產品描述: TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
靶點:
HDAC9:23 nM (IC50);HDAC7:43 nM (IC50);HDAC5:97 nM (IC50);HDAC4:157 nM (IC50);HDAC8:42000 nM (IC50);HDAC6:82000 nM (IC50);HDAC |
體內研究:
In vivo angiogenesis assay, MDA-MB-231 cells are mixed with growth factor-reduced Matrigel and implanted subcutaneously into the flanks of nude mice. TMP269 (subcutaneous injection; 15 mg/kg; every other day; 10 days) shows an obvious antiangiogenic effect with 76% inhibition of angiogenesis in mice |
參考文獻:
1. Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25. 2. Sinnett-Smith J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71. 3. Kikuchi S, et al. Class IIa HDAC inhibition enhances ER stress-mediated cell death in multiple myeloma. Leukemia. 2015 Sep;29(9):1918-1927. 4. EricSalgado, et al. Volume 503 HDAC9 overexpression confers invasive and angiogenic potential to triple negative breast cancer cells via modulating microRNA-206. Biochemical and Biophysical Research Communications. |
溶解性:
DMSO : 100 mg/mL (194.36 mM; Need ultrasonic) |
保存條件:
2-8℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
1.944 ml |
9.718 ml |
19.436 ml |
5 mM |
0.389 ml |
1.944 ml |
3.887 ml |
10 mM |
0.194 ml |
0.972 ml |
1.944 ml |
50 mM |
0.039 ml |
0.194 ml |
0.389 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。 |