40
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T12499 |
PKR-IN-2
|
PKM | Metabolism |
PKR-IN-2 是丙酮酸激酶PKR 亚型的激活剂,可用于 PKR 功能相关疾病的研究,包括癌症、糖尿病、肥胖、自身免疫性疾病、良性前列腺增生等。 | |||
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。 | |||
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。 | |||
T11765 |
KPLH1130
|
Dehydrogenase; PDK | Metabolism; PI3K/Akt/mTOR signaling |
KPLH1130,一种选择性丙酮酸脱氢酶激酶(PDK)抑制剂,在高脂饮食(HFD)喂养的小鼠中提高了糖耐量。KPLH1130 抑制巨噬细胞极化并减轻了炎症反应。 | |||
T2447 |
AZD7545
|
Dehydrogenase | Metabolism |
AZD7545 是竞争性和选择性的PDHK2抑制剂,能够抑制PDHK1和PDHK2的活性,其IC50值分别为 36.8 nM 和 6.4 nM。 | |||
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。 | |||
T22350 |
JX06
|
Apoptosis; Dehydrogenase; PDK | Apoptosis; Metabolism; PI3K/Akt/mTOR signaling |
JX06 是一种选择性共价PDK 抑制剂,抑制PDK1,PDK2和PDK3,IC50值分别为 49 nM,101 nM 和 313 nM。它以不可逆的方式与半胱氨酸残基共价结合来抑制PDK1活性,具有抗肿瘤活性。 | |||
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。 | |||
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。 | |||
T12412L |
PDK4-IN-1 hydrochloride
|
Apoptosis; PDK | Apoptosis; PI3K/Akt/mTOR signaling |
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物,对丙酮酸脱氢酶激酶 4有抑制作用,IC50为 84 nM,具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏,抗糖尿病和抗癌作用。 | |||
T19783 |
Dehydroabiethylamine
NSC-2955,NSC 2955,Dehydroabietylamine,NSC2955,Leelamine free base,Leelamine,脱氢松香胺 |
P450; PDK | Metabolism; PI3K/Akt/mTOR signaling |
Dehydroabiethylamine (NSC-2955) 是肝脏 CYP2B 活性的诱导剂。 Dehydroabiethylamine 抑制丙酮酸脱氢酶激酶 (PDK) 和细胞内胆固醇转运,具有抗肿瘤活性。 | |||
T0745 |
Disodium monofluorophosphate
Sodium Monofluorophosphate,单氟磷酸钠,NSC248 |
Phosphatase; PKM; Phosphorylase | Metabolism |
Disodium monofluorophosphate (NSC248) 是丙酮酸激酶和碱性磷酸酶的竞争性抑制剂,它也不可逆地抑制磷酸化酶磷酸酶。 | |||
T67900 | PKM2 inhibitor G | PKM | Metabolism |
PKM2 inhibitor G是丙酮酸激酶抑制剂。 | |||
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。 | |||
T15944 |
M77976
|
PDK | PI3K/Akt/mTOR signaling |
M77976 是一种选择性 ATP 竞争丙酮酸脱氢酶激酶 PDK4 抑制剂,对 PDK4 有抑制作用 ,IC50 值为 648 μM。M77976 有用于研究肥胖症和糖尿病。 | |||
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。 | |||
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。 | |||
T69865 |
Mitapivat sulfate
|
||
Mitapivat sulfate, also known as AG-348 sulfate hydrate, is an allosteric activator of Pyruvate Kinase (PK) that may be useful in the treatment of Pyruvate Kinase Deficiency. | |||
T69677 | Mitapivat sulfate anhydrous | ||
Mitapivat sulfate anhydrous is an allosteric activator of Pyruvate Kinase (PK) that may be useful in the treatment of Pyruvate Kinase Deficiency. | |||
T70665 |
PF-06284674
|
||
PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator. | |||
T70418 |
TLN-232
|
||
TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells. | |||
T12498 |
PKR activator 2
|
Others | Others |
PKR activator 2 is a potent activator of pyruvate kinase-R (PKR). | |||
T12497 | PKR activator 1 | Others | Others |
PKR activator 1 is a potent activator of pyruvate kinase-R (PKR). | |||
T71867 |
PKM2 inhibitor 2825-0090
|
||
PKM2 inhibitor 2825-0090 is a Novel pyruvate kinase M2 (PKM2) inhibitor, reducing tumor growth of NSCLC xenografts in vivo. | |||
T75132 | PKR activator 4 | ||
PKR activator 4 (example 7A) 是一种高效的丙酮酸激酶 R (pyruvate kinase R (PKR)) 激活剂,展现出研究血液疾病的潜力。 | |||
T74024 |
2,5-Anhydro-D-glucitol-1,6-diphosphate
|
||
2,5-Anhydro-D-glucitol-1,6-diphosphate 为酵母丙酮酸激酶(Pyruvate Kinase)的有限刺激剂,并可作为 a 型2,5-anhydro-D-mannitol 1,6-bisphosphate的同系物。后者为丙酮酸激酶的有效变构激活剂。 | |||
T12412 |
PDK4-IN-1
|
Others | Others |
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM). | |||
T68986 |
ZINC08383544
|
||
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. | |||
T39753 |
Etavopivat
FT-4202 |
||
Etavopivat is a powerful, specific, orally bioavailable activator of pyruvate kinase (PKR) in red blood cells (RBCs). It exhibits potent properties against sickling. | |||
T60527 | PDHK-IN-3 | ||
PDHK-IN-3 (compound 7) 是有效的丙酮酸脱氢酶激酶(PDHK)抑制剂,对PDHK2的IC50值为0.21μM,对PDHK4的IC50值为1.54 μM。 | |||
T63012 | TM-1 | ||
TM-1 是一种强效的丙酮酸脱氢酶激酶 (PDHK) 抑制剂,能够抑制 PDHK1 (IC50: 2.97 μM) 和 PDHK2 (IC50: 5.2 μM)的活性。TM-1 可以阻断丙酮酸脱氢酶复合物 (PDHC) 磷酸化,并抑制癌细胞增殖。 | |||
T74128 |
NCGC00188636
|
||
NCGC00188636为一新型共价PYK抑制剂,可通过阻断核苷酸与PYK活性位点的结合,应用于不同生物及细胞类型的代谢研究中。 | |||
T72663 |
(Rac)-Etavopivat
(Rac)-FT-4202 |
||
(Rac)-Etavopivat((Rac)-FT-4202) 是Etavopivat 异构体。Etavopivat 是一种具有口服活性的的红细胞丙酮酸激酶-R (PKR) 激活剂,可以用于镰状细胞病和其他血红蛋白疾病研究。 | |||
T73525 |
ML202
|
||
ML202作为一种变构激活剂,针对人丙酮酸激酶M2 (hPK-M2)展现出高度特异性,能够影响磷酸烯醇丙酮酸(PEP)结合的协同性,而对二磷酸腺苷(ADP)的结合几乎无影响。 | |||
T74830 | PDK-IN-1 | ||
PDK-IN-1(compound 7o)是一种针对丙酮酸脱氢酶激酶(PDK)的抑制剂,其对PDK1和HSP90的IC50值分别为0.03和0.1μM。通过靶向PDH/PDK轴,PDK-IN-1能有效降低肿瘤质量。 | |||
T81788 | Mito-SilylDCA | ||
Mito-SilylDCA 是一种针对线粒体网络中的 PDK1 的丙酮酸氢酶激酶抑制剂。这种化合物结合了具有靶向 TPP 部分的 DCA 分子,以及聚乙烯长链与硅基,以实现其对 PDK1 的抑制作用。 | |||
T79637 | CIAC001 | ||
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。 | |||
T37355 |
CAY10703
|
||
Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against perip... | |||
T38357 |
1,3,6,8-Pyrenetetrasulfonic Acid (sodium salt hydrate)
|
||
1,3,6,8-Pyrenetetrasulfonic acid is an intermediate in the synthesis of the color additive pyranine.1It has been used to stabilize intermolecular interactions for the crystallization ofL. mexicanapyruvate kinase.2 1.Jitian, S., White, S.R., Yang, H.-H.W., et al.Conventional high-performance liquid chromatography versus derivative spectrophotometry for the determination of 1,3,6-pyrenetrisulfonic acid trisodium salt and 1,3,6,8-pyrenetetrasulfonic acid tetrasodium salt in the color additive D&C G... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0809 |
Dicoumarol
Dicumarol,双羟香豆素,双香豆素 |
Dehydrogenase; NADPH; PDK | Metabolism; PI3K/Akt/mTOR signaling |
Dicoumarol (Dicumarol) 是一种 NAD(P)H: 醌氧化还原酶 1 和PDK1的抑制剂,它们的IC50值分别为 0.37 和 19.42 μM。 | |||
T3604 |
Sodium dichloroacetate
Sodium Dichloroacetate,DCA,BCA,bichloroacetic acid,二氯乙酸钠,Sodium dichloroacetate (DCA),二氯醋酸酯 |
Apoptosis; Dehydrogenase; Reactive Oxygen Species; PDK | Apoptosis; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling |
Sodium dichloroacetate (BCA) 是癌细胞线粒体中的一种代谢调节剂,具有抗癌活性。它抑制丙酮酸脱氢酶激酶,从而导致肿瘤微环境中的乳酸减少。它增加活性氧的产生并促进癌细胞凋亡,还可作为NKCC 抑制剂。 | |||
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。 | |||
T5213 |
Acetyl phosphate(lithium potassium)
乙酰磷酸锂钾盐,Lithium potassium acetyl phosphate,Acetylphosphoric acid |
Others; Endogenous Metabolite | Metabolism; Others |
Acetyl phosphate lithium potassium (Lithium potassium acetyl phosphate) 是内源性代谢产物的一种。 | |||
T4898 |
Potassium 1-carboxyvinyl hydrogenphosphate
PEP-K,磷酸烯醇丙酮酸单钾盐,Phospho(enol)pyruvic acid monopotassium |
Others; Endogenous Metabolite | Metabolism; Others |
Potassium 1-carboxyvinyl hydrogenphosphate (PEP-K) 是内源性代谢产物的一种。 | |||
T8363 |
DL-Serine
|
PKM | Metabolism |
DL-Serine 是 D-丝氨酸和 L-丝氨酸的混合物,是一种基础代谢物。它具有抗病毒作用,能抑制烟草花叶病毒的增殖。 | |||
T60581 |
Alkannin
|
||
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). |