| Identification | Back Directory | [Name]
4,4'-(dithiodicarbonothioyl)dimorpholine | [CAS]
729-46-4 | [Synonyms]
JX 06
Bis(morpholinothiocarbonyl) disulfide
Bis(morpholinocarbonothioyl) persulfide
4,4'-(dithiodicarbonothioyl)dimorpholine
Morpholine, 4,4-(dithiodicarbonothioyl)bis- | [EINECS(EC#)]
211-980-6 | [Molecular Formula]
C10H16N2O2S4 | [MOL File]
729-46-4.mol | [Molecular Weight]
324.51 |
| Hazard Information | Back Directory | [Uses]
JX 06 is a covalent inhibitor of Potent Covalent Pyruvate Dehydrogenase Kinase (PDK). | [Biological Activity]
JX06 is a potentPDK1-selectivecovalent pyruvate dehydrogenase (PDH) kinase (PDHKPDK) inhibitor (PDK1/2/3 IC50 = 49/101/313 nM; PDK4 IC50 >10 μMIC50 >10 μM against >300 other kinases). JX06 inhibits cellular PDK substrate PDHA1 Ser293/232 phosphorylationresulting in reduced aerobic glycolysis and cancer proliferation in cultures (1-10 μM) and in mice in vivo (40-80 mg/kg via daily i.p. injection; A549 & HT-29 xenografts). JX06 is shown to target PDK1 Cys240 for covalent modification. | [in vivo]
JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo[1]. | Animal Model: | A549 subcutaneous xenograft mice[1] | | Dosage: | 40, 80?mg/kg | | Administration: | I.p. injections for 21 days | | Result: | Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.
Well tolerated at the administration dose.
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| [storage]
Store at -20°C |
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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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