Биологическая активность
JX-06 is a мощный and селективный pyruvate dehydrogenase киназы (PDK) 1/2/3 ингибитор (IC50 values are 28, 49 and 313 nM for PDK2, PDK1 and PDK3, respectively). JX06 Selectively Inhibits Pyruvate Dehydrogenase киназы PDK1 by a Covalent Cysteine Modification. JX06, as a селективный covalent ингибитор of PDK1 in cells, forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme.
Оригинал на английском
JX-06 is a potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 28, 49 and 313 nM for PDK2, PDK1 and PDK3, respectively). JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. JX06, as a selective covalent inhibitor of PDK1 in cells, forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme.
Химические свойства
- CAS №
- 729-46-4
- Брутто-формула
- C₁₀H₁₆N₂O₂S₄
- Мол. масса
- 324.49 г/моль
- SMILES
- S=C(SSC(N1CCOCC1)=S)N2CCOCC2
- Синонимы
- JX-06; JX 06; JX06.
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.