JX06


Catalog No. Size PriceQuantity
M7378-2 2mg solid $85
M7378-10 10mg solid $255
M7378-100 100mg solid $1,530

Description

JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively.

Product information

CAS Number: 729-46-4

Molecular Weight: 324.51

Formula: C10H16N2O2S4

Chemical Name: Bis(morpholinothiocarbonyl) disulfide

Smiles: S=C(SSC(=S)N1CCOCC1)N1CCOCC1

InChiKey: KKVYOWPPMNSLCP-UHFFFAOYSA-N

InChi: InChI=1S/C10H16N2O2S4/c15-9(11-1-5-13-6-2-11)17-18-10(16)12-3-7-14-8-4-12/h1-8H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (308.16 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM. JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR. JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells. JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner. JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells. JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .

In Vivo:

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.

References:

  1. Wenyi S, et, al. JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. Cancer Res. 2015 Nov 15; 75(22): 4923-36.

Products are for research use only. Not for human use.

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