產品描述: Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts |
靶點:
Glutaminase C;Glutaminase |
體外研究:
Glutaminase C-IN-1 (Compound 968) (10 μM; 14 d) inhibits cellular transformation in NIH 3T3 cells. Glutaminase C-IN-1 (10 μM; 6 d) blocks the signaling activity of a specific target of Dbl. Glutaminase C-IN-1 blocks the transforming activity of human breast cancer cells. Glutaminase C-IN-1 (10 μM) blocks glutaminolysis in transformed cells. Glutaminase C-IN-1 preferentially binds to the monomeric state of Glutaminase C. Cell Viability Assay Cell Line: MDA-MB231 cells, SKBR3 cells, and NIH 3T3 cells Concentration: 10 μM Incubation Time: 5 h Result: Inhibited cell growth. |
體內研究:
Glutaminase C-IN-1 (Compound 968) (200 μg/mouse; i.p.; daily for 12 days) reduces tumor volume in mice. Animal Model: SCID mice with P493 B lymphoma cells Dosage: 200 μg/mouse Administration: Intraperitoneal injection, daily for 12 days Result: Caused a ~50% reduction in the size of the tumors. |
參考文獻:
1. Wang JB, et al. Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell. 2010 Sep 14;18(3):207-19. 2. Stalnecker CA, et al. Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells. Proc Natl Acad Sci U S A. 2015 Jan 13;112(2):394-9. |
溶解性:
Soluble in DMSO |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
2.103 ml |
10.517 ml |
21.034 ml |
5 mM |
0.421 ml |
2.103 ml |
4.207 ml |
10 mM |
0.21 ml |
1.052 ml |
2.103 ml |
50 mM |
0.042 ml |
0.21 ml |
0.421 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。 |