| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
8.85±0.10(Predicted) | [color ]
white to beige | [InChI]
1S/C25H21F3N6O3/c26-25(27,28)21-9-5-4-8-20(21)24(36)33(14-18-10-12-19(13-11-18)23(35)30-37)16-22-29-31-32-34(22)15-17-6-2-1-3-7-17/h1-13,37H,14-16H2,(H,30,35) | [InChIKey]
MEWDNULKAXEKII-UHFFFAOYSA-N | [SMILES]
FC(F)(C1=CC=CC=C1C(N(CC2=CC=C(C=C2)C(NO)=O)CC3=NN=NN3CC4=CC=CC=C4)=O)F |
| Hazard Information | Back Directory | [Uses]
NR160 is a selective HDAC6 inhibitor with an IC50 value of 30 nM. NR160 shows low cytotoxicity against leukemia cell line. NR160 augments the apoptosis induction of Bortezomib.html" class="link-product" target="_blank">Bortezomib (HY-10227) (proteasome inhibitor), Epirubicin.html" class="link-product" target="_blank">Epirubicin (HY-13624) and Daunorubicin.html" class="link-product" target="_blank">Daunorubicin (HY-13062A) significantly[1][2]. | [Biological Activity]
NR-160 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 0.03 μM).1 It is selective for HDAC6 over HDAC1, -2, -3, -4, and -8 (IC50s = 5.18, 2.26, 8.48, 55.4, and 14.7 μM, respectively). NR-160 is cytotoxic against a panel of seven cancer cell lines (IC50s = 22.5-51.8 μM). It enhances cytotoxicity induced by bortezomib in HL-60 cells, as well as cytotoxicity induced by epirubicin or daunorubicin in CCRF-HSB-2 T cell acute lymphoblastic leukemia cells. | [IC 50]
HDAC6: 30 nM (IC50) | [References]
1.Re?ing, N., S?nnichsen, M., Osko, J.D., et al.Multicomponent synthesis, binding mode, and structure-activity relationship of selective histone deacetylase 6 (HDAC6) inhibitors with bifurcated capping groupsJ. Med. Chem.63(18)10339-10351(2020)
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| Company Name: |
ChemeGen
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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