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

CAS: 1684386-71-7 Cat. No.: V656206 分子式: C₂₈H₂₃ClF₂N₄O₄ 分子量: 552.96 PubChem CID: 86280454

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

名前と識別子

異性体SMILES

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

MeSH用語

VER-246608

分子量

552.96

関連ターゲット（人間）

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)

よくある質問

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.