11
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T63327 | PDHK-IN-5 | ||
PDHK-IN-5 是 PDHK 的有效抑制剂,能够作用于 PDHK2 (IC50: 0.006μM) 和 PDHK4 (IC50: 0.0329μM)。其中丙酮酸脱氢酶激酶 (PDHK) 是许多疾病(包括糖尿病和癌症)的药物靶点。PDHK-IN-5 对癌症疾病具有研究潜力。 | |||
T62407 | PDHK-IN-4 | ||
PDHK-IN-4 (Compound 30) 是一种 PDHK 的有效抑制剂,能够作用于 PDHK2 (IC50: 0.0051 μM) 和 PDHK4 (IC50: 0.0122 μM)。其中丙酮酸脱氢酶激酶 (PDHK) 是许多疾病(包括糖尿病和癌症)的有效药物靶点。PDHK-IN-4 具有潜力进行癌症疾病的研究。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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... | |||
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。 |
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。 |