產品描述: | GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively. |
靶點: |
IC50: 2.6 nM (hLDHA), 43 nM (hLDHB);Dehydrogenase |
體外研究: |
GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells。 |
體內研究: |
Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL。 |
參考文獻: |
1. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.539 ml |
7.697 ml |
15.394 ml |
5 mM |
0.308 ml |
1.539 ml |
3.079 ml |
10 mM |
0.154 ml |
0.77 ml |
1.539 ml |
50 mM |
0.031 ml |
0.154 ml |
0.308 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |