PDK-1

3-Phosphoinositide-dependent protein kinase 1

PDK-1

Related Products

PDK-1 (3-Phosphoinositide-dependent protein kinase 1), a member of the protein A, G and C (AGC) family of proteins, is a Ser/Thr protein kinase. PDK-1, is the pivotal node in the PI3K pathway, has a key role in insulin and growth-factor signalling through phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B.

PDK-1 is responsible for the regulation of cell proliferation and migration and it also has been found to play a key role in different cancers, pancreatic and breast cancer amongst others. Many cancer-driving mutations induce activation of PDK-1 targets including Akt, S6K (p70 ribosomal S6 kinase) and SGK. Thus, PDK1 is a critical activator of multiple pro-survival and oncogenic protein kinases, for which it has garnered considerable interest as an oncology drug target.

PDK-1 Related Products (29)
Antibodies (2)

By Effects:	Inhibitors (23) Activators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10514

BX795	Inhibitor	99.84%
BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.

HY-14981

GSK2334470	Inhibitor	99.78%
GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC₅₀ of 10 nM.

HY-N0047

Polyphyllin I	Inhibitor	99.89%
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.

HY-11005

BX-912	Inhibitor	99.13%
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC₅₀=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.

HY-15967

PS48	Activator	99.71%
PS48 is an activator of PDK1 with an AC₅₀ of 8 μM.

HY-W998345

SMART1	Inhibitor
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .

HY-13844

PDK1-IN-3	Inhibitor
PDK1-IN-3 (Compound C) is a PDK1 inhibitor, with an IC₅₀ of 34 nM.

HY-N0047R

Polyphyllin I (Standard)	Inhibitor
Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.

HY-124379

TPCK	Inhibitor	98.55%
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats.

HY-10547

OSU-03012	Inhibitor	98.88%
OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC₅₀ of 5 μM.

HY-W005629

Leelamine	Inhibitor	98.36%
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC₅₀ value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells.

HY-14440

MP7	Inhibitor	99.67%
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

HY-121629

PS210	Activator	98.30%
PS210 is a potent and selective PDK1 activator with a K_d of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.

HY-13842

BX517	Inhibitor	≥98.0%
BX517 is a potent and selective inhibitor of PDK1 with IC₅₀ of 6 nM.

HY-114645

PDK1-IN-RS2	Inhibitor	98.50%
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a K_d of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.

HY-13856

(R)-PS210	Inhibitor	98.09%
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC₅₀ value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.

HY-10515

BX-320	Inhibitor	99.4%
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC₅₀ of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.

HY-131962A

PKD-IN-1 dihydrochloride	Inhibitor	99.58%
PKD-IN-1 dihydrochloride (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research.

HY-13851

PS47		98.83%
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48.

HY-156375

PKM2 activator 6	Inhibitor
PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (K_D: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC₅₀: 10.04, 2.16, 3.57, 66.39 μM).

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PDK-1

PDK-1

PDK-1 Related Products (29)

Antibodies (2)

PDK-1 Related Products (29):