Enolase (phosphopyruvate hydratase) is a metalloenzyme responsible for the catalysis of the conversion of 2-phosphoglycerate (2-PG) tophosphoenolpyruvate (PEP), the ninth and penultimate step of glycolysis. Enolase belongs to the class Lyase. Enolase can also catalyze the reverse reaction, depending on environmental concentrations of substrates. The optimum pH for this enzyme is 6.5. Enolase is present in all tissues and organisms capable of glycolysis or fermentation. Small-molecule inhibitors of enolase have been synthesized as chemical probes of the catalytic mechanism of the enzyme. The most potent of inhibitors is phosphonoacetohydroxamate, which in its unprotonated form has pM affinity for the enzyme. It has structural similarity to the presumed catalytic intermediate, between PEP and 2-PG. Attempts have been made to use this inhibitor as an anti-trypanosome drug, and more recently, as an anti-cancer agent.
| Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
|---|---|---|---|---|
| KM9623 |
AP-III-a4
ENOblock(AP-III-a4)是第一个非底物类似物，可直接与烯醇酶结合，IC50为0.576 uM，能抑制体内癌细胞转移。 |
1177827-73-4 | ≥98% |
|
| KM9624 |
AP-III-a4 hydrochloride
AP-III-a4 hydrochloride (ENOblock hydrochloride) 能直接与烯醇酶结合，IC50为576nM，还能抑制体内癌细胞转移。 |
2070014-95-6 |
|
|
| KM8108 |
Hex
Hex 是烯醇酶 (enolase) 的抑制剂，其对 ENO2 和 ENO1 的 Ki 值分别为 74.4 nM 和 269.4 nM。 |
2004714-32-1 |
|
|
| KM10757 |
POMHEX
POMHEX 是一个消旋混合物，是具有细胞渗透性的 HEX 的 POM 前体药物，是ENO2 的特异性抑制剂。POMHEX 对ENO1 缺失的细胞表现出低纳摩尔级别活性，并对 ENO1 缺失的肿瘤模型表现出良好的抗癌效果。POMHEX 是有效的糖酵解抑制剂。 |
2004714-34-3 | 98% |
|
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