VER-246608 - 10mM in DMSO , CAS No.1684386-71-7

CAS: 1684386-71-7 Cat. No.: V656206 Fórmula: C₂₈H₂₃ClF₂N₄O₄ Peso molecular: 552.96 PubChem CID: 86280454

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase ( PDK ) with IC 50 s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1 , PDK-3 , PDK-2 , and PDK-4 , respectively.

In Vitro

VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser 293 residue of E1α (phosphorylated by all four PDK isozymes) with IC 50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)

Specifications

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase ( PDK ) with IC 50 s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1 , PDK-3 , PDK-2 , and PDK-4 , respectively.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

• SMILES isoméricas: CC1=CN=C(N=C1C2=CC=C(C=C2)N(CC3=CC=C(C=C3)CNC(=O)C(F)F)C(=O)C4=C(C=C(C=C4)O)O)Cl
• PubChem CID: 86280454
• Termos de entrada MeSH: VER-246608
• Peso molecular: 552.96

Alvos associados (humanos)

PDK4 Tchem [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial (0 Activities)

Discover Target: PDK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDK1 Tchem [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (0 Activities)

Discover Target: PDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDK3 Tchem [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial (0 Activities)

Discover Target: PDK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDK2 Tchem [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial (0 Activities)

Discover Target: PDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Perguntas frequentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1684386-71-7, the molecular formula is C28H23ClF2N4O4, and the molecular weight is 552.96 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.