There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Pyruvate dehydrogenase kinase PDK1 is a metabolic enzyme responsible for switching glucose metabolism from mitochondrial oxidation to aerobic glycolysis in cancer cells, a general hallmark of malignancy termed the Warburg effect. JX06 is a potent, selective and covalent inhibitor of PDK with IC50s of 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively. In A549 cells, JX06 (0-0.6 μM; 72 hours) dose-dependently inhibited the cell growth, and JX06 (0.1-10 μM; 6-24 hours) inhibited PDHA1 phosphorylation in a time- and dose-dependent manner. JX06 (1-10 μM) increased glucose uptake and intracellular ATP level and reduced aerobic glycolysis determined by the lactate production. JX06 (1-10 μM; 24 hours) induced ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR). In A549 xenograft models, JX06 (40-80 mg/kg; i.p. for 21 days) inhibited tumor growth[2].
作用机制
JX06 forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme[2].
JX06/双(吗啉硫代羰基)二硫化物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
PDC (Patient-derived EC cells)
0.5 ×10−6m
To verify the inhibitory effect of JX06-NPs and Met on patient-derived endometrial cancer cells. Results showed that the combination of JX06-NPs and Met had a significantly higher inhibition rate than JX06 or Met alone.
Adv Sci (Weinh). 2022 Mar;9(8):e2104472
Hepa1-6 cells
200 nM
24 hours
JX06 treatment effectively eliminated the increased p-PDHA and lactate levels induced by Prmt3 in Hepa1-6 cells
Cell Death Dis. 2025 Mar 6;16(1):158
Huh7 cells
200 nM
24 hours
JX06 treatment effectively abolished the malignant phenotype induced by PRMT3, including proliferation, migration, and invasion in Huh7 cells
Cell Death Dis. 2025 Mar 6;16(1):158
JX06/双(吗啉硫代羰基)二硫化物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Huh7 xenograft model
Intraperitoneal injection
30 mg/kg
Every 2 days until the end of the study
JX06 treatment attenuated the tumor-promoting role of PRMT3 in HCC
Cell Death Dis. 2025 Mar 6;16(1):158
C57BL/6 male mice
Destabilization of the medial meniscus (DMM)-induced osteoarthritis model
Intraarticular injection
30 mg/ml
Once weekly for 3 weeks
By inhibiting PDK1, cartilage loss is markedly accelerated in DMM-induced OA through ECM degradation and apoptosis of chondrocytes.
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