| S1274 |
BX-795
|
BX-795 是一種有效的,特異性的PDK1抑制劑,在無(wú)細(xì)胞試驗(yàn)中IC50為6 nM,作用于PDK1比作用于PKA和PKC選擇性分別高140和1600倍。同時(shí),相比于 GSK3β,作用于PDK1的選擇性高出100多倍。BX-795 可通過(guò)抑制 ULK1 來(lái)調(diào)節(jié)自噬。BX-795 還是一種有效的 TBK1 抑制劑,可阻斷 TBK1 和 IKKε,IC 50 值分別為 6 nM 和 41 nM。 |
-
Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791
-
Cell Rep, 2025, 44(7):115972
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
|
|
| S8615 |
Sodium Dichloroacetate (DCA)
|
DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特異性抑制劑,對(duì)PDK2和PDK4的IC50值分別為183和80 μM;可抑制 Na+-K+-2Cl- cotransporter 和線粒體鉀離子通道軸。Sodium dichloroacetate 可增加活性氧的生成,引起癌細(xì)胞凋亡,并抑制腫瘤生長(zhǎng)。 |
-
bioRxiv, 2025, 2025.04.03.647023
-
bioRxiv, 2025, 2025.08.24.671623
-
bioRxiv, 2025, 2023.08.11.552890
|
|
| S0983 |
JX06
|
JX06 是一種細(xì)胞中的 PDK1 的選擇性共價(jià)抑制劑。JX06 可劑量依賴(lài)性地抑制PDK1、PDK2和PDK3,對(duì)應(yīng)的IC50值分別為0.049 μM、0.101 μM 和 0.313 μM。 |
-
Biochem Biophys Res Commun, 2021, 587:153-159
|
|
| F1103 |
PDK1 Antibody [P9M7]
|
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, Pyruvate dehydrogenase kinase isoform 1, PDH kinase 1, PDK1, PDHK1, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial, Pyruvate dehydrogenase kinase isoform 4, PDK4, PDHK4, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial, Pyruvate dehydrogenase kinase isoform 3, PDK3, PDHK3, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial, Pyruvate dehydrogenase kinase isoform 2, PDH kinase 2, PDKII, PDK2, PDHK2 |
|
|
| F0401 |
Phospho-PDK1 (Ser241) Antibody [K13M24]
|
|
|
|
| F2759 |
PDK4 Antibody [C15G7]
|
|
|
|
| F2345 |
PDK2 Antibody [L2A10]
|
|
|
|
| S2949 |
KPLH1130
|
KPLH1130 是丙酮酸脫氫酶激酶(pyruvate dehydrogenase kinase, PDK)的特異性抑制劑,可阻斷巨噬細(xì)胞極化并減弱促炎反應(yīng)。 |
|
|
| S1274 |
BX-795
|
BX-795 是一種有效的,特異性的PDK1抑制劑,在無(wú)細(xì)胞試驗(yàn)中IC50為6 nM,作用于PDK1比作用于PKA和PKC選擇性分別高140和1600倍。同時(shí),相比于 GSK3β,作用于PDK1的選擇性高出100多倍。BX-795 可通過(guò)抑制 ULK1 來(lái)調(diào)節(jié)自噬。BX-795 還是一種有效的 TBK1 抑制劑,可阻斷 TBK1 和 IKKε,IC 50 值分別為 6 nM 和 41 nM。 |
- Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791
- Cell Rep, 2025, 44(7):115972
- EMBO J, 2024, 10.1038/s44318-024-00244-9
|
|
| S8615 |
Sodium Dichloroacetate (DCA)
|
DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特異性抑制劑,對(duì)PDK2和PDK4的IC50值分別為183和80 μM;可抑制 Na+-K+-2Cl- cotransporter 和線粒體鉀離子通道軸。Sodium dichloroacetate 可增加活性氧的生成,引起癌細(xì)胞凋亡,并抑制腫瘤生長(zhǎng)。 |
- bioRxiv, 2025, 2025.04.03.647023
- bioRxiv, 2025, 2025.08.24.671623
- bioRxiv, 2025, 2023.08.11.552890
|
|
| S0983 |
JX06
|
JX06 是一種細(xì)胞中的 PDK1 的選擇性共價(jià)抑制劑。JX06 可劑量依賴(lài)性地抑制PDK1、PDK2和PDK3,對(duì)應(yīng)的IC50值分別為0.049 μM、0.101 μM 和 0.313 μM。 |
- Biochem Biophys Res Commun, 2021, 587:153-159
|
|
| S2949 |
KPLH1130
|
KPLH1130 是丙酮酸脫氫酶激酶(pyruvate dehydrogenase kinase, PDK)的特異性抑制劑,可阻斷巨噬細(xì)胞極化并減弱促炎反應(yīng)。 |
|
|
| F1103 |
PDK1 Antibody [P9M7]
|
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, Pyruvate dehydrogenase kinase isoform 1, PDH kinase 1, PDK1, PDHK1, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial, Pyruvate dehydrogenase kinase isoform 4, PDK4, PDHK4, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial, Pyruvate dehydrogenase kinase isoform 3, PDK3, PDHK3, [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial, Pyruvate dehydrogenase kinase isoform 2, PDH kinase 2, PDKII, PDK2, PDHK2 |
|
|
| F0401 |
Phospho-PDK1 (Ser241) Antibody [K13M24]
|
|
|
|
| F2759 |
PDK4 Antibody [C15G7]
|
|
|
|
| F2345 |
PDK2 Antibody [L2A10]
|
|
|
|