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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4170 |
PKM2-IN-1
PKM2 inhibitor,compound 3k |
PKM | Metabolism |
PKM2-IN-1 (compound 3k) 是丙酮酸激酶 M2 (PKM2) 抑制剂,其IC50=2.95 μM。 | |||
T67900 |
PKM2 inhibitor G
|
PKM | Metabolism |
PKM2 inhibitor G是丙酮酸激酶抑制剂。 | |||
T39984 |
PKM2-IN-3
PKM2-IN-3 |
Others | Others |
PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect. | |||
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。 | |||
T81446 |
PKM2 activator 6
|
Others | Others |
PKM2 activator 6 (Compound Z10) 作为一种PKM2激活剂同时抑制PDK1,其KD值分别为121 μM和19.6 μM。该化合物诱导结直肠细胞发生凋亡,并显著抑制细胞增殖与迁移。通过抑制糖酵解作用,PKM2 activator 6降低DLD-1、HCT-8、HT-29、MCF-10A细胞的增殖,IC50值分别为10.04、2.16、3.57、66.39 μM。 | |||
T72693 |
PKM2 activator 5
|
PKM | Metabolism |
PKM2 activator 5 是一种新型有效的 PKM2 激活剂( AC50:0.316 µM),具有潜在的抗癌活性,可用于研究癌症代谢相关疾病。 | |||
T72692 |
PKM2 activator 4
|
Others | Others |
PKM2 activator 4 是PKM2激活剂,AC50值为 1-10 μM。PKM2 activator 4 可用于癌症的研究, | |||
T61504 |
PKM2 activator 3
|
Others | Others |
PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.) | |||
T79636 |
PKM2-IN-4
|
Others | Others |
PKM2-IN-4 (compound 5C)为PKM2的选择性抑制剂,具有0.35 μM的半抑制浓度(IC50),能够调控丙酮酸依赖的呼吸作用,并诱导线粒体H202的产生和电子传递系统的偶联效应。 | |||
T71867 |
PKM2 inhibitor 2825-0090
|
Others | Others |
PKM2 inhibitor 2825-0090 is a Novel pyruvate kinase M2 (PKM2) inhibitor, reducing tumor growth of NSCLC xenografts in vivo. | |||
T74814 |
PKM2/PDK1-IN-1
|
Others | Others |
PKM2/PDK1-IN-1 是一种紫草素硫醚衍生物,是PKM2/PDK1的双重抑制剂。 PKM2/PDK1-IN-1抑制NSCLC 细胞的增殖,并诱导细胞凋亡 (apoptosis)。 PKM2/PDK1-IN-1 诱导细胞间 ROS 产生,调节凋亡蛋白,参与线粒体和死亡受体通路。 | |||
T4223 |
Mitapivat
PKR-IN-1 |
PKM | Metabolism |
Mitapivat (PKR-IN-1) 是口服具有活性的变构丙酮酸激酶 (pyruvate kinase) 激活剂,其AC50=20 nM。它在广泛的 PKLR 基因型中增加酶活性、蛋白质稳定性和 ATP 水平。它有潜在的恢复 PK 缺乏的糖酵解途径活性的作用。 | |||
T6816 |
DASA-58
|
PKM | Metabolism |
DASA58 是一种有效的丙酮酸激酶M2 (PKM2) 活化剂,其中AC90=680 nM,AC50=38 nM。 | |||
T7214 |
TEPP-46
ML265 |
PKM | Metabolism |
TEPP-46 (ML265) 是选择性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活剂,AC50=92 nM,对 PKM1,PKL 和 PKR 作用较小或没有作用。 | |||
T60102L |
Dimethylaminomicheliolide HCl
|
PKM | Metabolism |
Dimethylaminomicheliolide HCl 具有潜在的抗炎和抗肿瘤活性,通过靶向丙酮酸激酶 2 (PKM2) 和重新连接有氧细胞群来抑制胶质母细胞瘤细胞的增殖。 | |||
T15362 |
FX-11
LDHA Inhibitor FX11 |
Dehydrogenase | Metabolism |
FX-11 (LDHA Inhibitor FX11) 是一种有效的、选择性的和竞争性的乳酸脱氢酶 A (LDHA) 的特异性抑制剂,对LDHA 的Ki 为 8 μM。FX-11 对PKM2 (丙酮酸激酶 M2)具有激活作用。FX-11 可降低 ATP 水平,诱导氧化应激和ROS 生成,可引起细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植过程中表现出抗肿瘤 活性。 | |||
T68986 |
ZINC08383544
|
Others | Others |
ZINC08383544 is a specific pyruvate kinase M2 activator which promotes the formation of PKM2 tetramer. ZINC08383544 effectively blocks PKM2 nuclear translocation, and inhibits the growth of tumor. | |||
T70665 |
PF-06284674
|
Others | Others |
PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator. | |||
T75317 |
Vitamin K5
|
Others | Others |
Vitamin K5,一种光敏剂,对细菌和真菌展现出强效抗菌特性。作为PKM2的特异性抑制剂,其对PKM2、PKM1及PKL的IC50值分别为28、191和120 μM。此外,Vitamin K5能诱导colon 26细胞进入凋亡。因其具备的这些性质,Vitamin K5在感染和癌症研究中有应用,并可作为药品、食品和饮料的防腐剂。 | |||
T77775 |
TP-1454
|
Others | Others |
TP-1454是一种针对PKM2的激活剂,其生化测定的AC50为10 Nm。它可通过作用于T调节细胞来调控肿瘤的免疫反应。 | |||
T79602 |
MTP
|
Autophagy | Autophagy |
MTP作为一种PKM2抑制剂,能够通过激活caspase-3来诱导癌细胞发生凋亡(apoptosis),同时诱导自噬(autophagy)过程并提高ROS的产生量。此外,MTP对JAK2信号传递通路也有抑制作用。该化合物主要用于研究口腔鳞状细胞癌。 | |||
T79637 |
CIAC001
|
Others | Others |
CIAC001是一种丙酮酸激酶PKM2的抑制剂,它展现出了抗神经炎症活性。这种化合物能够抑制LPS诱导的一氧化氮(NO)产生(IC50=2.5 μM),并保护BV-2免疫活性细胞。在小鼠模型中,CIAC001减轻了慢性吗啡引起的成瘾和神经炎症症状。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3376 |
Cynaroside
朝蓟糖甙,Luteoloside,Luteolin 7-β-D-Glucopyranoside,Luteolin 7-O-Glucoside,Luteolin 7-O-β-D-glucoside,木犀草苷,Luteolin 7-glucoside |
Others; Influenza Virus; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Cynaroside (Luteolin 7-O-Glucoside) 是一个抗氧化类黄酮。它还是一种流感依赖 RNA 的RNA 聚合酶抑制剂,IC50为 32 nM。 | |||
T1125 |
Shikonin
NSC 252844,Isoarnebin 4,(+)-Shikonin,紫草素,Alkanna Red,C.I. 75535,Anchusa acid |
TNF; NF-κB; Chloride channel; HIV Protease; PKM | Apoptosis; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome |
Shikonin (Anchusa acid) 属于天然产物,是一种 TMEM16A 氯离子通道抑制剂 (IC50=6.5 μM) 和选择性 PKM2 抑制剂。Shikonin 具有抗肿瘤、抗炎和伤口愈合活性。 | |||
T60581 |
Alkannin
|
Others | Others |
Alkannin 是一种有效且特异性的肿瘤型丙酮酸激酶-M2 (PKM2) 抑制剂,不抑制 PKM1 和丙酮酸激酶-L (PKL)。Alkannin 是一种潜在的抗癌剂。 | |||
T16837 |
SAICAR
|
Others | Others |
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner (EC50: 0.3 mM). |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-03362 |
PKM2 Protein, Rat, Recombinant (His & Myc)
Pkm,Threonine-protein kinase PKM2... |
Rat | Baculovirus Insect Cells |
PKM2 Protein, Rat, Recombinant (His & Myc) is expressed in Baculovirus insect cells with N-10xHis and C-Myc tag. The predicted molecular weight is 61.8 kDa and the accession number is P11980. | |||
TMPH-02871 |
PKM2 Protein, Mouse, Recombinant (His & Myc)
Pkm,Pyruvate kinase muscle isozyme,Pyruvate kinase ... |
Mouse | Baculovirus Insect Cells |
PKM2 Protein, Mouse, Recombinant (His & Myc) is expressed in Baculovirus insect cells with N-10xHis and C-Myc tag. The predicted molecular weight is 61.8 kDa and the accession number is P52480. | |||
TMPY-04465 |
PKM2 Protein, Human, Recombinant (His)
pyruvate kinase, muscle,OIP3,CTHBP,PK3,THBP1,HEL-S-30,TCB, |
Human | E. coli |
PKM2 Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 59 kDa and the accession number is P14618-1. | |||
TMPH-03363 |
PKM2 Protein, Rat, Recombinant (E. coli, His & Myc)
Pyruvate kinase PKM,Tyrosine-protein kinase PKM... |
Rat | E. coli |
PKM2 Protein, Rat, Recombinant (E. coli, His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 62.8 kDa and the accession number is P11980. | |||
TMPH-02872 |
PKM2 Protein, Mouse, Recombinant (E. coli, His & Myc)
Pyruvate kinase PKM,Pkm,Threonine-protein ... |
Mouse | E. coli |
PKM2 Protein, Mouse, Recombinant (E. coli, His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 62.8 kDa and the accession number is P52480. | |||
TMPY-04766 |
PKM2 Protein, Mouse, Recombinant (His)
AL024424,AA414905,Pk3,Pk-3,pyruvate kinase... |
Mouse | Baculovirus Insect Cells |
PKM2 Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 60 kDa and the accession number is P52480-2. | |||
TMPY-04387 |
AKT2 Protein, Human, Recombinant (His & GST)
RAC-β,RAC-BETA,HIHGHH,PKBBETA,PKBβ,PRKBB,PKBB,v-akt murine t... |
Human | Baculovirus Insect Cells |
AKT (AK mouse plus Transforming or Thymoma) is a frequent oncogene expressed in most tissues which includes three isoforms AKT1, AKT2, and AKT3. Hyperactivation of AKT signaling is a central key in many human cancer progressions, through modulating angiogenesis, tumor growth, and cell migration, invasion, metastasis, and chemoresistance. Among all three isoforms, AKT2 is most related to cancer cell invasion, metastasis, and survival. Amplification and overexpression of AKT2 have been shown in ma... |