1. PI3K/Akt/mTOR
  2. PDK-1

PDK-1

PDK-1 (phosphoinositide dependent protein kinase-1) is a protein which in humans is encoded by the PDK1 gene. It is implicated in the development and progression of melanomas. PDK-1 is a master kinase, which is crucial for the activation of AKT/PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDK-1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling. More recent data indicate that alteration of PDK-1 is a critical component of oncogenic PI3K signalling in breast cancer, suggesting that inhibition of PDK-1 can inhibit breast cancer progression. PDK-1 has an essential role in regulating cell migration especially in the context of PDK-1 deficiency. PDK-1 is a valid therapeutic target and suggests that PDK-1 inhibitors may be useful to prevent cancer progression and abnormal tissue dissemination.

PDK-1 相关产品 (10):

Cat. No. Product Name Effect Purity
  • HY-18657
    TEPP-46 Activator 99.35%
    TEPP-46 是一种有效的,选择性的丙酮酸激酶 M2 (pyruvate kinase M2) 的激活剂,半数激活浓度 AC50 值为 92 nM,对其他 PKM1,PKL 和 PKR 作用较小或没有作用。
  • HY-10514
    BX795 Inhibitor 99.33%
    BX795 是一种有效的,选择性的 TBK1/PDK1 双重抑制剂,IC50 值为 2 nM/6 nM,对其选择性是对 PKA,PKC,c-Kit,GSK3β 等的 50 多倍。
  • HY-14981
    GSK2334470 Inhibitor 99.87%
    GSK2334470是高效特异性的的PDK1抑制剂,IC50值为10 nM。
  • HY-15967
    PS48 Activator 99.97%
    PS48是一小分子PDK1激动剂,Kd值为10.3uM,特异性结合PDK1的PIF-binding pocket,区别于ATP结合位点。
  • HY-10547
    OSU-03012 99.43%
    OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.
  • HY-N0645
    Dicoumarol Inhibitor 98.70%
    Dicoumarol 是 NAD(P)H: 醌氧化还原酶 1 (NQO1) 和 PDK1 的抑制剂,IC50 值分别为 0.37 和 19.42 μM。
  • HY-14440
    PDK1 inhibitor Inhibitor 99.36%
    PDK1 inhibitor是PDK1抑制剂,有抗肿瘤活性。
  • HY-13842
    BX517 Inhibitor >98.0%
    BX517 是一种有效的,选择性的 PDK1 抑制剂,IC50 值为 6 nM。
  • HY-11005
    BX-912 Inhibitor
    BX-912是PDK1抑制剂,IC50为12 nM,比对PKA,PKC,C-Kit和EGFR的抑制性强10倍。
  • HY-13333
    NVP-BAG956 Inhibitor
    NVP-BAG956(BAG 956)是ATP竞争性PI3K和PDK1双重抑制剂,对PI3K p110 alpha,beta,delta,gamma和PDK1的IC50分别为56,444,34,117和240 nM。