酸脱氢酶激酶抑制剂,对PDK-1,PDK-3,PDK-2,和PDK-4的IC50分别为 35 nM,40 nM,84 nM 和 91 nM。
T36953 Naphthofluorescein

Naphthafluorescein

HIF Angiogenesis; Chromatin/Epigenetic
Naphthofluorescein (Naphthafluorescein)是一种 Mint3 抑制剂,具有潜在的抗肿瘤和抗炎活性,抑制 HIF-1 和 Mint3 之间的相互作用,抑制 Mint3 依赖性 HIF-1 活性,抑制癌细胞和巨噬细胞的糖酵解活动,同时未显示出明显的体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针,可用于功能性切伦科夫成像。
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。
T23953 Dactylarin

Altersolanol B

Dactylarin is a cytotoxic antibiotic. Dactylarin isolated from Dactylaria lutea. Dactylarin interacts with thiols, which explains its inhibitory effect on the above glycolytic enzymes.
T76097 Aldolase

Aldolase 是一种糖酵解酶,也是 vATP 酶复合物的组成部分。Aldolase 可使 1,6-二磷酸果糖分解成二羟基丙酮和 3-磷酸甘油醛。
T70032 NCI-006

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.
T76111 Hexokinase (ScHEX1)

Hexokinase(ScHEX1) 是一种糖酵解酶己糖激酶,收到 N-乙酰氨基葡萄糖的抑制。N-乙酰氨基葡萄糖对 Hexokinase(ScHEX1) 的抑制导致其与线粒体外膜分离,而导致 NLRP3炎症小体激活。
T76154 Triosephosphate isomerase

Triosephosphate isomerase (TPI) 是一种能够在糖酵解过程中快速转换磷酸二羟丙酮(dihydroxyacetone phosphate)与D: -甘油醛-3-磷酸(D: -glyceraldehyde-3-phosphate)的酶。其催化位点位于酶的二聚体界面。
T79723 PDK-IN-2

PDK-IN-2(Compound 1F)是一种具有IC50为68 nM的PDK抑制剂。该化合物能够抑制PDK1和PDK4在细胞内的表达,增强线粒体生物能并降低糖酵解表型,同时诱导细胞走向线粒体途径的apoptosis。此外,PDK-IN-2在4T1同基因小鼠模型中能够有效抑制肿瘤生长。
T60858 MOPIPP

MOPIPP 是新型的吲哚基查尔酮,可以透过血脑屏障。MOPIPP 对胶质母瘤细胞的肿瘤进展有抑制作用。MOPIPP 诱导细胞空泡化并增加自噬体数量。MOPIPP 还会触发细胞巨泡式死亡,并且中断葡萄糖摄取和糖酵解代谢。
T76152 Glucose 6-phosphate isomerase

Glucose 6-phosphate isomeras (GPI) 葡萄糖 6-磷酸异构酶,即磷酸葡萄糖异构酶/磷酸葡萄糖异构酶 (PGI) 或磷酸己糖异构酶 (PHI),常用于生化研究。Glucose 6-phosphate isomeras 是一种高度保守的糖酵解酶和二聚酶。Glucose 6-phosphate isomeras 催化葡萄糖-6-磷酸异构成果糖-6-磷酸。
T37119 1,2,3-Trioctanoyl-rac-glycerol-13C3

1,2,3-Trioctanoyl-rac-glycerol-13C3

1,2,3-Trioctanoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2,3-trioctanoyl-rac-glycerol by GC- or LC-MS. 1,2,3-Trioctanoyl-rac-glycerol is a triacylglycerol that contains octanoic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trioctanoyl-rac-glycerol increases hippocampal levels of the glycolytic metabolites glucose 6-phosphate, fructose 6-phosphate, and β-hydroxybutyrate and the seizure threshold in the 6 Hz psychomo...
T79285 TRAP1-IN-1

HSP Cytoskeletal Signaling; Metabolism
TRAP1-IN-1(化合物35)是一种高效、具有高选择性的TRAP1抑制剂,其中TRAP1为Hsp90蛋白质家族中的一种线粒体同源体。该抑制剂对TRAP1的选择性优于Grp94超过250倍,能够破坏TRAP1四聚体的稳定性,并诱导下游蛋白质的降解。此外,TRAP1-IN-1能够抑制线粒体氧化磷酸化复合体(OXPHOS),破坏线粒体膜电位,并促进糖酵解过程。
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。
T35874 CC260

CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...
T35683 2-deoxy-D-Glucose-13C6

2-deoxy-D-Glucose-13C6

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B oste...

化合物

VLX600
Cat.No: T8500
Synonym:
Target: OXPHOS, Mitochondrial Metabolism, Autophagy
BAY-876
Cat.No: T3713
Synonym:
Target: transporter
D-Fructose-6-phosphate (sodium salt hydrate)
Cat.No: T37985
Synonym: D-Fructose-6-phosphate (sodium salt hydrate) (643-13-0 free base)
Target:
Lonidamine
Cat.No: T0239
Synonym: AF1890,氯尼达明,DICA,Diclondazolic Acid
Target: Apoptosis, Hexokinase, Mitochondrial Metabolism
PKM2 activator 2
Cat.No: T62758
Synonym:
Target: PKM
POMHEX
Cat.No: T36491
Synonym:
Target: Glucokinase
CBR-470-1
Cat.No: T40063
Synonym:
Target: Nrf2
VER-246608
Cat.No: T17224
Synonym:
Target: Dehydrogenase, PDK
Naphthofluorescein
Cat.No: T36953
Synonym: Naphthafluorescein
Target: HIF
Pyruvate kinase
Cat.No: T76115
Synonym:
Target:
Dactylarin
Cat.No: T23953
Synonym: Altersolanol B
Target:
Aldolase
Cat.No: T76097
Synonym:
Target:
NCI-006
Cat.No: T70032
Synonym:
Target:
Hexokinase (ScHEX1)
Cat.No: T76111
Synonym:
Target:
Triosephosphate isomerase
Cat.No: T76154
Synonym:
Target:
PDK-IN-2
Cat.No: T79723
Synonym:
Target:
MOPIPP
Cat.No: T60858
Synonym:
Target:
Glucose 6-phosphate isomerase
Cat.No: T76152
Synonym:
Target:
1,2,3-Trioctanoyl-rac-glycerol-13C3
Cat.No: T37119
Synonym: 1,2,3-Trioctanoyl-rac-glycerol-13C3
Target:
TRAP1-IN-1
Cat.No: T79285
Synonym:
Target: HSP
Phosphoglycerate kinase
Cat.No: T76122
Synonym:
Target:
CC260
Cat.No: T35874
Synonym:
Target:
2-deoxy-D-Glucose-13C6
Cat.No: T35683
Synonym: 2-deoxy-D-Glucose-13C6
Target:
Cat. No. Product Name Target Signaling Pathways
T9352 hydrocotarnine

Others Others
hydrocotarnine 是 Cbl 的抑制剂。
T19344 Glycogen, Mussel

α-1,6 葡聚糖,Glycogen

Endogenous Metabolite Metabolism
Glycogen, Mussel 是一种糖酵解的中间产物和高能磷酸盐,它是人类、动物、真菌和细菌的一种能量储存形式。
T4941 D-Fructose-6-phosphate disodium salt

D-FRUCTOSE 6-PHOSPHATE DISODIUM SALT,D-果糖-6-磷酸二钠

Others; Endogenous Metabolite Metabolism; Others
D-Fructose-6-phosphate disodium salt (D-FRUCTOSE 6-PHOSPHATE DISODIUM SALT) 是内源性代谢产物的一种。
T83405 2,3-Diphosphoglyceric acid

2,3-DPG

2,3-Diphosphoglyceric acid (2,3-DPG) 是一种糖酵解途径的中间产物,能够通过变构作用结合并稳定脱氧血红蛋白,从而促进氧气在组织部位的释放。此外,2,3-Diphosphoglyceric acid 与血红蛋白结合,有效降低了其对氧的亲和力。
T75492 Ellipyrone A

Ellipyrone A为一种大环肽,对二肽基肽酶 4 (dipeptidyl peptidase-4: IC50=0.35 mM) 显示出抑制活性,并对α-葡萄糖苷酶 (IC50=0.74 mM) 及α-淀粉酶 (IC50=0.59 mM) 也具有明显的抑制效果,表现出其抗碳水化合物分解的性能。

天然产物

hydrocotarnine
Cat.No: T9352
Synonym:
Target: Others
Glycogen, Mussel
Cat.No: T19344
Synonym: α-1,6 葡聚糖,Glycogen
Target: Endogenous Metabolite
D-Fructose-6-phosphate disodium salt
Cat.No: T4941
Synonym: D-FRUCTOSE 6-PHOSPHATE DISODIUM SALT,D-果糖-6-磷酸二钠
Target: Others, Endogenous Metabolite
2,3-Diphosphoglyceric acid
Cat.No: T83405
Synonym: 2,3-DPG
Target:
Ellipyrone A
Cat.No: T75492
Synonym:
Target:
TargetMol Loading
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