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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
14 Results for "
PDK-IN-1
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "PDK-IN-1" in MCE Product Catalog:
PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass [1].
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4 Cited Publications
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1 .
PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
Cat. No.: HY-177913
CAS No.: 618068-98-7
OSU-02067 is a selective 3-phosphoinositide-dependent protein kinase-1 (PDK-1) inhibitor (IC50=9 μM). OSU-02067 is promising for research of solid tumors (e.g., prostate, breast, colorectal cancers) [1].
Cat. No.: HY-146977
CAS No.: 2490699-40-4
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases [1].
Cat. No.: HY-184945
CAS No.: 252016-13-0
Research Areas:
PDK ligand-1 (Compound 16) is a target protein ligand that serves as an HsClpP recruitment module for constructing mitochondrially targeted pan-PDK degraders. PDK ligand-1 can be used for the synthesis of Pan-PDK degrader-1 (HY-184943) [1].
Cat. No.: HY-184943
Research Areas:
Pan-PDK degrader-1 is a pan-PDK class PROTAC degrader that degrades PDK2, PDK3 and PDK4 with DC50 values of 9.2 nM, 9.9 nM and 11.5 nM, respectively. Pan-PDK degrader-1 recruits the mitochondrial protease HsClpP and induces selective pan-PDK degradation via HsClpP-mediated proteolysis. Pan-PDK degrader-1 reprograms mitochondrial metabolism toward oxidative phosphorylation, promoting ROS accumulation, mitochondrial permeability transition pore opening, endogenous mitochondrial apoptosis, calreticulin exposure and HMGB1 release. Pan-PDK degrader-1 upregulates cleaved Caspase-9, Caspase-3 and PARP. Pan-PDK degrader-1 inhibits primary and distal tumor growth via selective degradation of PDK in tumor tissues. Pan-PDK degrader-1 can be used for the research of breast cancer [1].
Cat. No.: HY-184944
Target:
Research Areas:
HsClpP-ligand-1 is an intermediate derived from HsClpP ligands, and also serves as an HsClpP recruitment module for constructing mitochondria-targeted pan-PDK degraders. HsClpP-ligand-1 acts as the HsClpP ligand of the bifunctional degrader Pan-PDK degrader-1 (HY-184943) [1].
Cat. No.: HY-10547R
CAS No.: 742112-33-0
Synonyms: AR-12 (Standard); PDK1 INhibitor AR-12 (Standard)
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Research Areas:
OSU-03012 (Standard) is the analytical standard of OSU-03012 (HY-10547). This product is intended for research and analytical applications. OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM [1] .
Cat. No.: HY-L015
1,125 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.
MCE owns a unique collection of 1,125 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
